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Journal articles on the topic 'Acyl thiourea compounds'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Ölmez, Nevin Arıkan, and Faryal Waseer. "New Potential Biologically Active Compounds: Synthesis and Characterization of Urea and Thiourea Derivativpes Bearing 1,2,4-oxadiazole Ring." Current Organic Synthesis 17, no. 7 (2020): 525–34. http://dx.doi.org/10.2174/1570179417666200417112106.

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Background: Urea, thiourea, and 1,2,4-oxadiazole compounds are of great interest due to their different activities such as anti-inflammatory, antiviral, analgesic, fungicidal, herbicidal, diuretic, antihelminthic and antitumor along with antimicrobial activities. Objective: In this work, we provide a new series of potential biologically active compounds containing both 1,2,4-oxadiazole and urea/thiouprea moiety. Materials and Methods: Firstly, 5-chloromethyl-3-aryl-1,2,4-oxadiazoles (3a-j) were synthesized from the reaction of different substituted amidoximes (2a-j) and chloroacetyl chloride i

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2

Wang, Han, Zhi-Wen Zhai, Yan-Xia Shi, et al. "Novel Trifluoromethylpyrazole Acyl Thiourea Derivatives: Synthesis, Antifungal Activity and Docking Study." Letters in Drug Design & Discovery 16, no. 7 (2019): 785–91. http://dx.doi.org/10.2174/1570180815666180704103047.

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Background: In recent years, pyrazole carboxamide derivatives possessed excellent fungicidal activity. In the process of designing new fungicides, the carboxamide group was modified in order to find novel structure pyrazole carboxamide derivatives. Methods: Ten novel trifluoromethyl pyrazole acyl thiourea derivatives were designed and synthesized. In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum, Corynespora mazei and Botrytis cinerea, respectively Results: Particularly compounds exhibited significant control effective at 100 mg/L. More importantly, some

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3

Ru, Chengjie, Yulu Wang, Jianping Li, et al. "Synthesis and Physiological Activity of the Acyl Thiourea Compounds." Chinese Journal of Applied Chemistry 11, no. 3 (1994): 92–95. http://dx.doi.org/10.3724/j.issn.1000-0518.1994.3.92.

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4

Ru, Chengjie, Yulu Wang, Jianping Li, et al. "Synthesis and Physiological Activity of the Acyl Thiourea Compounds." Chinese Journal of Applied Chemistry 11, no. 3 (1994): 92–95. http://dx.doi.org/10.3724/j.issn.1000-0518.1994.3.9295.

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5

BREL, A. K., S. V. LISINA, K. M. ETERSKOVA, and J. N. BUDAEVA. "SYNTHESIS OF N-ACYLATED UREA AND THIOUREA BASED ON HYDROXY AND METHOXYBENZOIC ACIDS AS POTENTIAL DRUGS." IZVESTIA VOLGOGRAD STATE TECHNICAL UNIVERSITY, no. 12(295) (December 2024): 21–27. https://doi.org/10.35211/1990-5297-2024-12-295-21-27.

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N-acylated ureas and thioureas based on hydroxy- and methoxybenzoic acids were synthesized using the Schotten-Baumann reaction in two stages without isolating the intermediate acyl chloride (one-pot multicomponent synthesis) under optimal conditions. The structure of the obtained compounds was confirmed by 1H and 13C NMR spectroscopy. The spectrum of biological activity of the compounds was estimated using the PASS (Predictor of Activity Spectra for Substance) program. Using the ChemAxon online platform, theoretical calculations of descriptor values such as hydrophilic-lipophilic balance (LogP

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6

Al-Amily, Duraid H., and Mohammed Hassan Mohammed. "Design, Synthesis, and Docking Study of Acyl Thiourea Derivatives as Possible Histone Deacetylase Inhibitors with a Novel Zinc Binding Group." Scientia Pharmaceutica 87, no. 4 (2019): 28. http://dx.doi.org/10.3390/scipharm87040028.

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Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-

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7

Sijia, Xue, Guo Yanling, Li Jingzhi, Ke Shaoyong, and Duan Liping. "Synthesis and biological activity of N'-(substituted pyrimidin-2-yl)- N-dichlorochrysanthemoyl thioureas and their fused heterocyclic compounds." Journal of Indian Chemical Society Vol. 82, Mar 2005 (2005): 262–64. https://doi.org/10.5281/zenodo.5827025.

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College of Life-and Environmental Science, Department of Chemistry, Shanghai Normal University, Shanghai, 200234, P. R. China <em>E-mail</em> : ylguo420@ 163.com <em>Manuscript received 25 June 2004, accepted 24 November 2004</em> Five <em>N'</em> -(substituted pyrimidin-2-yi)-<em>N</em>-dichlorochrysanthemoyl thioureas (Sa-Se) were synthesized from corresponding dichlorochrysanthemic acid in three steps. And two dichlorochrysanthemoylimino-2<em>H</em>-1,2,4-thiadiazolo[2,3-a]pyrimidines were prepared by oxidizing cyclization of 5a, 5b. The structures of these novel target compounds were c

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8

Nossa González, Diana L., Aamer Saeed, Ghulam Shabir, Ulrich Flörke, and Mauricio F. Erben. "Conformational and crystal structure of acyl thiourea compounds: The case of the simple (2,2-dimethyl-propionyl) thiourea derivative." Journal of Molecular Structure 1215 (September 2020): 128227. http://dx.doi.org/10.1016/j.molstruc.2020.128227.

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9

Makhaeva, Galina F., Nadezhda V. Kovaleva, Natalia P. Boltneva, et al. "Bis-Amiridines as Acetylcholinesterase and Butyrylcholinesterase Inhibitors: N-Functionalization Determines the Multitarget Anti-Alzheimer’s Activity Profile." Molecules 27, no. 3 (2022): 1060. http://dx.doi.org/10.3390/molecules27031060.

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Using two ways of functionalizing amiridine—acylation with chloroacetic acid chloride and reaction with thiophosgene—we have synthesized new homobivalent bis-amiridines joined by two different spacers—bis-N-acyl-alkylene (3) and bis-N-thiourea-alkylene (5) —as potential multifunctional agents for the treatment of Alzheimer’s disease (AD). All compounds exhibited high inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with selectivity for BChE. These new agents displayed negligible carboxylesterase inhibition, suggesting a probable lack of untoward drug–dru

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10

J. Ekowati, D. Pebrianti, G. C. Ananda, D. R. Ramadhan, R. Widyowati, and K. A. Nofianti. "DESIGN AND SYNTHESIS NOVEL COMPOUNDS OF ORTHOCOUMARIC ACID DERIVATES AS ANTI-THROMBOTIC CANDIDATE." RASAYAN Journal of Chemistry 17, no. 03 (2024): 1387–94. http://dx.doi.org/10.31788/rjc.2024.1738657.

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It has been reported that aspirin and P2Y inhibitors have emerged as the preferred therapeutic agents for managing vaso-occlusive illness due to their anti-thrombotic properties. However, complaints about the side effects of these drugs are still being reported. Ongoing research is being conducted on the design and development of novel antithrombotic agents to obtain good health and well-being. ortho-Coumaric acid derivates were designed using the ChemDraw program, while a physicochemical prediction study was carried out by the Swiss ADME program, and the MOE platform was operated to predict t

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11

Roman, Roxana, Lucia Pintilie, Miron Teodor Căproiu, et al. "New N-acyl Thiourea Derivatives: Synthesis, Standardized Quantification Method and In Vitro Evaluation of Potential Biological Activities." Antibiotics 12, no. 5 (2023): 807. http://dx.doi.org/10.3390/antibiotics12050807.

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New N-acyl thiourea derivatives with heterocyclic rings have been synthesized by first obtaining isothiocyanate, which further reacted with a heterocyclic amine, characterized by (FT-IR, NMR spectroscopy and FT-ICR) and tested for their in vitro antimicrobial, anti-biofilm and antioxidant activities to obtain a drug candidate in a lead-optimization process. From the tested compounds, those bearing benzothiazole (1b) and 6-methylpyridine (1d) moieties revealed anti-biofilm activity against E. coli ATCC 25922 at MBIC values of 625 µg/mL. Compound 1d exhibited the highest antioxidant capacity (~4

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12

Baltaş, Nimet. "Synthesis of quinazolinone derivatives containing an acyl hydrazone skeleton as potent anti-urease agents enzyme kinetic studies and anti-oxidant properties." Journal of Chemical Research 46, no. 3 (2022): 174751982210965. http://dx.doi.org/10.1177/17475198221096568.

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This paper covers the synthesis, in vitro urease inhibition, enzyme kinetic parameters, and anti-oxidant studies of a novel series of quinazolinone derivatives containing an acyl hydrazone skeleton. Compounds 3a, 3b, 5a, and 5b, having IC50 values ranging from 1.86 ± 0.07 to 6.38 ± 0.11 µg mL−1, show greater inhibitory activity than the standard inhibitor, thiourea. Among the products, (2-[2-(3-methoxybenzyl)-4-oxoquinazolin-3(4 H)-yl]acetohydrazide) proves to be the most potent, exhibiting enzyme inhibition activity with an IC50 value of 1.86 ± 0.07 µg mL−1. Kinetic studies involving the Line

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13

Roman, Roxana, Lucia Pintilie, Diana Camelia Nuță, et al. "Contribution to the Synthesis, Characterization, Separation and Quantification of New N-Acyl Thiourea Derivatives with Antimicrobial and Antioxidant Potential." Pharmaceutics 15, no. 10 (2023): 2501. http://dx.doi.org/10.3390/pharmaceutics15102501.

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The present study aimed to synthesize, characterize, and validate a separation and quantification method of new N-acyl thiourea derivatives (1a–1o), incorporating thiazole or pyridine nucleus in the same molecule and showing antimicrobial potential previously predicted in silico. The compounds have been physiochemically characterized by their melting points, IR, NMR and MS spectra. Among the tested compounds, 1a, 1g, 1h, and 1o were the most active against planktonic Staphylococcus aureus and Pseudomonas aeruginosa, as revealed by the minimal inhibitory concentration values, while 1e exhibited

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14

Saeed, Aamer, Sajid ur-Rehman, Pervaiz Channar, et al. "Jack Bean Urease Inhibitors, and Antioxidant Activity Based on Palmitic acid Derived 1-acyl-3- Arylthioureas: Synthesis, Kinetic Mechanism and Molecular Docking Studies." Drug Research 67, no. 10 (2017): 596–605. http://dx.doi.org/10.1055/s-0043-113832.

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AbstractA series of acylthioureas was synthesized and their inhibitory effects on the DPPH and jack bean urease were evaluated. The results showed that all of the synthesized compounds exhibited significant jack bean urease inhibitory activities. Especially, 1-(4-chlorophenyl)-3 palmitoylthiourea 5a bearing 4-chloro substituted phenyl ring exhibited the most potent tyrosinase inhibitory activity with an IC50 value 0.0170 μM compared to the IC50 value of 4.720 μM of thiourea used as standard. The inhibition mechanism analyzed by Lineweaver–Burk plots revealed that the type of inhibition of comp

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15

Arshad, Tanzila, Hamdullah Khadim Sheikh, Mehdi Hassan Kazmi, Sadia Farheen, Tehmina Sohail, and Mehreen Lateef. "New bioactive triaryl triglyceride esters: Synthesis, characterization and biological activities." Bangladesh Journal of Pharmacology 13, no. 4 (2018): 302. http://dx.doi.org/10.3329/bjp.v13i4.37210.

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<p class="Abstract">Four new bioactive aryl triester derivatives of glycerol and benzoic acids were synthesized. The synthetic compounds were studied for their antimicrobial and urease inhibition activities. Esterification was carried out by using carbonyldiimidazole to enhance the acyl elimination addition reaction with benzoic acid derivatives. The structure of triglycerides were studied by EI-MS, <sup>1</sup>H, <sup>13</sup>C-NMR, FT-IR and elemental analysis. All synthetic compounds showed urease inhibition activity with highest value of IC<sub>50 </s

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16

Hussein, Modather F. "New sulfonamide hybrids: synthesis, in vitro antimicrobial activity and docking study of some novel sulfonamide derivatives bearing carbamate/acyl-thiourea scaffolds." Mediterranean Journal of Chemistry 7, no. 5 (2018): 370–85. http://dx.doi.org/10.13171/mjc751912111445mh.

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In this study, the novel hybrids sulfonamide carbamates were synthesized by treatment of N-substituted 4-isothiocyanatophenyl sulfonamides with ethyl carbamate in dry 1,4-dioxane at reflux temperature in the presence of triethylamine. Also, treatment of Phenylacetylisothiocyanate with sulfanilamide in refluxing acetonitrile afforded the corresponding hybrid sulfonamide acylthiourea derivatives. The anti-microbial activities of the synthesized compounds were evaluated. Ethyl ({4-[(5-methyl-1,2-oxazol-3-yl)sulfamoyl)-phenyl]carbamothioyl)- carbamate and 2-Phenyl-N-((4-(N-thiazol-2-yl)sulfamoyl)-

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17

Zohny, Yasser M., Samir M. Awad, Maha A. Rabie, and Omar Awad Alsaidan. "Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Pyrimidine Derivatives as Potential Calcium Channel Blockers." Molecules 28, no. 12 (2023): 4869. http://dx.doi.org/10.3390/molecules28124869.

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Pyrimidines play an important role in modern medical fields. They have a wide spectrum of biological activities such as antimicrobial, anticancer, anti-allergic, anti-leishmanial, antioxidant agents and others. Moreover, in recent years, 3,4-dihydropyrimidin-2(1H)ones have attracted researchers to synthesize them via Biginelli reaction and evaluate their antihypertensive activities as bioisosters of Nifedipine, which is a famous calcium channel blocker. Our new target compounds were prepared through one-pot reaction of thiourea 1, ethyl acetoacetate 2 and/or 1H-indole-2-carbaldehyde, 2-chloroq

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18

Arshad, Nasima, Uzma Parveen, Pervaiz Ali Channar, et al. "Investigation of Newly Synthesized Bis-Acyl-Thiourea Derivatives of 4-Nitrobenzene-1,2-Diamine for Their DNA Binding, Urease Inhibition, and Anti-Brain-Tumor Activities." Molecules 28, no. 6 (2023): 2707. http://dx.doi.org/10.3390/molecules28062707.

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Bis-acyl-thiourea derivatives, namely N,N’-(((4-nitro-1,2-phenylene)bis(azanediyl)) bis(carbonothioyl))bis(2,4-dichlorobenzamide) (UP-1), N,N’-(((4-nitro-1,2-phenylene) bis(azanediyl))bis(carbonothioyl))diheptanamide (UP-2), and N,N’-(((4-nitro-1,2-phenylene)bis(azanediyl))bis(carbonothioyl))dibutannamide (UP-3), were synthesized in two steps. The structural characterization of the derivatives was carried out by FTIR, 1H-NMR, and 13C-NMR, and then their DNA binding, anti-urease, and anticancer activities were explored. Both theoretical and experimental results, as obtained by density functiona

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19

Ahmed, Atteeque, Mubashir Aziz, Syeda Abida Ejaz, et al. "Design, Synthesis, Kinetic Analysis and Pharmacophore-Directed Discovery of 3-Ethylaniline Hybrid Imino-Thiazolidinone as Potential Inhibitor of Carbonic Anhydrase II: An Emerging Biological Target for Treatment of Cancer." Biomolecules 12, no. 11 (2022): 1696. http://dx.doi.org/10.3390/biom12111696.

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Carbonic anhydrases (CA), having Zn2+ metal atoms, are responsible for the catalysis of CO2 and water to bicarbonate and protons. Any abnormality in the functioning of these enzymes may lead to morbidities such as glaucoma and different types of cancers including brain, renal and pancreatic carcinomas. To cope with the lack of presence of a promising therapeutic agent against these cancers, searching for an efficient and suitable carbonic anhydrase inhibitor is crucial. In the current study, ten novel 3-ethylaniline hybrid imino-thiazolidinones were synthesized and characterized by FTIR, NMR (

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20

Kholodniak, Olena, and Sergiy Kovalenko. "Substituted acyl thioureas and acyl thiosemicarbazides: synthesis and biological activity (minireview)." ScienceRise: Pharmaceutical Science, no. 2(36) (April 29, 2022): 56–71. http://dx.doi.org/10.15587/2519-4852.2022.255738.

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Acyl isothiocyanates and their functional derivatives (acyl thioureas and acyl thiosemicarbazides) are an important group of organic compounds that are widely used in the synthesis of heterocycles and in chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been an increased interest towards this class of compounds as promising biologically active compounds, especially since the latest advances in medicinal chemistry for them are not sufficiently studied. The aim. To summarize and systematize information for the last 10 years on methods of synthesis a

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21

Olena, Kholodniak, and Kovalenko Sergiy. "Substituted acyl thioureas and acyl thiosemicarbazides: synthesis and biological activity (minireview)." ScienceRise: Pharmaceutical Science, no. 2(36) (April 29, 2022): 56–71. https://doi.org/10.15587/2519-4852.2022.255738.

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Acyl isothiocyanates and their functional derivatives (acyl thioureas and acyl thiosemicarbazides) are an important group of organic compounds that are widely used in the synthesis of heterocycles and in chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been an increased interest towards this class of compounds as promising biologically active compounds, especially since the latest advances in medicinal chemistry for them are not sufficiently studied. <strong>The aim. </strong>To summarize and systematize information for the last 10 years on method

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22

Jiang, Yanhong, and Weiping Zheng. "Cyclic Tripeptide-based Potent and Selective Human SIRT5 Inhibitors." Medicinal Chemistry 16, no. 3 (2020): 358–67. http://dx.doi.org/10.2174/1573406415666190603101937.

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Background:: SIRT5 is one of the seven members (SIRT1-7) of the mammalian sirtuin family of protein acyl-lysine deacylase enzymes. In recent years, important regulatory roles of SIRT5 in (patho)physiological conditions (e.g. metabolism and cancer) have been increasingly demonstrated. For a better biological understanding and therapeutic exploitation of the SIRT5- catalyzed deacylation reaction, more effort on identifying potent and selective SIRT5 inhibitors beyond those currently known would be rewarding. Objective:: In the current study, we would like to see if it would be possible to develo

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23

Sergiy, Vlasov, Kovalenko Sergiy, Orlenko Inna, Zhuravel Iryna, Krolenko Konstantin, and Vlasov Vitaliy. "Synthesis and antimicrobial activity of 3-(2-N-(aryl,acyl)amino-5-methyl-1,3-thiazol-4-yl)-2H-chromen-2-ones." ScienceRise: Pharmaceutical Science, no. 6(28) (December 30, 2020): 50–55. https://doi.org/10.15587/2519-4852.2020.221701.

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<strong>The aim </strong>of this work is to study methods of 3-(2-N-(aryl,acyl)amino-5-methyl-1,3-thiazol-4-yl)-2H-chromen-2-ones preparation and their antimicrobial activity. <strong>Materials and methods. </strong><sup>1</sup>Н NMR spectra were recorded on Varian Mercury-200 (200 MHz), <sup>13</sup>C NMR spectra were acquired on Bruker Avance 500 <sup>1</sup>H NMR (500 MHz) and <sup>13</sup>C NMR (125 MHz) in DMSO-d<sub>6</sub> and CDCl<sub>3</sub>. LC-MS analysis of compounds was performed on an Agilent 1100 HPLC instrument with chemical ionization at atmospher

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24

I., M. Khazi, S. Koti R., V. Chadha Monica, and S. Mahajanshetti C. "Synthesis and antibacterial activity of new N-acyl-N' -(3-chloro-4- fluorophenyl)thioureas." Journal of Indian Chemical Society Vol. 82, Aug 2005 (2005): 761–63. https://doi.org/10.5281/zenodo.5830300.

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Department of Chemistry, Karnatak University, Dharwad7580 003, India <em>E-mail</em> : dr_imk@yahoo.com Department of Medicinal Chemistry, College of Pharmacy, J. N. Medical College Campus, Belgaum-590 010, India  <em>Manuscript received 3 November 2004, revised 2 March 2005, accepted 6 May 2005 </em> A new series of N-acyl-N' -(3-chloro-4-fluorophenyl)thioureas have been prepared in excellent yield by the reaction of acylthioeyanates and 3-chloro-4-fluormtniline under solid-liquid phase transfer catalysis using PEG-400. All synthesised compounds were screened against <em>Escheri

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25

Nossa González, Diana Lisseth, Arles Javanny Gómez Castaño, Gustavo A. Echeverria, Oscar E. Piro, Aamer Saeed, and Mauricio Federico Erben. "Effect of Terminal Hydroxy Groups on the Structural Properties of Acyl Thioureas." ChemPhysChem, August 8, 2024. http://dx.doi.org/10.1002/cphc.202300680.

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The 1‐acyl thiourea family [R1C(O)NHC(S)NR2R3] exhibits the flexibility to incorporate a wide variety of substituents into their structure. The structural attributes of these compounds are intricately tied to the type and extent of substitution. In the case of 3‐mono‐substituted thioureas (R2 = H), the conformational behavior is predominantly shaped by the presence of an intramolecular N–H···O=C hydrogen bond. This study delves into the structural consequences stemming from the inclusion of substituents possessing hydrogen‐donor capabilities within four novel 1‐acyl‐3‐mono‐substituted thiourea

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26

Seraj, Faiza, Khalid Mohammed Khan, Jamshed Iqbal, et al. "Evaluation of synthetic aminoquinoline derivatives as urease inhibitors: in vitro, in silico and kinetic studies." Future Medicinal Chemistry, October 10, 2023. http://dx.doi.org/10.4155/fmc-2023-0168.

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Background: Quinoline and acyl thiourea scaffolds have major chemical significance in medicinal chemistry. Quinoline-based acyl thiourea derivatives may potentially target the urease enzyme. Materials & methods: Quinoline-based acyl thiourea derivatives 1–26 were synthesized and tested for urease inhibitory activity. Results: 19 derivatives (1–19) showed enhanced urease enzyme inhibitory potential (IC50 = 1.19–18.92 μM) compared with standard thiourea (IC50 = 19.53 ± 0.032 μM), whereas compounds 20–26 were inactive. Compounds with OCH3, OC2H5, Br and CH3 on the aryl ring showed significant

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27

Ekowati, Juni, Iwan Sahrial Hamid, Kholis Amalia Nofianti, and Shigeru Sasaki. "SYNTHESIS OF THIOUREA DERIVATIVES FROM M-METHOXYCINNAMIC ACID AS ANTIANGIOGENIC CANDIDATE." Jurnal Teknologi 81, no. 4 (2019). http://dx.doi.org/10.11113/jt.v81.13410.

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Microwave-assisted nucleophilic acyl substitution was employed to obtain thiourea derivatives (3a, 3b, 3c) from m-methoxycinnamic acid (1). This synthesis method successfully yielded 60-70% reaction product. In vivo anti-angiogenic evaluation was conducted by chick chorioallantoic membrane model, by which each of the derivative at dose 30, 60, and 90 µg induced by bFGF and compared to celecoxib 60 µg as positive control. It was found that all of the synthesized compound at the tested dose were able to inhibit neovascularization and formation of endothelial cell of new blood vessels by 51-75%.

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28

EFEOĞLU, Çağla, Şit TİKEN, Hayati SARI, and Yahya NURAL. "Synthesis and Determination of Acid Dissociation Constants of Bis-Acyl Thiourea Derivatives." Journal of the Turkish Chemical Society Section A: Chemistry, June 19, 2023, 835–44. http://dx.doi.org/10.18596/jotcsa.1269213.

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N,N'-((dodecane-1,12-diylbis(azanediyl))bis(carbonothioyl))bis(4-nitrobenzamide) 5 and N,N'-((dodecane-1,12-diylbis(azanediyl))bis(carbonothioyl))bis(3-nitrobenzamide) 6 as bis acyl thiourea derivatives were synthesized and their molecular structures were characterized using 1H NMR, 13C NMR, COSY, DEPT, HMQC, FT-IR, and HRMS techniques. The acid dissociation constants (pKa) of the bis-acyl thiourea derivatives 5, 6 were determined potentiometrically and spectrophotometrically. The pKa values of products 5, 6 were determined in 50% (v/v) dimethyl sulfoxide–water hydro-organic solvent in the pre

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29

Huang, Mei, Min Huang, Xiu Wang, Wen-Gui Duan, Gui-Shan Lin, and Fu-Hou Lei. "Synthesis, antifungal activity and 3D-QSAR study of novel acyl thiourea compounds containing gem-dimethylcyclopropane ring." Molecular Diversity, April 29, 2021. http://dx.doi.org/10.1007/s11030-020-10163-6.

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30

Ahmed, Atteeque, Abdul Manan, Aamer Saeed, et al. "Innovative Pivaloyl Fixed 1,3‐Thiazole‐2‐imines as Multitarget Inhibitors: Synthesis, Enzyme Inhibition, Molecular Docking and Structure Activity Relationship (SAR) Studies." ChemistrySelect 10, no. 15 (2025). https://doi.org/10.1002/slct.202501366.

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AbstractA small library of Pivaloyl‐Fixed 1,3‐Thiazole‐2‐imine pharmacophores (5a‐j) was synthesized in three steps, starting with the reaction of pivaloyl chloride with potassium thiocyanate, followed by condensation with p‐toluidine. In the final step, the resulting acyl thiourea intermediate was cyclized with α‐halo ketone, yielding the target compounds. The structure of newly synthesized compounds was confirmed by spectroscopic and elemental analyses. The overexpression of the urease, α‐amylase, and α‐glucosidase enzymes causes various physiological conditions, and inhibition of these enzy

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31

Nyulasi, Bálint, Tamara Teski, András György Németh, Sára Sprőber, Simig Gyula, and Balázs Volk. "Practical synthesis of variously substituted 2,3,4-benzothiadiazepine 2,2-dioxides." Synthesis, March 14, 2022. http://dx.doi.org/10.1055/a-1797-5298.

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The significant pharmacological activity of 2,3-benzodiazepine-4-ones led to an increased interest in this compound family. However, the literature of the closely related 2,3,4-benzothiadiazepine 2,2-dioxides is rather scarce. Earlier we elaborated a synthesis of 5-aryl congeners variously substituted at the aromatic ring. In the present study, a new synthetic route was investigated via highly versatile intermediates, to extend the reaction to a wider aromatic substitution pattern and to the preparation of 5-alkyl and 5-H derivatives. The essence of this approach is, starting from benzaldehyde

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32

Brindley, Jocelyn C., Jennifer M. Caldwell, G. Denis Meakins, Simon J. Plackett, and Susan J. Price. "N′-substituted N-acyl- and N-imidoyl-thioureas: preparation and conversion of N′,N′-disubstituted compounds into 2-(N,N-disubstituted amino)thiazol-5-yl ketones." J. Chem. Soc., Perkin Trans. 1, 1987, 1153–58. http://dx.doi.org/10.1039/p19870001153.

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BRINDLEY, J. C., J. M. CALDWELL, G. D. MEAKINS, S. J. PLACKETT, and S. J. PRICE. "ChemInform Abstract: N′-Substituted N-Acyl- and N-Imidoyl-thioureas: Preparation and Conversion of N′,N′-Disubstituted Compounds into 2-(N,N-Disubstituted Amino)thiazol-5-yl Ketones." ChemInform 18, no. 37 (1987). http://dx.doi.org/10.1002/chin.198737209.

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