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Journal articles on the topic 'Telmisartan is pharmacologically active molecule'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Premchand, Patil Deepak V. Nagarale and Bhata R. Chaudhari*. "RECENT ADVANCES AND APPLICATIONS OF TELMISARTAN." Indo American Journal of Pharmaceutical Sciences 04, no. 10 (2017): 3935–45. https://doi.org/10.5281/zenodo.1035249.

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Telmisartan is pharmacologically active molecule, Here we reviewed some synthetic methods and their application like angiotensin II receptor, quantitative determination for the biological activity using NMR, restrict NFAT nuclear translocation and etc..

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Pingali, Subramanya, James P. Donahue, and Florastina Payton-Stewart. "Tetrahydroberberine, a pharmacologically active naturally occurring alkaloid." Acta Crystallographica Section C Structural Chemistry 71, no. 4 (2015): 262–65. http://dx.doi.org/10.1107/s2053229615004076.

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Tetrahydroberberine (systematic name: 9,10-dimethoxy-5,8,13,13a-tetrahydro-6H-benzo[g][1,3]benzodioxolo[5,6-a]quinolizine), C20H21NO4, a widely distributed naturally occurring alkaloid, has been crystallized as a racemic mixture about an inversion center. A bent conformation of the molecule is observed, with an angle of 24.72 (5)° between the arene rings at the two ends of the reduced quinolizinium core. The intermolecular hydrogen bonds that play an apparent role in crystal packing are 1,3-benzodioxole –CH2...OCH3and –OCH3...OCH3interactions between neighboring molecules.

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3

Motterlini, Roberto, Philip Sawle, Sandip Bains, et al. "CORM‐A1: a new pharmacologically active carbon monoxide‐releasing molecule." FASEB Journal 19, no. 2 (2004): 1–24. http://dx.doi.org/10.1096/fj.04-2169fje.

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4

Parmar, Dixit, Lena Henkel, Josef Dib, and Magnus Rueping. "Iron catalysed cross-couplings of azetidines – application to the formal synthesis of a pharmacologically active molecule." Chemical Communications 51, no. 11 (2015): 2111–13. http://dx.doi.org/10.1039/c4cc09337b.

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A protocol for the cross-coupling of azetidines with aryl, heteroaryl, vinyl and alkyl Grignard reagents has been developed under iron catalysis. In addition, a short formal synthesis of a pharmacologically active molecule was demonstrated.

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5

Patel, Navin B., and Imran H. Khan. "Synthesis of 1,2,4-triazole derivatives containing benzothiazoles as pharmacologically active molecule." Journal of Enzyme Inhibition and Medicinal Chemistry 26, no. 4 (2011): 527–34. http://dx.doi.org/10.3109/14756366.2010.535794.

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Terekhova, Irina, Iliya Kritskiy, Mikhail Agafonov, Roman Kumeev, Carlos Martínez-Cortés, and Horacio Pérez-Sánchez. "Selective Binding of Cyclodextrins with Leflunomide and Its Pharmacologically Active Metabolite Teriflunomide." International Journal of Molecular Sciences 21, no. 23 (2020): 9102. http://dx.doi.org/10.3390/ijms21239102.

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The selectivity of encapsulation of leflunomide and teriflunomide by native α-, β- and γ-cyclodextrins was investigated through 1H NMR and molecular modeling. Thermodynamic analysis revealed the main driving forces involved in the binding. For α-cyclodextrin, the partial encapsulation was obtained while deep penetration was characterized for the other two cyclodextrins, where the remaining polar fragment of the molecule is located outside the macrocyclic cavity. The interactions via hydrogen bonding are responsible for high negative enthalpy and entropy changes accompanying the complexation of

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Manish S. Junagade and Anju Goyal. "‘Mutual Prodrug’ and approach to increase the effectiveness of Non-Steroidal Anti-inflammatory Drugs." World Journal of Biological and Pharmaceutical Research 1, no. 1 (2021): 035–45. http://dx.doi.org/10.53346/wjbpr.2021.1.1.0011.

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A clinically useful drug may have limitations in practice because of undesirable side effects, poor solubility, and poor bioavailability, short duration of action, first-pass effect, poor absorption & adverse effects. There are increased efforts in research to increase the therapeutic efficacy of drugs by eliminating or minimizing the undesirable properties of drug molecules. Some of the problems can be solved using a formulation development approach but in some cases, chemical modification in the molecule is necessary to correct the pharmacokinetic parameters. One of the approaches to con

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Manikkam, Rajalakshmi. "Molecular docking analysis of quercetin with known CoVid-19 targets." Bioinformation 19, no. 11 (2023): 1081–85. http://dx.doi.org/10.6026/973206300191081.

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Combat and care during CoVid-19 was non-trivial. Therefore, it is of interest to use the pharmacologically active plant component quercetin for the treatment of CoVid-19. Quercetin exhibits favourable ADMET values and abides by Lipinski's rule of five. When quercetin and remdesivir were positioned in relation to the CoVid-19 targets, quercetin exhibited a greater propensity for binding and H-bond interaction in their molecular interactions. Thus, the quercetin molecule can be used to manage CoVid-19.

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Jiao, Luzhen, Dawei Teng, Zixuan Wang, and Guorui Cao. "Silver Catalyzed Site-Selective C(sp3)−H Bond Amination of Secondary over Primary C(sp3)−H Bonds." Molecules 27, no. 19 (2022): 6174. http://dx.doi.org/10.3390/molecules27196174.

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Sulfamates are widespread in numerous pharmacologically active molecules. In this paper, Silver/Bathophenanthroline catalyzed the intramolecular selective amination of primary C(sp3)−H bonds and secondary C(sp3)−H bonds of sulfamate esters, to produce cyclic sulfamates in good yields and with a high site-selectivity. DFT calculations revealed that the interaction between sulfamates and L10 makes the molecule more firmly attached to the catalyst, benefiting the catalysis reaction. The in vitro anticancer activity of the final products was evaluated in MCF-7 breast cancer cells.

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10

Kiseleva, E. A., S. G. Krylova, T. N. Povet`eva, et al. "Study Into Antinociceptive Activity of a New Molecule from the Class of Hexaazaizowurzitane." Journal Biomed 19, no. 1 (2023): 61–72. http://dx.doi.org/10.33647/2074-5982-19-1-61-72.

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In this work, we studied the pharmacological activity of a newly-synthesized compound 4-(3,4- dibromothiophenylcarbonyl)-10-(2-ethoxyacetyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane (M3) using somatogenic pain models of various genesis (thermal and visceral pain, mechanical compression of a paw). The compound showed a high antinociceptive efficacy, comparable to or exceeding that of tramadol. It was shown that the new molecule from the class of hexaazaisowurtzitane effectively blocks nociceptive reactions at the supraspinal and peripheral levels of pain se

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Nguyen, Truong Thai Ha, Bao G. Huynh, Duy L. Nguyen, Thuy TH Dao, and Tuong M. Ho. "#39 : Identification of Pharmacologically Active Small Molecules that Induce Spheroid Attachment and Embryo Implantation In Vitro and In Vivo." Fertility & Reproduction 05, no. 04 (2023): 492. http://dx.doi.org/10.1142/s2661318223742613.

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Background and Aims: Human endometrium is receptive to embryo implantation during the mid-secretory phase of the menstrual cycle. The in vitro spheroid-endometrial epithelial cells co-culture model was used in this study. We hypothesized that the small molecules from thelibrary of pharmacologically active compounds (LOPAC) can effectively enhance embryo implantation. Method: We established a high-throughput in-vitro spheroid-endometrial epithelial (BeWo-Ishikawa) cells coculture model to screen 1280 LOPAC. The top 20 small molecules which increased spheroid attachment rate were further studied

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Masamrekh, R. A., A. V. Kuzikov, T. A. Filippova, K. A. Sherbakov, A. V. Veselovsky, and V. V. Shumyantseva. "The interactions of abiraterone and its pharmacologically active metabolite D4A with cytochrome P450 2C9 (CYP2C9)." Biomeditsinskaya Khimiya 68, no. 3 (2022): 201–11. http://dx.doi.org/10.18097/pbmc20226803201.

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Interactions of cytochrome P450 2C9 (CYP2C9) were studied with the antitumor drug abiraterone and its pharmacologically active metabolite D4A, promising as an agent for prostate cancer treatment. It was shown by absorption spectroscopy, that both investigated compounds induced spectral changes of CYP2C9, indicating interactions of the pyridine nitrogen atom with the heme iron ion of the active site of the enzyme, but interactions of the ligands with the enzyme could be mediated by a water molecule bound to the heme iron ion. Based on the spectral changes, the values of dissociation constants (

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13

Sturm, Sonja, Christina Högner, Christoph Seger, and Hermann Stuppner. "Combining HPLC-DAD-QTOF-MS and HPLC-SPE-NMR to Monitor In Vitro Vitetrifolin D Phase I and II Metabolism." Metabolites 11, no. 8 (2021): 529. http://dx.doi.org/10.3390/metabo11080529.

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By combining HPLC-DAD-QTOF-MS and HPLC-SPE-NMR, the in vitro metabolism of vitetrifolin D, a pharmacologically active key molecule from Vitex agnus-castus in liver cell fractions, was investigated. Twenty-seven phase I and phase II metabolites were tentatively identified from the culture broth by HPLC-DAD-QTOF-MS. The subsequent HPLC-SPE-NMR analysis allowed for the unequivocal structural characterization of nine phase I metabolites. Since the preparative isolation of the metabolites was avoided, the substance input was much lower than in conventional strategies. The study did prove that the u

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14

Parmar, Dixit, Lena Henkel, Josef Dib, and Magnus Rueping. "ChemInform Abstract: Iron Catalyzed Cross-Couplings of Azetidines - Application to the Formal Synthesis of a Pharmacologically Active Molecule." ChemInform 46, no. 25 (2015): no. http://dx.doi.org/10.1002/chin.201525136.

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15

Thenin-Houssier, Suzie, Ian Mitchelle S. de Vera, Laura Pedro-Rosa, et al. "Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication." Antimicrobial Agents and Chemotherapy 60, no. 4 (2016): 2195–208. http://dx.doi.org/10.1128/aac.02574-15.

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ABSTRACTThe human immunodeficiency virus type 1 (HIV-1) capsid plays crucial roles in HIV-1 replication and thus represents an excellent drug target. We developed a high-throughput screening method based on a time-resolved fluorescence resonance energy transfer (HTS-TR-FRET) assay, using the C-terminal domain (CTD) of HIV-1 capsid to identify inhibitors of capsid dimerization. This assay was used to screen a library of pharmacologically active compounds, composed of 1,280in vivo-active drugs, and identified ebselen [2-phenyl-1,2-benzisoselenazol-3(2H)-one], an organoselenium compound, as an in

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Najar, Adel M., Ruwida M. K. Omar, Eman Bobtaina, et al. "Design, Synthesis, Pharmacological Evaluation and DFT Investigation of New Bioactive Unsymmetrical Bi-Functional Ligand." Journal of Drug Delivery and Therapeutics 12, no. 4 (2022): 73–80. http://dx.doi.org/10.22270/jddt.v12i4.5429.

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Compounds with more than one bioactive motif become of great interest. In this regard, a new tridentate 1,2-unsymmetrical ligand consists of flexible and rigid bioactive arms spaced by benzene ring in an ortho position designed to form a bifunctional molecule. The 2-((3-(pyridin-2-yl)-1H-pyrazol-1-yl)methyl)benzonitrile (PPMB) synthesized under phase transfer reaction and characterized using 1H-NMR and mass spectroscopy and studied as potent kinase inhibitors. Theoretically, the molecule structure was investigated at the B3LYP/6-311++G(d,p) level of theory in the gas phase and revealed that al

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Siles, Samuel A., Anand Srinivasan, Christopher G. Pierce, José L. Lopez-Ribot, and Anand K. Ramasubramanian. "High-Throughput Screening of a Collection of Known Pharmacologically Active Small Compounds for Identification of Candida albicans Biofilm Inhibitors." Antimicrobial Agents and Chemotherapy 57, no. 8 (2013): 3681–87. http://dx.doi.org/10.1128/aac.00680-13.

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ABSTRACTCandida albicansis the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective againstC. albicansbiofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting of 1,200 off-patent drugs already approved by the Food and Drug Administration (FDA), the Prestwick Chemical Library, to identify inhibitors ofC. albicansbiofilm formation. According to their pharmacological

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18

Creaser, Colin S., John R. Griffiths, and Brian M. Stockton. "Gas-Phase Ion Mobility Studies of Amines and Polyether/Amine Complexes Using Tandem Quadrupole Ion Trap/Ion Mobility Spectrometry." European Journal of Mass Spectrometry 6, no. 2 (2000): 213–18. http://dx.doi.org/10.1255/ejms.339.

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The gas-phase positive ion mobility spectra of isomeric amines and polyether/amine complexes have been measured using a tandem quadrupole ion trap/ion mobility spectrometer. Ion mobilities of isomeric amines in helium, determined relative to benzene at pressures in the range 1–2 Torr, vary with the structure of the amine. The ability of quadrupole ion trap/ion mobility spectrometry to differentiate between a pharmacologically-active substance and an associated isomeric amine is demonstrated. Non-covalent complexes of cyclic and acyclic polyethers with protonated amines were generated by ion/mo

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19

THAPA, SHANKAR, SACHINDRA L. NARGUND, and MAHALAKSHMI SURESHA BIRADAR. "A systematic review on diverse synthetic route and pharmacological activities of benzimidazole as optimized lead." Journal of Ultra Chemistry 18, no. 2 (2022): 24–36. http://dx.doi.org/10.22147/juc/180202.

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The aim of this review is to provide the systematic information of synthetic scheme and biological activity of synthesized benzimidazole derivatives. Benzimidazole is widely used lead molecule for the synthesis of various types of pharmacologically active moiety. It is heterocyclic aromatic fused colorless solid having molecular mass of 118.053 g/mol. It is basic in nature and can be served as ligand in coordination chemistry. It is bioactive compound showed various pharmacological activity till now viz. anthelmintics (albendazole, mebendazole), proton pump inhibitors (omeprazole, pantoprazole

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Che, Kepeng, Ajaybabu V. Pobbati, Caleb N. Seavey, et al. "Aurintricarboxylic acid is a canonical disruptor of the TAZ-TEAD transcriptional complex." PLOS ONE 17, no. 4 (2022): e0266143. http://dx.doi.org/10.1371/journal.pone.0266143.

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Disrupting the formation of the oncogenic YAP/TAZ-TEAD transcriptional complex holds substantial therapeutic potential. However, the three protein interaction interfaces of this complex cannot be easily disrupted using small molecules. Here, we report that the pharmacologically active small molecule aurintricarboxylic acid (ATA) acts as a disruptor of the TAZ-TEAD complex. ATA was identified in a high-throughput screen using a TAZ-TEAD AlphaLISA assay that was tailored to identify disruptors of this transcriptional complex. We further used fluorescence polarization assays both to confirm disru

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Packialakshmi, Ponnusamy, Perumal Gobinath, Daoud Ali, et al. "Novel Chitosan Polymer Design, Synthesis Using Mentha piperita of ZnO NPs as a Catalyst: Antibacterial Evaluation against Gram-Negative Multidrug-Resistant Pathogens." Journal of Nanomaterials 2021 (December 9, 2021): 1–11. http://dx.doi.org/10.1155/2021/8804837.

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The goal of this research is to create a novel Schiff base of chitosan polymer derivatives 1a-1j. Nanotechnology is a promising field since it avoids the usage of hazardous chemicals while also saving time. Using the leaf extract of the pharmacologically valuable herb Mentha piperita, we described a green synthesis of ZnO NPs. Zinc oxide ions may be easily reduced into ZnO NPs using a Mentha piperita extract. ZnO NPs were employed as a phytocatalyst in this investigation to make chitosan derivatives. The synthetic procedure is straightforward, with a short reaction time and a high yield. Our n

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Ho, Yi-Hsun, Lan Chen, and Rong Huang. "Development of A Continuous Fluorescence-Based Assay for N-Terminal Acetyltransferase D." International Journal of Molecular Sciences 22, no. 2 (2021): 594. http://dx.doi.org/10.3390/ijms22020594.

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N-terminal acetylation catalyzed by N-terminal acetyltransferases (NATs) has various biological functions in protein regulation. N-terminal acetyltransferase D (NatD) is one of the most specific NAT with only histone H4 and H2A proteins as the known substrates. Dysregulation of NatD has been implicated in colorectal and lung cancer progression, implying its therapeutic potential in cancers. However, there is no reported inhibitor for NatD yet. To facilitate the discovery of small-molecule NatD inhibitors, we report the development of a fluorescence-based acetyltransferase assay in 384-well hig

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Hess, Jessica D., Luca H. Macias, Denisse A. Gutierrez, et al. "Identification of a Unique Cytotoxic Thieno[2,3-c]Pyrazole Derivative with Potent and Selective Anticancer Effects In Vitro." Biology 11, no. 6 (2022): 930. http://dx.doi.org/10.3390/biology11060930.

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In recent years, the thienopyrazole moiety has emerged as a pharmacologically active scaffold with antitumoral and kinase inhibitory activity. In this study, high-throughput screening of 2000 small molecules obtained from the ChemBridge DIVERset library revealed a unique thieno[2,3-c]pyrazole derivative (Tpz-1) with potent and selective cytotoxic effects on cancer cells. Compound Tpz-1 consistently induced cell death at low micromolar concentrations (0.19 μM to 2.99 μM) against a panel of 17 human cancer cell lines after 24 h, 48 h, or 72 h of exposure. Furthermore, an in vitro investigation o

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Chiaverini, Lorenzo, Damiano Cirri, Iogann Tolbatov, et al. "Medicinal Hypervalent Tellurium Prodrugs Bearing Different Ligands: A Comparative Study of the Chemical Profiles of AS101 and Its Halido Replaced Analogues." International Journal of Molecular Sciences 23, no. 14 (2022): 7505. http://dx.doi.org/10.3390/ijms23147505.

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Ammonium trichloro (dioxoethylene-O,O′) tellurate (AS101) is a potent immunomodulator prodrug that, in recent years, entered various clinical trials and was tested for a variety of potential therapeutic applications. It has been demonstrated that AS101 quickly activates in aqueous milieu, producing TeOCl3−, which likely represents the pharmacologically active species. Here we report on the study of the activation process of AS101 and of two its analogues. After the synthesis and characterization of AS101 and its derivatives, we have carried out a comparative study through a combined experiment

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Ho, Yi-Hsun, Lan Chen, and Rong Huang. "Development of A Continuous Fluorescence-Based Assay for N-Terminal Acetyltransferase D." International Journal of Molecular Sciences 22, no. 2 (2021): 594. http://dx.doi.org/10.3390/ijms22020594.

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N-terminal acetylation catalyzed by N-terminal acetyltransferases (NATs) has various biological functions in protein regulation. N-terminal acetyltransferase D (NatD) is one of the most specific NAT with only histone H4 and H2A proteins as the known substrates. Dysregulation of NatD has been implicated in colorectal and lung cancer progression, implying its therapeutic potential in cancers. However, there is no reported inhibitor for NatD yet. To facilitate the discovery of small-molecule NatD inhibitors, we report the development of a fluorescence-based acetyltransferase assay in 384-well hig

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26

Caporale, Andrea, Fabiola Mascanzoni, Biancamaria Farina, et al. "FRET-Protease-Coupled Peptidyl-Prolyl cis-trans Isomerase Assay." Journal of Biomolecular Screening 21, no. 7 (2016): 701–12. http://dx.doi.org/10.1177/1087057116650402.

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In this work, a sensitive and convenient protease-based fluorimetric high-throughput screening (HTS) assay for determining peptidyl-prolyl cis-trans isomerase activity was developed. The assay was based on a new intramolecularly quenched substrate, whose fluorescence and structural properties were examined together with kinetic constants and the effects of solvents on its isomerization process. Pilot screens performed using the Library of Pharmacologically Active Compounds (LOPAC) and cyclophilin A (CypA), as isomerase model enzyme, indicated that the assay was robust for HTS, and that compara

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Fukuyasu, Sho, Hiroki Kayashima, Akihito Moribayashi, et al. "Cell-Based Double-Screening Method to Identify a Reliable Candidate for Osteogenesis-Targeting Compounds." Biomedicines 10, no. 2 (2022): 426. http://dx.doi.org/10.3390/biomedicines10020426.

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Small-molecule compounds strongly affecting osteogenesis can form the basis of effective therapeutic strategies in bone regenerative medicine. A cell-based high-throughput screening system might be a powerful tool for identifying osteoblast-targeting candidates; however, this approach is generally limited with using only one molecule as a cell-based sensor that does not always reflect the activation of the osteogenic phenotype. In the present study, we used the MC3T3-E1 cell line stably transfected with the green fluorescent protein (GFP) reporter gene driven by a fragment of type I collagen p

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Oprita, Elena Iulia, Andreea Iosageanu, and Oana Craciunescu. "Progress in Composite Hydrogels and Scaffolds Enriched with Icariin for Osteochondral Defect Healing." Gels 8, no. 10 (2022): 648. http://dx.doi.org/10.3390/gels8100648.

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Osteochondral structure reconstruction by tissue engineering, a challenge in regenerative medicine, requires a scaffold that ensures both articular cartilage and subchondral bone remodeling. Functional hydrogels and scaffolds present a strategy for the controlled delivery of signaling molecules (growth factors and therapeutic drugs) and are considered a promising therapeutic approach. Icariin is a pharmacologically-active small molecule of prenylated flavonol glycoside and the main bioactive flavonoid isolated from Epimedium spp. The in vitro and in vivo testing of icariin showed chondrogenic

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Wang, Yuchen, Junfeng Wang, Jinqian Ma, Yun Zhou, and Rong Lu. "Focusing on Future Applications and Current Challenges of Plant Derived Extracellular Vesicles." Pharmaceuticals 15, no. 6 (2022): 708. http://dx.doi.org/10.3390/ph15060708.

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Plant derived extracellular vesicles (EVs) are nano-sized membranous vesicles released by plant cells, which contain lipids, proteins, nucleic acids and specific pharmacologically active substances. They are safe, widely available and expediently extractive. They have gratifyingly biological activity against inflammation, cancer, bacteria and oxidative aging, especially for the prevention or treatment of colitis, cancer, alcoholic liver, and COVID-19. In addition, as natural drug carriers, plant derived EVs have the potential to target the delivery of small molecule drugs and nucleic acid thro

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Danthi, Sanjay J., Beirong Liang, Oanh Smicker, et al. "Identification and Characterization of Inhibitors of a Neutral Amino Acid Transporter, SLC6A19, Using Two Functional Cell-Based Assays." SLAS DISCOVERY: Advancing the Science of Drug Discovery 24, no. 2 (2018): 111–20. http://dx.doi.org/10.1177/2472555218794627.

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SLC6A19 (B0AT1) is a neutral amino acid transporter, the loss of function of which results in Hartnup disease. SLC6A19 is also believed to have an important role in amino acid homeostasis, diabetes, and weight control. A small-molecule inhibitor of human SLC6A19 (hSLC6A19) was identified using two functional cell-based assays: a fluorescence imaging plate reader (FLIPR) membrane potential (FMP) assay and a stable isotope-labeled neutral amino acid uptake assay. A diverse collection of 3440 pharmacologically active compounds from the Microsource Spectrum and Tocriscreen collections were tested

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Alzahrani, Faisal A., Mohammad Imran Khan, Nader Kameli, Elham Alsahafi, and Yasir Mohamed Riza. "Plant-Derived Extracellular Vesicles and Their Exciting Potential as the Future of Next-Generation Drug Delivery." Biomolecules 13, no. 5 (2023): 839. http://dx.doi.org/10.3390/biom13050839.

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Plant cells release tiny membranous vesicles called extracellular vesicles (EVs), which are rich in lipids, proteins, nucleic acids, and pharmacologically active compounds. These plant-derived EVs (PDEVs) are safe and easily extractable and have been shown to have therapeutic effects against inflammation, cancer, bacteria, and aging. They have shown promise in preventing or treating colitis, cancer, alcoholic liver disease, and even COVID-19. PDEVs can also be used as natural carriers for small-molecule drugs and nucleic acids through various administration routes such as oral, transdermal, or

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Frisoni, Paolo, Giorgia Corli, Sabrine Bilel та ін. "Effect of Repeated Administration of ɣ-Valerolactone (GVL) and GHB in the Mouse: Neuroadaptive Changes of the GHB and GABAergic System". Pharmaceuticals 16, № 9 (2023): 1225. http://dx.doi.org/10.3390/ph16091225.

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Background: Gamma-hydroxybutyric acid (GHB) at low dosages has anxiolytic effects and promotes REM sleep and low-wave deep sleep. In the U.S., the legal form of GHB is prescribed to adults suffering from narcolepsy-associated cataplexy; the sodium salt of GHB is reserved for alcohol-addiction treatment. GHB is also a molecule of abuse and recreational use, it is a controlled substance in several countries, so gamma-valerolactone (GVL) has frequently been used as a legal substitute for it. GHB’s abuse profile is most likely attributable to its anxiolytic, hypnotic, and euphoric properties, as w

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Wysocki, Jan, Laura Garcia-Halpin, Minghao Ye, et al. "Regulation of urinary ACE2 in diabetic mice." American Journal of Physiology-Renal Physiology 305, no. 4 (2013): F600—F611. http://dx.doi.org/10.1152/ajprenal.00600.2012.

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Angiotensin-converting enzyme-2 (ACE2) enhances the degradation of ANG II and its expression is altered in diabetic kidneys, but the regulation of this enzyme in the urine is unknown. Urinary ACE2 was studied in the db/db model of type 2 diabetes and stretozotocin (STZ)-induced type 1 diabetes during several physiological and pharmacological interventions. ACE2 activity in db/db mice was increased in the serum and to a much greater extent in the urine compared with db/m controls. Neither a specific ANG II blocker, telmisartan, nor an ACE inhibitor, captopril, altered the levels of urinary ACE2

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Lucumi, Edinson, Claire Darling, Hyunil Jo, et al. "Discovery of Potent Small-Molecule Inhibitors of Multidrug-Resistant Plasmodium falciparum Using a Novel Miniaturized High-Throughput Luciferase-Based Assay." Antimicrobial Agents and Chemotherapy 54, no. 9 (2010): 3597–604. http://dx.doi.org/10.1128/aac.00431-10.

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ABSTRACT Malaria is a global health problem that causes significant mortality and morbidity, with more than 1 million deaths per year caused by Plasmodium falciparum. Most antimalarial drugs face decreased efficacy due to the emergence of resistant parasites, which necessitates the discovery of new drugs. To identify new antimalarials, we developed an automated 384-well plate screening assay using P. falciparum parasites that stably express cytoplasmic firefly luciferase. After initial optimization, we tested two different types of compound libraries: known bioactive collections (Library of Ph

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Kapri, Anandi, Nitin Gupta, and Sumitra Nain. "Recent Advances in the Synthesis of Xanthines: A Short Review." Scientifica 2022 (November 8, 2022): 1–24. http://dx.doi.org/10.1155/2022/8239931.

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Xanthine and its derivatives are considered a pharmacologically potential moiety that manifests immense biological activities. Owing to this much diversity in the biological field, this scaffold has fascinated the attention of many researchers around the globe to scrutinize its basic structure chemically as well as biologically. In recent years, xanthine derivatives have been used therapeutically in different pathological conditions due to their presence in day-to-day life. Herein, we review the recent progress in the synthesis of xanthine and its derivatives. Some of the widely used synthetic

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Nurkenov, O. A., S. D. Fazylov, G. K. Mukusheva, et al. "HYBRID MOLECULES BASED ON ALKALOIDS." Chemical Journal of Kazakhstan 3 (September 30, 2021): 67–82. http://dx.doi.org/10.51580/2021-1/2710-1185.40.

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This review has been summarized the data on the synthesis of new hybrid derivatives based on alkaloid molecules. At the same time, there have been analyzed methods for obtaining hybrid structures containing fragments of natural compounds molecules in combination with other biologically active plant metabolites, as leading compounds for the development of new pharmacologically valuable agents, with the aim of creating new original drugs. The combination of pharmacophoric residues in one molecule, namely various aromatic and heterocyclic substituents in the nucleoside position of natural alkaloi

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Rashid, N., AA Paul, S. Islam, et al. "Studies on antioxidant potential, phytochemical properties and toxicity of four popular medicinal plants of Bangladesh." Journal of Bio-Science 25 (July 18, 2018): 27–37. http://dx.doi.org/10.3329/jbs.v25i0.37495.

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Medicinal plant extract has long been used successfully in ‘unani’ or ‘ayurvedic’ medicine. Medicinal plant extract contains bioactive molecules and activity of these molecules may help to mitigate, eradicate or cure diseases. In the advent for the search for new medicinally important bioactive molecule, the current paper deals with the anti-oxidative, cytotoxic and phytochemical analysis of Scoparia dulcis leaf and root, Curculigo orchioides root, Pandanus fascicularis root and Baccaurea sapida leaf extract. Aqueous and methanolic extracts were made for each of the extracts where they posses

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Ishima, Yu, Ulrich Kragh-Hansen, Toru Maruyama, and Masaki Otagiri. "Poly-S-Nitrosated Albumin as a Safe and Effective Multifunctional Antitumor Agent: Characterization, Biochemistry and Possible Future Therapeutic Applications." BioMed Research International 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/353892.

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Nitric oxide (NO) is a ubiquitous molecule involved in multiple cellular functions. Inappropriate production of NO may lead to disease states. To date, pharmacologically active compounds that release NO within the body, such as organic nitrates, have been used as therapeutic agents, but their efficacy is significantly limited by unwanted side effects. Therefore, novel NO donors with better pharmacological and pharmacokinetic properties are highly desirable. TheS-nitrosothiol fraction in plasma is largely composed of endogenousS-nitrosated human serum albumin (Mono-SNO-HSA), and that is why we

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Maddela, Srinubabu, Githa Elizabeth Mathew, Della Grace Thomas Parambi, Fakhria Aljoufi, and Bijo Mathew. "Dual Acting Isatin-heterocyclic Hybrids: Recent Highlights as Promising Pharmacological Agents." Letters in Drug Design & Discovery 16, no. 2 (2018): 220–36. http://dx.doi.org/10.2174/1570180815666180516102100.

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Background: For the development of suitable lead molecules to different diseases is a highly challenging task for medicinal chemists. Nowadays, hybrid pharmacophore concept has developed as a useful structural modification tool in the drug design of new drug candidates for different diseases. Hybrid pharmacophore approach consists of combination of two or more pharmacophoric moieties from different biologically active compounds with complementary functions or different mechanisms of action into a single molecule. This often results in synergistic activity or enhanced drug efficacy. Objective:

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Akhter, Naheed, Sidra Batool, Samreen Gul Khan, et al. "Bio-Oriented Synthesis and Molecular Docking Studies of 1,2,4-Triazole Based Derivatives as Potential Anti-Cancer Agents against HepG2 Cell Line." Pharmaceuticals 16, no. 2 (2023): 211. http://dx.doi.org/10.3390/ph16020211.

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Triazole-based acetamides serve as important scaffolds for various pharmacologically active drugs. In the present work, structural hybrids of 1,2,4-triazole and acetamides were furnished by chemically modifying 2-(4-isobutylphenyl) propanoic acid (1). Target compounds 7a–f were produced in considerable yields (70–76%) by coupling the triazole of compound 1 with different electrophiles under different reaction conditions. These triazole-coupled acetamide derivatives were verified by physiochemical and spectroscopic (HRMS, FTIR, 13CNMR, and 1HNMR,) methods. The anti-liver carcinoma effects of al

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Tanabe, Kenji. "Abstract LB238: Image-based phenotypic profiling of a chemogenomic screening library identifies nobel targets of known inhibitors." Cancer Research 83, no. 8_Supplement (2023): LB238. http://dx.doi.org/10.1158/1538-7445.am2023-lb238.

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Abstract The gene encoding epidermal growth factor receptor (EGFR) is a major driver gene in cancer. Many drugs targeting EGFR-associated molecules have been developed, yet many have failed in clinical trials due to a lack of efficacy and/or unexpected side effects. In this study, I used image-based phenotypic profiling to screen a pharmacologically active compound library with the aim of identifying new druggable targets in the EGFR pathway. As anticipated, the phenotypic screen identified compounds that produce phenotypes resulting from targeting a known specific molecule or pathway. The ass

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Schaertl, Sabine, Michael Prime, John Wityak, et al. "A Profiling Platform for the Characterization of Transglutaminase 2 (TG2) Inhibitors." Journal of Biomolecular Screening 15, no. 5 (2010): 478–87. http://dx.doi.org/10.1177/1087057110366035.

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Huntington’s disease (HD) is associated with increased expression levels and activity of tissue transglutaminase (TG2), an enzyme primarily known for its cross-linking of proteins. To validate TG2 as a therapeutic target for HD in transgenic models and for eventual clinical development, a selective and brain-permeable inhibitor is required. Here, a comprehensive profiling platform of biochemical and cellular assays is presented which has been established to evaluate the potency, cellular efficacy, subtype selectivity and the mechanism-of-action of known and novel TG2 inhibitors. Several classe

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Li, Xia, Yuan-bo Wang, Chao-chen Wang, et al. "Antidepressant Mechanism of Kaixinsan and Its Active Compounds Based on Upregulation of Antioxidant Thioredoxin." Evidence-Based Complementary and Alternative Medicine 2022 (July 19, 2022): 1–12. http://dx.doi.org/10.1155/2022/7302442.

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Objectives. Kaixinsan (KXS), a traditional Chinese medicine formula, has been demonstrated to be effective in the treatment of depression. The present study applied a network pharmacology approach to dig out the new targets and mechanism of action of KXS and the active compounds in the treatment of depression. Methods. A network pharmacology approach based on public databases including ADME (absorption, distribution, metabolism, and excretion) evaluation, targets prediction, construction of networks, and molecule docking was used and validated the predicted new antioxidant targets and mechanis

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Boni, Valentina, Victor Moreno, Emiliano Calvo, et al. "OMX-0407: A novel spectrum-selective small molecule kinase inhibitor in advanced/metastatic solid tumors." Journal of Clinical Oncology 43, no. 16_suppl (2025): 3103. https://doi.org/10.1200/jco.2025.43.16_suppl.3103.

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3103 Background: OMX-0407 is an orally available spectrum-selective kinase inhibitor that targets key oncology-relevant tyrosine kinases and salt-inducible kinases and is being developed as a first-in-class treatment for solid tumor indications. Preclinical investigations indicate a dual mode of action by sensitizing tumor cells to immune cell induced apoptotic cell death as well as direct inhibition of tumor growth promoting kinases. Methods: This is a phase Ia/Ib dose escalation and expansion study of OMX-0407 (NCT05826600). Eligible patients for the phase Ia dose escalation part had advance

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Hricovíniová, Jana, Zuzana Hricovíniová, and Katarína Kozics. "Antioxidant, Cytotoxic, Genotoxic, and DNA-Protective Potential of 2,3-Substituted Quinazolinones: Structure—Activity Relationship Study." International Journal of Molecular Sciences 22, no. 2 (2021): 610. http://dx.doi.org/10.3390/ijms22020610.

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The evaluation of antioxidant compounds that counteract the mutagenic effects caused by the direct action of reactive oxygen species on DNA molecule is of considerable interest. Therefore, a series of 2,3-substituted quinazolinone derivatives (Q1–Q8) were investigated by different assays, and the relationship between their biological properties and chemical structure was examined. Genotoxicity and the potential DNA-protective effects of Q1–Q8 were evaluated by comet assay and DNA topology assay. Antioxidant activity was examined by DPPH-radical-scavenging, reducing-power, and total antioxidant

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Sharma, Ankita, and Swaran Jeet Singh Flora. "Positive and Negative Regulation of Ferroptosis and Its Role in Maintaining Metabolic and Redox Homeostasis." Oxidative Medicine and Cellular Longevity 2021 (April 28, 2021): 1–13. http://dx.doi.org/10.1155/2021/9074206.

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Ferroptosis is a recently recognized regulated form of cell death characterized by accumulation of lipid-based reactive oxygen species (ROS), particularly lipid hydroperoxides and loss of activity of the lipid repair enzyme glutathione peroxidase 4 (GPX4). This iron-dependent form of cell death is morphologically, biochemically, and also genetically discrete from other regulated cell death processes, which include autophagy, apoptosis, necrosis, and necroptosis. Ferroptosis is defined by three hallmarks, defined as the loss of lipid peroxide repair capacity by GPX4, the bioavailability of redo

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Ouyang, Dan, Lan-Chun Wang, Ting Tang, and Hong Feng. "Genomic-Wide Identification and Characterization of the Uridine Diphosphate Glycosyltransferase Family in Eucommia ulmoides Oliver." Plants 10, no. 9 (2021): 1934. http://dx.doi.org/10.3390/plants10091934.

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Eucommia ulmoides Oliver is a woody plant with great economic and medicinal value. Its dried bark has a long history of use as a traditional medicinal material in East Asia, which led to many glycosides, such as aucubin, geniposide, hyperoside, astragalin, and pinoresinol diglucoside, being recognized as pharmacologically active ingredients. Uridine diphosphate glycosyltransferases (UGTs) catalyze a glycosyl-transferring reaction from the donor molecule uridine-5′-diphosphate-glucose (UDPG) to the substrate, which plays an important role in many biological processes, such as plant growth and d

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Hricovíniová, Jana, Zuzana Hricovíniová, and Katarína Kozics. "Antioxidant, Cytotoxic, Genotoxic, and DNA-Protective Potential of 2,3-Substituted Quinazolinones: Structure—Activity Relationship Study." International Journal of Molecular Sciences 22, no. 2 (2021): 610. http://dx.doi.org/10.3390/ijms22020610.

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The evaluation of antioxidant compounds that counteract the mutagenic effects caused by the direct action of reactive oxygen species on DNA molecule is of considerable interest. Therefore, a series of 2,3-substituted quinazolinone derivatives (Q1–Q8) were investigated by different assays, and the relationship between their biological properties and chemical structure was examined. Genotoxicity and the potential DNA-protective effects of Q1–Q8 were evaluated by comet assay and DNA topology assay. Antioxidant activity was examined by DPPH-radical-scavenging, reducing-power, and total antioxidant

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Floresta, Giuseppe, Davide Gentile, Giancarlo Perrini, Vincenzo Patamia, and Antonio Rescifina. "Computational Tools in the Discovery of FABP4 Ligands: A Statistical and Molecular Modeling Approach." Marine Drugs 17, no. 11 (2019): 624. http://dx.doi.org/10.3390/md17110624.

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Small molecule inhibitors of adipocyte fatty-acid binding protein 4 (FABP4) have received interest following the recent publication of their pharmacologically beneficial effects. Recently, it was revealed that FABP4 is an attractive molecular target for the treatment of type 2 diabetes, other metabolic diseases, and some type of cancers. In past years, hundreds of effective FABP4 inhibitors have been synthesized and discovered, but, unfortunately, none have reached the clinical research phase. The field of computer-aided drug design seems to be promising and useful for the identification of FA

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McCoy, Eric S., Wendy A. Lea, Bryan T. Mott, et al. "High-Throughput Screen Identifies Cyclic Nucleotide Analogs That Inhibit Prostatic Acid Phosphatase." Journal of Biomolecular Screening 18, no. 4 (2012): 481–89. http://dx.doi.org/10.1177/1087057112468613.

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The secretory and transmembrane isoforms of prostatic acid phosphatase (PAP) can dephosphorylate extracellular adenosine 5′-monophosphate (AMP) to adenosine, classifying PAP as an ectonucleotidase. Currently, there are no compounds that inhibit PAP in living cells. To identify small-molecule modulators of PAP, we used a 1536-well–based quantitative high-throughput fluorogenic assay to screen the Library of Pharmacologically Active Compounds (LOPAC1280) arrayed as eight-concentration dilution series. This fluorogenic assay used difluoro-4-methylumbelliferyl phosphate as substrate and collected

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