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Artykuły w czasopismach na temat „Novel Potent Enzyme Inhibitors”

Autor: Grafiati

Data publikacji: 3 czerwca 2025

Data aktualizacji: 31 lipca 2025

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1

Yamali, Cem, Halise Inci Gul, Tahir Cakir, Yeliz Demir, and Ilhami Gulcin. "Aminoalkylated Phenolic Chalcones: Investigation of Biological Effects on Acetylcholinesterase and Carbonic Anhydrase I and II as Potential Lead Enzyme Inhibitors." Letters in Drug Design & Discovery 17, no. 10 (2020): 1283–92. http://dx.doi.org/10.2174/1570180817999200520123510.

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Background: Phenolic Mannich bases have been reported as acetylcholinesterase (AChE) inhibitors for the medication of Alzheimer's disease. Carbonic Anhydrases (CAs) are molecular targets for anticonvulsant, diuretic and antiglaucoma drugs in the clinic. Phenolic compounds have also been mentioned as CA inhibitors. The importance of Mannich bases in drug design inspired our research group to design novel phenolic Mannic bases as potent enzyme inhibitors. Objective: In this study, novel Mannich bases, 1-(3,5-bis-aminomethyl-4-hydroxyphenyl)-3-(4- substitutedphenyl)-2-propen-1-ones (1-9), were de

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2

Pilkington, Leung, and Barker. "Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors." Proceedings 22, no. 1 (2019): 67. http://dx.doi.org/10.3390/proceedings2019022067.

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The phosphatidyl–choline-specific phospholipase C (PC-PLC) enzyme has been shown to be an important enzyme involved in various cell-signaling processes. Furthermore, PC-PLC has been shown to be upregulated in various cancer cell lines, thereby presenting itself as a potential anti-cancer therapeutic target. Current PC-PLC inhibitors, including the literature standard inhibitor D609 possess characteristics making them unsuitable for clinical use. We have discovered a new class of potent PC-PLC inhibitors with much improved activity and drug-like properties than D609. The synthesis and SAR study

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Jeng, Arco Y., Paul Mulder, Aij-Lie Kwan, and Bruno Battistini. "Nonpeptidic endothelin-converting enzyme inhibitors and their potential therapeutic applications." Canadian Journal of Physiology and Pharmacology 80, no. 5 (2002): 440–49. http://dx.doi.org/10.1139/y02-025.

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Endothelins (ETs) are potent vasoconstrictors, promitogens, and inflammatory mediators. They have been implicated in the pathogenesis of various cardiovascular, renal, pulmonary, and central nervous system diseases. Since the final step of the biosynthesis of ETs is catalyzed by a family of endothelin-converting enzymes (ECEs), inhibitors of these enzymes may represent novel therapeutic agents. Currently, seven isoforms of these metalloproteases have been identified; they all share a significant amino acid sequence identity with neutral endopeptidase 24.11 (NEP), another metalloprotease. There

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4

Hassan, Sidra, Pervaiz Ali Channar, Fayaz Ali Larik, et al. "Synthesis of novel ( E )-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5′-nucleotidase inhibitors." Royal Society Open Science 5, no. 9 (2018): 180837. http://dx.doi.org/10.1098/rsos.180837.

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Ecto-5′-nucleotidase (e5′NT), a membrane-bound enzyme and an essential member of ecto-nucleotidases which regulates extracellular purinergic signalling. Their upregulation results in various disease conditions, for example, inflammation, hypoxia and cancer. Therefore, efforts have been made to synthesize potent and selective inhibitors of e5′NT. Here we have synthesized, characterized and evaluated six thiazole derivatives (3a–3f) as potent e5′NT inhibitors. Among all derivatives, the compound ( E )-1-(4-methyl-2-(2-(pyridin-3-ylmethylene)hydrazinyl) thiazol-5-yl)ethanone (3a) exhibited maximu

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5

Wang, Q. May, Robert B. Johnson, Louis N. Jungheim, Jeffrey D. Cohen, and Elcira C. Villarreal. "Dual Inhibition of Human Rhinovirus 2A and 3C Proteases by Homophthalimides." Antimicrobial Agents and Chemotherapy 42, no. 4 (1998): 916–20. http://dx.doi.org/10.1128/aac.42.4.916.

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ABSTRACT The 2A and 3C proteases encoded by human rhinoviruses (HRVs) are attractive targets for antiviral drug development due to their important roles in viral replication. Homophthalimides were originally identified as inhibitors of rhinovirus 3C protease through our screening effort. Previous studies have indicated that the antiviral activity of certain homophthalimides exceeded their in vitro inhibitory activity against the viral 3C protease, suggesting that an additional mechanism might be involved. Reported here is the identification of homophthalimides as potent inhibitors for another

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6

Buryska, Tomas, Lukas Daniel, Antonin Kunka, Jan Brezovsky, Jiri Damborsky, and Zbynek Prokop. "Discovery of Novel Haloalkane Dehalogenase Inhibitors." Applied and Environmental Microbiology 82, no. 6 (2016): 1958–65. http://dx.doi.org/10.1128/aem.03916-15.

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ABSTRACTHaloalkane dehalogenases (HLDs) have recently been discovered in a number of bacteria, including symbionts and pathogens of both plants and humans. However, the biological roles of HLDs in these organisms are unclear. The development of efficient HLD inhibitors serving as molecular probes to explore their function would represent an important step toward a better understanding of these interesting enzymes. Here we report the identification of inhibitors for this enzyme family using two different approaches. The first builds on the structures of the enzymes' known substrates and led to

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7

Hurst, Douglas R., Martin A. Schwartz, Yonghao Jin, et al. "Inhibition of enzyme activity of and cell-mediated substrate cleavage by membrane type 1 matrix metalloproteinase by newly developed mercaptosulphide inhibitors." Biochemical Journal 392, no. 3 (2005): 527–36. http://dx.doi.org/10.1042/bj20050545.

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MT1-MMP (membrane type 1 matrix metalloproteinase, or MMP-14) is a key enzyme in molecular carcinogenesis, tumour-cell growth, invasion and angiogenesis. Novel and potent MMP inhibitors with a mercaptosulphide zinc-binding functionality have been designed and synthesized, and tested against human MT1-MMP and other MMPs. Binding to the MT1-MMP active site was verified by the competitive-inhibition mechanism and stereochemical requirements. MT1-MMP preferred deep P1′ substituents, such as homophenylalanine instead of phenylalanine. Novel inhibitors with a non-prime phthalimido substituent had Ki

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8

Ma, Ling, Jiajia Wen, Biao Dong, et al. "Design and Evaluation of Novel HIV-1 Protease Inhibitors Containing Phenols or Polyphenols as P2 Ligands with High Activity against DRV-Resistant HIV-1 Variants." International Journal of Molecular Sciences 23, no. 22 (2022): 14178. http://dx.doi.org/10.3390/ijms232214178.

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With the increasing prevalence of drug-resistant variants, novel potent HIV-1 protease inhibitors with broad-spectrum antiviral activity against multidrug-resistant causative viruses are urgently needed. Herein, we designed and synthesized a new series of HIV-1 protease inhibitors with phenols or polyphenols as the P2 ligands and a variety of sulfonamide analogs as the P2′ ligands. A number of these new inhibitors showed superb enzymatic inhibitory activity and antiviral activity. In particular, inhibitors 15d and 15f exhibited potent enzymatic inhibitory activity in the low picomolar range, a

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9

Khunluck, Tueanjai, Veerapol Kukongviriyapan, Laddawan Senggunprai, Wutthipong Duangarsong, and Auemduan Prawan. "The Inhibition Kinetics and Potential Anti-Migration Activity of NQO1 Inhibitory Coumarins on Cholangiocarcinoma Cells." Integrative Cancer Therapies 18 (December 25, 2018): 153473541882044. http://dx.doi.org/10.1177/1534735418820444.

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Altered expression of a cytosolic flavoenzyme NAD(P)H:quinone oxidoreductase-1 (NQO1) has been seen in many human tumors. Its remarkable overexpression in cholangiocarcinoma (CCA; an aggressive malignancy of the biliary duct system) was associated with poor prognosis and short survival of the patients. Inhibition of NQO1 has been proposed as a potential strategy to improve the efficacy of anticancer drugs in various cancers including CCA. This study investigated novel NQO1 inhibitors and verified the mechanisms of their enzyme inhibition. Among the different chemical classes of natural NQO1 in

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10

Chu, Ming-Jie, Wei Wang, Zi-Li Ren, et al. "Discovery of Novel Triazole-Containing Pyrazole Ester Derivatives as Potential Antibacterial Agents." Molecules 24, no. 7 (2019): 1311. http://dx.doi.org/10.3390/molecules24071311.

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To develop new antibacterial agents, a series of novel triazole-containing pyrazole ester derivatives were designed and synthesized and their biological activities were evaluated as potential topoisomerase II inhibitors. Compound 4d exhibited the most potent antibacterial activity with Minimum inhibitory concentration (MIC) alues of 4 µg/mL, 2 µg/mL, 4 µg/mL, and 0.5 µg/mL against Staphylococcus aureus, Listeria monocytogenes, Escherichia coli, and Salmonella gallinarum, respectively. The in vivo enzyme inhibition assay 4d displayed the most potent topoisomerase II (IC50 = 13.5 µg/mL) and topo

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11

Brophy, Victoria Hertle, John Vasquez, Richard G. Nelson, John R. Forney, Andre Rosowsky, and Carol Hopkins Sibley. "Identification of Cryptosporidium parvum Dihydrofolate Reductase Inhibitors by Complementation in Saccharomyces cerevisiae." Antimicrobial Agents and Chemotherapy 44, no. 4 (2000): 1019–28. http://dx.doi.org/10.1128/aac.44.4.1019-1028.2000.

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ABSTRACT There is a pressing need for drugs effective against the opportunistic protozoan pathogen Cryptosporidium parvum. Folate metabolic enzymes and enzymes of the thymidylate cycle, particularly dihydrofolate reductase (DHFR), have been widely exploited as chemotherapeutic targets. Although many DHFR inhibitors have been synthesized, only a few have been tested against C. parvum. To expedite and facilitate the discovery of effective anti-Cryptosporidium antifolates, we have developed a rapid and facile method to screen potential inhibitors of C. parvum DHFR using the model eukaryote, Sacch

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12

Baldwin, Jeffrey, Carolyn H. Michnoff, Nicholas A. Malmquist, et al. "High-throughput Screening for Potent and Selective Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase." Journal of Biological Chemistry 280, no. 23 (2005): 21847–53. http://dx.doi.org/10.1074/jbc.m501100200.

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Plasmodium falciparum is the causative agent of the most serious and fatal malarial infections, and it has developed resistance to commonly employed chemotherapeutics. The de novo pyrimidine biosynthesis enzymes offer potential as targets for drug design, because, unlike the host, the parasite does not have pyrimidine salvage pathways. Dihydroorotate dehydrogenase (DHODH) is a flavin-dependent mitochondrial enzyme that catalyzes the fourth reaction in this essential pathway. Coenzyme Q (CoQ) is utilized as the oxidant. Potent and species-selective inhibitors of malarial DHODH were identified b

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13

Vijaya Anand, A., V. Bharathi, G. Bupesh, Jaya Lakshmi, K. Meenakshi Sundaram, and M. Saradhadevi. "Identification of novel potent pancreatic lipase inhibitors from Ficus racemosa." Biomedicine 41, no. 1 (2021): 23–30. http://dx.doi.org/10.51248/.v41i1.528.

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Introduction and Aim: Obesity is a disorder of lipid metabolism and continues to be a global problem, ranking fifth for deaths worldwide. It is considered to be main reason for a number of physiological changes that resulting in many metabolic disorders such as cardiovascular diseases, diabetes, musculoskeletal disorders and various cancer types. Obesity develops from long-termed physiological imbalances in energy expenditure.. One of the therapeutic strategies in managing obesity is inhibition of pancreatic lipase, a key enzyme responsible for the digestion of fats and triglycerides. The aim

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14

Reichau, Sebastian, Wanting Jiao, Scott R. Walker, Richard D. Hutton, Edward N. Baker, and Emily J. Parker. "Potent Inhibitors of a Shikimate Pathway Enzyme from Mycobacterium tuberculosis." Journal of Biological Chemistry 286, no. 18 (2011): 16197–207. http://dx.doi.org/10.1074/jbc.m110.211649.

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Tuberculosis remains a serious global health threat, with the emergence of multidrug-resistant strains highlighting the urgent need for novel antituberculosis drugs. The enzyme 3-deoxy-d-arabino-heptulosonate 7-phosphate synthase (DAH7PS) catalyzes the first step of the shikimate pathway for the biosynthesis of aromatic compounds. This pathway has been shown to be essential in Mycobacterium tuberculosis, the pathogen responsible for tuberculosis. DAH7PS catalyzes a condensation reaction between P-enolpyruvate and erythrose 4-phosphate to give 3-deoxy-d-arabino-heptulosonate 7-phosphate. The en

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15

Aljohani, Ahmed K. B., Waheed Ali Zaki El Zaloa, Mohamed Alswah, et al. "Development of Novel Class of Phenylpyrazolo[3,4-d]pyrimidine-Based Analogs with Potent Anticancer Activity and Multitarget Enzyme Inhibition Supported by Docking Studies." International Journal of Molecular Sciences 24, no. 19 (2023): 15026. http://dx.doi.org/10.3390/ijms241915026.

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Phenylpyrazolo[3,4-d]pyrimidine is considered a milestone scaffold known to possess various biological activities such as antiparasitic, antifungal, antimicrobial, and antiproliferative activities. In addition, the urgent need for selective and potent novel anticancer agents represents a major route in the drug discovery process. Herein, new aryl analogs were synthesized and evaluated for their anticancer effects on a panel of cancer cell lines: MCF-7, HCT116, and HePG-2. Some of these compounds showed potent cytotoxicity, with variable degrees of potency and cell line selectivity in antiproli

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Bashir, Muhammad A., Kulsoom Javaid, Muniza Shaikh, Muhammad I. Choudhary та Hina Siddiqui. "Tyramine Derivatives as Potent Therapeutics for Type 2 Diabetes: Synthesis and In Vitro Inhibition of α-Glucosidase Enzyme". Medicinal Chemistry 16, № 8 (2020): 1124–35. http://dx.doi.org/10.2174/1573406416666200128114422.

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Background: Tyramine derivatives 3-16 were prepared and tested first time for their α- glucosidase (Sources: Saccharomyces cerevisiae) inhibitory activity by using an in vitro mechanismbased biochemical assay. All the compounds were found to be new, except compounds 3, 10-12 and 16. Objective: In continuation of our research to synthesize and identify potent inhibitors of α-glucosidase enzyme, we intended to synthesize new inhibitors of α-glucosidase enzyme with enhanced efficacy in order to provide the basis for the better treatment of the type-II diabetic. Methods: Tyramine (1) was allowed t

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Lipson, Victoria V., Fedyr G. Yaremenko, Volodymyr M. Vakula, et al. "Discovery of Novel N-Acylhydrazone Derivatives as Potent Inhibitors of Sirtuin-1." SynOpen 08, no. 02 (2024): 100–108. http://dx.doi.org/10.1055/s-0043-1763747.

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AbstractSIRT1 enzyme is a key family member of Silent Information Regulators (Sirtuins), which catalyze the deacetylation of proteins. Therefore, developing new SIRT1 inhibitors has potential application in treating cancer disease and age-related metabolic disorders. In this study, we synthesized a series of N-acylhydrazone (NAH) derivatives and performed high-throughput screening of their inhibitory activity against the recombinant SIRT1 protein by a luminescent assay. Using in silico screening, we identified a new NAH derivative that features both selectivity and a high binding affinity towa

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Krinkel, Ben, Mark Slayton, Jin Heon Jeon, et al. "Abstract 6675: Exploiting rewired metabolism in cancer: A biochemical focus on malic enzyme inhibitors using structure-based drug design." Cancer Research 85, no. 8_Supplement_1 (2025): 6675. https://doi.org/10.1158/1538-7445.am2025-6675.

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Abstract Background: Cancer continues to be a formidable adversary, claiming countless lives globally and fueling the pursuit of more effective therapies to enhance treatment outcomes and quality of life. A hallmark of cancer is the reprogramming of cellular metabolism, including the aberrant biosynthesis of essential metabolites that support survival and rapid cellular proliferation. This metabolic shift often involves increased reliance on glutamine as a fuel source and elevated expression of malic enzyme 2 (ME2) within the mitochondria. ME2 catalyzes the generation of pyruvate and NAD(P)H a

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Hejaz, Hatem A. "Synthesis and biological activities of flavonoid sulfamates as steroid sulfatase inhibitors." Journal of Medical pharmaceutical and allied sciences 12, no. 6 (2023): 6170–83. http://dx.doi.org/10.55522/jmpas.v12i6.5576.

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Synthesis of potent flavonoid sulfamate inhibitors of the enzyme steroid sulfatase (STS), a topical target in treating postmenopausal women with hormone-dependent breast cancer, is described in the current article. Novel compounds were examined for estrone sulfatase (E1-STS) inhibition in intact MCF-7 breast cells. The strategies adopted to develop STS inhibitors which, while active in vivo, are devoid of any estrogenicity that would limit their use for breast cancer therapy (e.g. estrone 3-O-sulfamate, EMATE), were broadly successful. Several molecules of flavonoid sulfamates were synthesized

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A Hejaz, Hatem, Atul Purohit, and Barry V L Potter. "Synthesis and biological activities of flavonoid sulfamates as steroid sulfatase inhibitors." Journal of Medical pharmaceutical and allied sciences 12, no. 5 (2023): 6025–37. http://dx.doi.org/10.55522/jmpas.v12i5.5576.

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Synthesis of potent flavonoid sulfamate inhibitors of the enzyme steroid sulfatase (STS), a topical target in treating postmenopausal women with hormone-dependent breast cancer, is described in the current article. Novel compounds were examined for estrone sulfatase (E1-STS) inhibition in intact MCF-7 breast cells. The strategies adopted to develop STS inhibitors which, while active in vivo, are devoid of any estrogenicity that would limit their use for breast cancer therapy (e.g. estrone 3-O-sulfamate, EMATE), were broadly successful. Several molecules of flavonoid sulfamates were synthesized

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Bhattacharya, Saurav, Nillohit Mitra Ray, Mitun Chakraborty, and Nandan Kumar Jana. "In-Silico Structure Based Drug Design of a Potent Inhibitor of Enzyme Lumazine Synthase- A Novel Therapeutic Target for Tuberculosis." Greener Journal of Biological Sciences 3, no. 8 (2013): 299–306. https://doi.org/10.15580/gjbs.2013.8.100713890.

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The biosynthetic pathway of riboflavin is an essential one for Mycobacterium tuberculosis. The inhibitors of the enzymes which are involved in this pathway are not likely to interfere with the enzymes of the mammalian metabolism. So these enzymes could be considered as attractive targets for the development of new drugs against M. tuberculosis. The present study focuses on the enzyme Lumazine synthase (LS) which catalyzes the penultimate step in the riboflavin biosynthesis pathway. The main objective is to search for an inhibitor of LS by virtual screening method. The binding energy of 11 alre

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22

Furbish, Amelia B., Ahmed S. Alford, Pieter Burger, et al. "Identification and Characterization of Novel Small-Molecule SMOX Inhibitors." Medical Sciences 10, no. 3 (2022): 47. http://dx.doi.org/10.3390/medsci10030047.

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The major intracellular polyamines spermine and spermidine are abundant and ubiquitous compounds that are essential for cellular growth and development. Spermine catabolism is mediated by spermine oxidase (SMOX), a highly inducible flavin-dependent amine oxidase that is upregulated during excitotoxic, ischemic, and inflammatory states. In addition to the loss of radical scavenging capabilities associated with spermine depletion, the catabolism of spermine by SMOX results in the production of toxic byproducts, including H2O2 and acrolein, a highly toxic aldehyde with the ability to form adducts

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Khan, Zahra, Izabela Stasik, and Joseph Hayes. "Computer-aided Design of Novel CDK5 Inhibitors; Towards New Treatments of Glioblastoma." Neuro-Oncology 24, Supplement_4 (2022): iv8. http://dx.doi.org/10.1093/neuonc/noac200.035.

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Abstract AIMS Design and statistically optimize an in silico screening protocol; apply the screening protocol to a compound database; in vitro validation of selected inhibitors (isolated CDK5 enzyme binding assay). METHOD Two large compound databases, ZINC15 and Analyticon Discovery, were used to screen for potential CDK5 ATP-binding site inhibitors. They were first filtered using a generated pharmacophore model and then virtually screened using Glide SP docking with a solved CDK5-p25 structure (PDB: 3O0G). The selected candidates were validated using enzyme binding assays to determine their i

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24

Mirgany, Tebyan O., Hanadi H. Asiri, A. F. M. Motiur Rahman, and Mohammed M. Alanazi. "Discovery of 1H-benzo[d]imidazole-(halogenated)Benzylidenebenzohydrazide Hybrids as Potential Multi-Kinase Inhibitors." Pharmaceuticals 17, no. 7 (2024): 839. http://dx.doi.org/10.3390/ph17070839.

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In an effort to develop improved and effective targeted tyrosine kinase inhibitors (TKIs), a series of twelve novel compounds with the structural motif “(E)-4-(((1H-benzo[d]imidazol-2-yl)methyl)amino)-N′-(halogenated)benzylidenebenzohydrazide” were successfully synthesized in three steps, yielding high product yields (53–97%). Among this new class of compounds, 6c and 6h-j exhibited excellent cytotoxic effects against four different cancer cell lines, with half-maximal inhibitory concentration (IC50) values ranging from 7.82 to 21.48 μM. Notably, compounds 6h and 6i emerged as the most potent

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Theodoropoulou, Maria A., Giorgos S. Koutoulogenis, Linlin Zhang, et al. "Identification of a Dual Inhibitor of Secreted Phospholipase A2 (GIIA sPLA2) and SARS-CoV-2 Main Protease." Pharmaceuticals 15, no. 8 (2022): 961. http://dx.doi.org/10.3390/ph15080961.

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The development of novel agents to combat COVID-19 is of high importance. SARS-CoV-2 main protease (Mpro) is a highly attractive target for the development of novel antivirals and a variety of inhibitors have already been developed. Accumulating evidence on the pathobiology of COVID-19 has shown that lipids and lipid metabolizing enzymes are critically involved in the severity of the infection. The purpose of the present study was to identify an inhibitor able to simultaneously inhibit both SARS-CoV-2 Mpro and phospholipase A2 (PLA2), an enzyme which plays a significant role in inflammatory di

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Prasasty, Vivitri Dewi, and Enade Perdana Istyastono. "Structure-Based Design and Molecular Dynamics Simulations of Pentapeptide AEYTR as a Potential Acetylcholinesterase Inhibitor." Indonesian Journal of Chemistry 20, no. 4 (2020): 953. http://dx.doi.org/10.22146/ijc.46329.

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Structure-based virtual screening protocol to identify potent acetylcholinesterase inhibitors was retrospectively validated. The protocol could be employed to examine the potential of designed compounds as novel acetylcholinesterase inhibitors. In a research project designing short peptides as acetylcholinesterase inhibitors, peptide AEYTR emerged as one of the potential inhibitors. This article presents the design of AEYTR assisted by the validated protocol and guided by literature reviews followed by molecular dynamics studies to examine the interactions of the pentapeptide in the binding po

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Barbotte, Laetitia, Abdelhakim Ahmed-Belkacem, Stéphane Chevaliez, et al. "Characterization of V36C, a Novel Amino Acid Substitution Conferring Hepatitis C Virus (HCV) Resistance to Telaprevir, a Potent Peptidomimetic Inhibitor of HCV Protease." Antimicrobial Agents and Chemotherapy 54, no. 6 (2010): 2681–83. http://dx.doi.org/10.1128/aac.01796-09.

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ABSTRACT We characterized a novel substitution conferring moderate resistance to telaprevir, a peptidomimetic inhibitor of hepatitis C virus protease. V36C conferred a 4.0-fold increase in the telaprevir 50% inhibitory concentration in an enzyme assay and a 9.5-fold increase in the replicon model. The replication capacity of a replicon harboring V36C was close to that of the wild-type protease. This case emphasizes the complexity of hepatitis C virus resistance to protease inhibitors.

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ONO, Takashi, Katsutoshi YAMADA, Yukiko CHIKAZAWA та ін. "Characterization of a novel inhibitor of cytosolic phospholipase A2α, pyrrophenone". Biochemical Journal 363, № 3 (2002): 727–35. http://dx.doi.org/10.1042/bj3630727.

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Cytosolic phospholipase A2α (cPLA2α), one of the three subtypes of cPLA2 (α, β and γ), is thought to be a rate-limiting enzyme in eicosanoid biosynthesis. We developed a novel and potent cPLA2α inhibitor with an optically active pyrrolidine, termed pyrrophenone, and characterized this compound in detail using enzyme and cellular assay systems. Pyrrophenone, which shows strong inhibition of cPLA2α activity, is one of the most potent cPLA2α inhibitors reported to date. Similar inhibitory potencies for cPLA2α were obtained from three different assays. The inhibitory activity of pyrrophenone is tw

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Wang, Mu-Xuan, Hong-Wei Qin, Chao Liu, et al. "Synthesis and biological evaluation of thiazolidine-2-thione derivatives as novel xanthine oxidase inhibitors." PLOS ONE 17, no. 5 (2022): e0268531. http://dx.doi.org/10.1371/journal.pone.0268531.

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Xanthine oxidase (XO) is a key enzyme in the generation and development of hyperuricemia. Thiazolidine-2-thione, a typical heterocyclic compound, have been widely used in the field of drug synthesis. In this study, a series of novel thiazolidine-2-thione derivatives were synthesized as XO inhibitors, and the XO inhibitory potencies of obtained compounds were evaluated by in vitro enzyme catalysis. The result shown that compound 6k behaved the strongest XO inhibitory activity with an IC50 value of 3.56 μmol/L, which was approximately 2.5-fold more potent than allopurinol. The structure-activity

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El-Helby, Abdel-Ghany A., Helmy Sakr, Rezk R. A. Ayyad, Khaled El-Adl, Mamdouh M. Ali, and Fathalla Khedr. "Design, Synthesis, In Vitro Anti-cancer Activity, ADMET Profile and Molecular Docking of Novel Triazolo[3,4-a]phthalazine Derivatives Targeting VEGFR-2 Enzyme." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (2018): 1184–96. http://dx.doi.org/10.2174/1871520618666180412123833.

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Background: Extensive studies were reported in the synthesis of several phthalazine derivatives as promising anticancer agents as potent VEGFR-2 inhibitors. Vatalanib (PTK787) was the first anilinophthalazine published derivative as a potent inhibitor of VEGFR. The discovery of vatalanib as a clinical candidate led to the design and synthesis of different anilinophthalazine derivatives as potent inhibitors for VEGFR-2. The objective of present research work is the synthesis of new agents with the same essential pharmacophoric features of the reported and clinically used VEGFR-2 inhibitors (e.g

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Kambo, Konan René, Koffi Charles Kouman, Ludovic Akonan, et al. "QSAR Modelling of Novel Coumarin Derivatives for MAO-B Inhibition." Journal of Pharmaceutical Research International 36, no. 10 (2024): 92–116. http://dx.doi.org/10.9734/jpri/2024/v36i107592.

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We report here the design of new inhibitors against human monoamine oxidase (hMAO-B) as potential treatment of Parkinson’s disease. We have completed computer-aided molecular design of MAO-B inhibitors by In situ modification of the reference crystal structure of 7-(3-chlorobenzyloxy)-4-(methylamino) methyl-coumarin cocrystallized (COU1) in complex with MAO-B (Protein Data Bank (PDB) entry code: 2v61) using MM-PB approach. A QSAR model built for a training set of 29 COUs with reported inhibitory activities (IC50exp) displayed a significant correlation between the computed relative Gibbs free e

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Zhu, Mei, Ling Ma, Biao Dong, et al. "Synthesis and evaluation of potent human immunodeficiency virus 1 protease inhibitors with epimeric isopropanol as novel P1′ ligands." Future Medicinal Chemistry 12, no. 9 (2020): 775–94. http://dx.doi.org/10.4155/fmc-2019-0331.

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Aim: HIV-1 protease inhibitors regimens suffered from a number of drawbacks, among which, the most egregious issue was the growing emergence of drug-resistant strains. Materials & methods: The design strategy of maximizing the protease active site interactions with the inhibitor, especially promoting extensive hydrogen bonding with the protein backbone atoms, might be in favor of combating drug resistance. A series of HIV-1 protease inhibitors that incorporated enantiomeric isopropanols as the P1′ ligands in combination with phenols as the P2 ligands were reported herein. Results: A number

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Habash, Maha, Sami Alshakhshir, Shady Awwad, and Mahmoud Abu-Samak. "The discovery of potential tumor necrosis factor alpha converting enzyme inhibitors via implementation of K Nearest Neighbor QSAR analysis." Pharmacia 70, no. (2) (2023): 247–61. https://doi.org/10.3897/pharmacia.70.e96423.

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Tumor necrosis factor-alpha converting enzyme (TACE) is considered as a pro-inflammatory cytokine which catalyzes the formation of TNF-α from membrane bound TNF-α precursor protein. It has important role in various pathological diseases such as inflammation, anorexia, rheumatoid arthritis, cancer and viral replication. Despite the reporting of a variety of TACE inhibitors of diverse chemical scaffolds whether peptide, peptide-like compounds or others, the bioavailability and pharmacokinetic problems are reflected strongly on its clinical effectiveness. In this effort we employed a novel combin

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Shahin, Afnan I., Sumera Zaib, Seyed-Omar Zaraei, et al. "Design and synthesis of novel anti-urease imidazothiazole derivatives with promising antibacterial activity against Helicobacter pylori." PLOS ONE 18, no. 6 (2023): e0286684. http://dx.doi.org/10.1371/journal.pone.0286684.

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Urease enzyme is a known therapeutic drug target for treatment of Helicobacter pylori infection due to its role in settlement and growth in gastric mucosa. In this study, we designed a new series of sulfonates and sulfamates bearing imidazo[2,1-b]thiazole scaffold that exhibit a potent inhibitory activity of urease enzyme. The most potent compound 2c inhibited urease with an IC50 value of 2.94 ± 0.05 μM, which is 8-fold more potent than the thiourea positive control (IC50 = 22.3 ± 0.031 μM). Enzyme kinetics study showed that compound 2c is a competitive inhibitor of urease. Molecular modeling

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Alici, Hakan, Senol Topuz, Kadir Demir, Parham Taslimi, and Hakan Tahtaci. "Synthesis, Biological Evaluation, and In Silico Characterization of Novel Imidazothiadiazole–Chalcone Hybrids as Multi-Target Enzyme Inhibitors." Pharmaceuticals 18, no. 7 (2025): 962. https://doi.org/10.3390/ph18070962.

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Background/Objectives: The need for dual-targeted enzyme inhibitors is critical in addressing complex diseases like Alzheimer’s and glaucoma. Imidazothiadiazole and chalcone moieties are known for diverse bioactivities. This study aimed to develop novel imidazothiadiazole–chalcone hybrids as potential inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase isoforms (hCAs), specifically hCA I and hCA II. Methods: Four hybrid molecules (8a–8d) were synthesized and structurally confirmed via 1H NMR, 13C NMR, FT-IR, MS, and elemental analysis technique

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36

Rodríguez-Lozada, Josué, Erika Tovar-Gudiño, Juan Guevara-Salazar, et al. "QSAR and Molecular Docking Studies of the Inhibitory Activity of Novel Heterocyclic GABA Analogues over GABA-AT." Molecules 23, no. 11 (2018): 2984. http://dx.doi.org/10.3390/molecules23112984.

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We have previously reported the synthesis, in vitro and in silico activities of new GABA analogues as inhibitors of the GABA-AT enzyme from Pseudomonas fluorescens, where the nitrogen atom at the γ-position is embedded in heterocyclic scaffolds. With the goal of finding more potent inhibitors, we now report the synthesis of a new set of GABA analogues with a broader variation of heterocyclic scaffolds at the γ-position such as thiazolidines, methyl-substituted piperidines, morpholine and thiomorpholine and determined their inhibitory potential over the GABA-AT enzyme from Pseudomonas fluoresce

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37

Han, Haozhen, Chunpu Li, Man Li, et al. "Design, Synthesis, and Biological Evaluation of 8-Mercapto-3,7-Dihydro-1H-Purine-2,6-Diones as Potent Inhibitors of SIRT1, SIRT2, SIRT3, and SIRT5." Molecules 25, no. 12 (2020): 2755. http://dx.doi.org/10.3390/molecules25122755.

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Sirtuins (SIRT1-7) are a family of NAD+-dependent deacetylases. They regulate many physiological processes and play important roles in inflammation, diabetes, cancers, and neurodegeneration diseases. Sirtuin inhibitors have potential applications in the treatment of neurodegenerative diseases and various cancers. Herein, we identified new sirtuin inhibitors based on the scaffold of 8-mercapto-3,7-dihydro-1H-purine-2,6-dione. To elucidate the inhibitory mechanism, the binding modes of the inhibitors in SIRT3 were established by molecular docking, showing that the inhibitors occupy the acetyl ly

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Cheng, X. M., S. S. Nikam, and A. M. Doherty. "Development of Agents to Modulate the Effects of Endothelin." Current Medicinal Chemistry 1, no. 4 (1994): 271–312. http://dx.doi.org/10.2174/092986730104220215154628.

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Abstract: Due partly to a greater understanding of the role of regulatory peptides and proteins in the pathophysiology of human disease there is considerable interest in designing agents that will modulate their effects. Endothelin-1 and its isopeptides belong to a family of novel vasoconstrictor agents first isolated from porcine aortic endothelial cells and subsequently found to be secreted from a variety of cell types. These peptides have potent biological effects on cardiovascular, renal, endocrine and neurological function. The rational design of receptor agonists and antagonists or proce

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39

Dr., M. Ajitha Raj* N. Sandhya Rani2. "In-Silico studies of Novel 4, 6-diphenylpyrimidine substituted Benzamide derivatives on HDAC enzymes." Journal of Pharma Research 11, no. 03 (2022): 15–25. https://doi.org/10.5281/zenodo.6844684.

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<strong><em>ABSTRACT</em></strong> <strong>The present study attempts to investigate the 4,6-diphenylpyrimidine substituted benzamide derivatives that act as HDAC inhibitors. Histone deacetylases (HDACs) have been widely recognized as promising targets for cancer treatment. It has been three decades ago, that the first potent Zn2+ dependent histone deacetylase inhibitor was recognized. Meanwhile, to date, SAHA (Vorinostat), Belinostat (PXD-101), Panobinostat (LBH-589), and Romidepsin (FK-228) four HDAC inhibitors have been approved by FDA for cancer chemotherapy, while more than 10 HDAC inhibi

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40

Habash, Maha, Sami Alshakhshir, Shady Awwad, and Mahmoud Abu-Samak. "The discovery of potential tumor necrosis factor alpha converting enzyme inhibitors via implementation of K Nearest Neighbor QSAR analysis." Pharmacia 70, no. 2 (2023): 247–61. http://dx.doi.org/10.3897/pharmacia.70.e96423.

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Tumor necrosis factor-alpha converting enzyme (TACE) is considered as a pro-inflammatory cytokine which catalyzes the formation of TNF-α from membrane bound TNF-α precursor protein. It has important role in various pathological diseases such as inflammation, anorexia, rheumatoid arthritis, cancer and viral replication. Despite the reporting of a variety of TACE inhibitors of diverse chemical scaffolds whether peptide, peptide-like compounds or others, the bioavailability and pharmacokinetic problems are reflected strongly on its clinical effectiveness. In this effort we employed a novel combin

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41

Herman, Bianka Edina, János Gardi, János Julesz, et al. "Steroidal ferrocenes as potential enzyme inhibitors of the estrogen biosynthesis." Biologia Futura 71, no. 3 (2020): 249–64. http://dx.doi.org/10.1007/s42977-020-00023-7.

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Abstract The potential inhibitory effect of diverse triazolyl-ferrocene steroids on key enzymes of the estrogen biosynthesis was investigated. Test compounds were synthesized via copper-catalyzed cycloaddition of steroidal azides and ferrocenyl-alkynes using our efficient methodology published previously. Inhibition of human aromatase, steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities was investigated with in vitro radiosubstrate incubations. Some of the test compounds were found to be potent inhibitors of the STS. A compound bearing ferrocenyl side chai

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Radimerski, Thomas, Fabienne Baffert, Catherine H. Regnier, et al. "Novel, Potent and Selective JAK2 Inhibitors." Blood 114, no. 22 (2009): 3777. http://dx.doi.org/10.1182/blood.v114.22.3777.3777.

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Abstract Abstract 3777 Poster Board III-713 The recent discovery of an acquired activating point mutation in JAK2, substituting valine at amino acid position 617 for phenylalanine, has greatly improved our understanding of the molecular mechanism underlying chronic myeloproliferative neoplasms. Strikingly, the JAK2V617F mutation is found in nearly all patients suffering from polycythemia vera and in roughly every second patient suffering from essential thrombocythemia and from primary myelofibrosis. Thus, JAK2 represents a promising target for the treatment of myeloproliferative disorders and

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Vardhan, D. M. Suyoga, H. K. Kumara, H. Pavan Kumar, and D. Channe Gowda. "INHIBITION OF UREASE ENZYME ACTIVITY BY UREA AND THIOUREA DERIVATIVES OF DIPEPTIDES CONJUGATED 2, 3-DICHLOROPHENYL PIPERAZINE." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 9 (2017): 92. http://dx.doi.org/10.22159/ijpps.2017v9i9.19425.

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Objective: Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs used in a variety of physiological conditions. In search of novel urease enzyme inhibitors, four dipeptides were synthesized, conjugated to 2,3-dichlorophenyl piperazine analogue and converted into urea/thiourea derivatives.Methods: The peptides were synthesized by solution phase method and conjugated to 2,3-dichlorophenyl piperazine (PZN) using 1-ethyl-3-(3-dimethyl aminopropyl)carbodiimide (EDCI)/hydroxybenzotriazole (HOBt) as a coupling agent a

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Preuss, Janina, Adam D. Richardson, Anthony Pinkerton, et al. "Identification and Characterization of Novel Human Glucose-6-Phosphate Dehydrogenase Inhibitors." Journal of Biomolecular Screening 18, no. 3 (2012): 286–97. http://dx.doi.org/10.1177/1087057112462131.

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Glucose-6-phosphate dehydrogenase (G6PD) is the key enzyme of the pentose phosphate pathway, converting glucose-6-phosphate to 6-phosphoglucono-δ-lactone with parallel reduction of NADP+. Several human diseases, including cancer, are associated with increased G6PD activity. To date, only a few G6PD inhibitors have been available. However, adverse side effects and high IC50 values hamper their use as therapeutics and basic research probes. In this study, we developed a high-throughput screening assay to identify novel human G6PD (hG6PD) inhibitors. Screening the LOPAC (Sigma-Aldrich; 1280 compo

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Rullo, Rosario, Carmen Cerchia, Rosarita Nasso, et al. "Novel Reversible Inhibitors of Xanthine Oxidase Targeting the Active Site of the Enzyme." Antioxidants 12, no. 4 (2023): 825. http://dx.doi.org/10.3390/antiox12040825.

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Xanthine oxidase (XO) is a flavoprotein catalysing the oxidation of hypoxanthine to xanthine and then to uric acid, while simultaneously producing reactive oxygen species. Altered functions of XO may lead to severe pathological diseases, including gout-causing hyperuricemia and oxidative damage of tissues. These findings prompted research studies aimed at targeting the activity of this crucial enzyme. During the course of a virtual screening study aimed at the discovery of novel inhibitors targeting another oxidoreductase, superoxide dismutase, we identified four compounds with non-purine-like

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Chehardoli, Gholamabbas, Fatemeh Karimi, Tahmineh Akbarzadeh, Roshanak Hariri, and Zahra Najafi. "Novel 2-Amino-pyrano[3,2-c]quinoline-3-carbonitrile Derivatives Bearing Benzyloxy Phenyl Moiety as Butyrylcholinesterase Inhibitors: Design, Synthesis, In Vitro Evaluation, and Molecular Docking Studies." Avicenna Journal of Pharmaceutical Research 3, no. 2 (2022): 82–90. http://dx.doi.org/10.34172/ajpr.1068.

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Background: Alzheimer’s disease (AD), the main form of dementia, is a multifactorial neurodegenerative disease, and several hypotheses have been proposed for its pathogenesis. Among them, cholinergic hypofunction is the main reason and plays a significant role in cognitive impairment. According to this theory, ChE inhibitors improve the performance of the cholinergic system and increase memory function. Thus, this study investigated a novel series of 2-amino-pyrano[3,2-c]quinoline-3-carbonitrile derivatives bearing benzyloxy phenyl moiety as ChE enzyme inhibitors. Methods: The synthesized comp

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47

Wegener, Dennis, Christian Hildmann, Daniel Riester, et al. "Identification of novel small-molecule histone deacetylase inhibitors by medium-throughput screening using a fluorigenic assay." Biochemical Journal 413, no. 1 (2008): 143–50. http://dx.doi.org/10.1042/bj20080536.

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HDACs (histone deacetylases) are considered to be among the most important enzymes that regulate gene expression in eukaryotic cells. In general, increased levels of histone acetylation are associated with increased transcriptional activity, whereas decreased levels are linked to repression of gene expression. HDACs associate with a number of cellular oncogenes and tumour-suppressor genes, leading to an aberrant recruitment of HDAC activity, which results in changes of gene expression, impaired differentiation and excessive proliferation of tumour cells. Therefore HDAC inhibitors are efficient

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Bitonti, A. J., P. J. Casara, P. P. McCann, and P. Bey. "Catalytic irreversible inhibition of bacterial and plant arginine decarboxylase activities by novel substrate and product analogues." Biochemical Journal 242, no. 1 (1987): 69–74. http://dx.doi.org/10.1042/bj2420069.

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Arginine decarboxylase (ADC) activity from Escherichia coli and two plant species (oats and barley) was inhibited by five new substrate (arginine) and product (agmatine) analogues. The five compounds, (E)-alpha-monofluoromethyldehydroarginine (delta-MFMA), alpha-monofluoromethylarginine (MFMA), alpha-monofluoromethylagatine (FMA), alpha-ethynylagmatine (EA) and alpha-allenylagmatine (AA), were all more potent inhibitors of ADC activity than was alpha-difluoromethylarginine (DFMA), the only irreversible inhibitor of this enzyme described previously. The inhibition caused by the five compounds w

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Focher, F., A. Verri, S. Spadari, R. Manservigi, J. Gambino, and G. E. Wright. "Herpes simplex virus type 1 uracil-DNA glycosylase: isolation and selective inhibition by novel uracil derivatives." Biochemical Journal 292, no. 3 (1993): 883–89. http://dx.doi.org/10.1042/bj2920883.

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We have purified Herpes simplex type 1 (HSV1) uracil-DNA glycosylase from the nuclei of HSV1-infected HeLa cells harvested 8 h post-infection, at which time the induction of the enzyme is a maximum. The enzyme has been shown to be distinct from the host enzyme, isolated from HeLa cells, by its lack of sensitivity to a monoclonal antibody to human uracil-DNA glycosylase. Furthermore, several uracil analogues were synthesized and screened for their capacity to discriminate between the viral and human uracil-DNA glycosylases. Both enzymes were inhibited by 6-(p-alkylanilino)uracils, but the viral

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Firooznia, Fariborz, Candido Gude, Kenneth Chan, et al. "Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors." Bioorganic & Medicinal Chemistry Letters 11, no. 3 (2001): 375–78. http://dx.doi.org/10.1016/s0960-894x(00)00657-0.

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