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Journal articles on the topic 'Thiazole Derivatives'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

Borde, Ramesh M., Satish B Jadhav, Rahul R Dhavse, and Achut S Munde. "DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF SOME NOVEL BIS-THIAZOLE DERIVATIVES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 4 (2018): 164. http://dx.doi.org/10.22159/ajpcr.2018.v11i4.23413.

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Objective: A series of substituted 5,2-bis-thiazoles derivatives were synthesized by Hantzsch reaction and evaluated in vitro for antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus. Methods: 2-(4-(benzyloxy)phenyl)-4-methylthiazole-5-carbothioamide were synthesized and allowed to react with various α-haloketones to give 5,2-bis-thiazoles, i.e., 2-(4-(benzyloxy)phenyl)-4-methyl-5-(4-substituted thiazol-2-yl)thiazole derivatives in excellent yield. The synthesized compounds were characterized by spectroscopic methods as well as e

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2

Mohareb, Rafat M., Amira E. M. Abdallah, and Ebtsam A. Ahmed. "Synthesis and cytotoxicity evaluation of thiazole derivatives obtained from 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene- 3-carbonitrile." Acta Pharmaceutica 67, no. 4 (2017): 495–510. http://dx.doi.org/10.1515/acph-2017-0040.

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Abstract Reactivity of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3- carbonitrile towards thioglycolic acid resulted in thiazole derivative 1. The latter reacted with different chemical reagents to give thiazole, pyrano[2,3-d]thiazole and thiazolo[ 4,5-d]thiazole derivatives. Cytotoxicity effects of the newly synthesized products against six cancer cell lines, namely, human gastric cancer (NUGC), human colon cancer (DLD- 1), human liver cancer (HA22T and HEPG-2), human breast cancer (MCF) and nasopharyngeal carcinoma (HONE-1) as well as against a normal fibroblast cell (WI-38) were evaluated.

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3

Erguc, Ali, Mehlika Dilek Altintop, Ozlem Atli, et al. "Synthesis and Biological Evaluation of New Quinoline-Based Thiazolyl Hydrazone Derivatives as Potent Antifungal and Anticancer Agents." Letters in Drug Design & Discovery 15, no. 2 (2018): 193–202. http://dx.doi.org/10.2174/1570180814666171003145227.

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Background: In medicinal chemistry, thiazoles have gained great importance in antifungal and anticancer drug design and development. Objectives: The aim of this study was to synthesize new quinoline-based thiazolyl hydrazone derivatives and evaluate their anticandidal and anticancer effects. Methods: New thiazolyl hydrazone derivatives were evaluated for their anticandidal effects using disc diffusion method. Ames MPF assay was carried out to determine the genotoxicity of the most effective antifungal derivative. MTT assay was also performed to assess the cytotoxic effects of the compounds on

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4

Ram, Sevak Verma*1 Nitin Mittal2 Bhumika Yogi3 Shikha Sharma4 Abhishek Mishra5. "A Review On Chemistry And Antimicrobial Activity Of Thiazole." International Journal in Pharmaceutical Sciences 2, no. 3 (2024): 1184–201. https://doi.org/10.5281/zenodo.10893122.

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The recent study classe of five-membered heterocyclic compounds is thiazoles. Several thiazoles, both synthetic and natural, and their derivatives exhibited strong biological activity. Thiazole derivatives exhibit strong antibacterial action against a variety of bacterial species & diseases because of their special characteristics. As a result, the current study assigns different thiazoles and there derivatives' antimicrobial activity. Through the use of many databases, every pertinent piece of literature has been examined. The important studies on the antibacterial activity of thiazole de

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5

Tokárová, Zita, and Anna Biathová. "Synthesis and structure-physicochemical properties relationship of thiophene-substituted bis(5,4-d)thiazoles." Nova Biotechnologica et Chimica 17, no. 2 (2018): 193–200. http://dx.doi.org/10.2478/nbec-2018-0020.

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Abstract Substituted thiophene-2-carbaldehydes 1a-dwere utilized in the synthesis of symmetrically substituted thiazolo[5,4-d]thiazoles 3a-d. Bis(5,4-d)thiazoles with thiophene core at the termini are the most employed in the chemistry of materials but exhibit insufficient solubility in majority of organic solvents with notable impact on the low yields of products. Accordingly, the synthetic approach towards 2,5-dithiophen- 2-yl-thiazolo[5,4-d]thiazole (3a) and its substituted derivatives 3b-d is discussed under the various reaction conditions. Appropriate structural characterisations are incl

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6

Nayak, Swarnagowri, and Santhosh L. Gaonkar. "A Review on Recent Synthetic Strategies and Pharmacological Importance of 1,3-Thiazole Derivatives." Mini-Reviews in Medicinal Chemistry 19, no. 3 (2019): 215–38. http://dx.doi.org/10.2174/1389557518666180816112151.

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Thiazole is the most common heterocyclic compound in heterocyclic chemistry and in drug design. Presence of several reaction sites in the thiazole moiety extends their range of applications and leads to new solutions for challenges in synthetic and medicinal chemistry. Thiazole derivatives are widely used as bioactive agents, liquid crystals, sensors, catalysts, etc. The motivating molecular architecture of 1,3-thiazoles makes them suitable moieties for drug development. In this review, our aim is to corroborate the recent data available on various synthetic strategies and biological propertie

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7

Dekate, Shital M., Kishor M. Hatzade, and Ajay M. Ghatole. "A Facile Synthesis of Thiazole Derivatives bearing Imidazole Moiety, Schiff Bases and their O-Glucosides." Asian Journal of Chemistry 35, no. 1 (2022): 29–38. http://dx.doi.org/10.14233/ajchem.2023.24049.

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A unique approach for the synthesis of new thiazole O-glycosides is presented in this work. 2-Amino-4-hydroxy-phenyl-1,3-thiazole-5-carboxaldehyde (3a) was reacted with phenyl glyoxal and benzil to form 4-(4-hydroxy-phenyl)-5-(4-phenyl-1H-imidazol-2-yl)-thiazol-2-amine (4a) and 4-(4-hydroxy-phenyl)-5-(4,5-diphenyl-1H-imidazol-2-yl)-thiazol-2-amine (4b), respectively. A series of substituted Schiff bases of 4a and 4b were synthesized reacting with various aryl aldehyde to form 2-(imino substituted benzal)-4-(4-hydroxy-phenyl)-5-(4-phenyl-1H-imidazol-2-yl)-thiazoles (5a-e) and 2-(imino substitut

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8

Rayala, Ramanjaneyulu, Prakash Chaudhari, Ashley Bunnell, Bracken Roberts, Debopam Chakrabarti, and Adel Nefzi. "Parallel Synthesis of Piperazine Tethered Thiazole Compounds with Antiplasmodial Activity." International Journal of Molecular Sciences 24, no. 24 (2023): 17414. http://dx.doi.org/10.3390/ijms242417414.

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Thiazole and piperazine are two important heterocyclic rings that play a prominent role in nature and have a broad range of applications in agricultural and medicinal chemistry. Herein, we report the parallel synthesis of a library of diverse piperazine-tethered thiazole compounds. The reaction of piperazine with newly generated 4-chloromethyl-2-amino thiazoles led to the desired piperazine thiazole compounds with high purities and good overall yields. Using a variety of commercially available carboxylic acids, the parallel synthesis of a variety of disubstituted 4-(piperazin-1-ylmethyl)thiazo

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9

Yadav, Pradeep, and Y. C. Joshi. "Synthesis and Spectral Study of Novel Norfloxacin Derivatives." E-Journal of Chemistry 5, s2 (2008): 1154–58. http://dx.doi.org/10.1155/2008/357073.

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Reaction of [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinolone-3-carboxylic acid (norfloxacin) with thiazole / benzothiazole diazonium chloride to get new piperazine substituted norfloxacin derivative. These norfloxacin derivatives were further condensed with variousβ-diketone to get novel acid derivatives of 1-Ethyl-6-fluoro-4-oxo-7- [4 (thiazol-2-yldiazenyl)-piperzin-1-yl]-1,4-dihydro-quinoline-3-carboxylic acid (6a-e) and 7-(4-(benzo[d]thiazol-2-yldiazenyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (6 f-j). Structures of these compounds were

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10

Wadave, Disha. "Molecular docking study of 2,4 disubstituted thiazole derivatives as antiulcer activity." International Journal of Biology and Chemistry 17, no. 2 (2024): 154–57. https://doi.org/10.26577/ijbch2024v17.i2.12.

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In this study, 2,4 disubstituted thiazole derivatives were used to create an antiulcer agent. These compounds were chosen based on molecular properties and a drug-likeness score, ensuring their suitability for oral absorption. The molecular docking of 2,4 disubstituted thiazole derivatives was performed using AutoDock Vina Ver.1.1.2. The thiazole derivatives were constructed using Cambridge's Chem Draw Ultra 8.0 software. The program Chem 3D Ultra 8.0 was used to convert 2D structures to 3D structures. Thiazole derivatives were docked into the H2 blocker, with nizatidine binding at the active

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11

Popovych, M. V., Ya R. Shalai, S. M. Mandzynets, N. E. Mitina, O. S. Zaichenko, and A. M. Babsky. "Effect of a novel thiazole derivative and its complex with polymeric carriers on the activity of antioxidant enzymes in murine lymphoma cells." Studia Biologica 15, no. 4 (2021): 37–48. http://dx.doi.org/10.30970/sbi.1504.673.

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Background. Previous studies have shown a pronounced cytotoxic effect of thiazole derivatives in combination with polymeric carriers on tumor cells. At the same time, the derivatives were not cytotoxic against non-cancerous cells in vitro. It was shown that thiazole derivatives at concentrations of 10 and 50 μM affected the prooxidant and antioxidant systems of lymphoma cells in vitro. The aim of this work was to study the effect of the complex of thiazole derivative N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide (BF1) in combination with polymeric carriers poly(VEP-co-G

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12

Shanmitha Jahnavi Kanchumarthy, Rasajna G, Govindarao Kamala, et al. "Current Advances in Synthesis and Therapeutic Applications of Thiazole and its Derivatives." Journal of Pharma Insights and Research 2, no. 6 (2024): 107–14. https://doi.org/10.69613/4ph6pj28.

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Thiazole, a five-membered heterocyclic compound with sulfur and nitrogen atoms, serves as a fundamental scaffold in medicinal chemistry. The aromatic nature and diverse substitution patterns of the thiazole ring system enable its extensive applications in drug development. Multiple synthetic routes, from classical Hantzsch synthesis to modern methods, yield varied thiazole derivatives under specific reaction conditions. The biological importance of thiazole-containing compounds extends to anticancer, antimicrobial, and antidepressant activities. Several thiazole-based drugs have demonstrated s

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13

Slyvka, N. Yu, L. M. Saliyeva, V. I. Zhylko, V. M. Tkachuk, and M. V. Vovk. "Synthesis and antioxidant activity of new 2-(2-oxoindoline-3-ylydene) substituted 5,6-dihydroimidazo[2,1-b]thiazolones and 6,7-dihydro-thiazolo[3,2-a]pyrimidinones." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 1 (February 2025): 71–79. https://doi.org/10.32434/0321-4095-2025-158-1-71-79.

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The paper presents the results of the study on the interaction of 5,6-dihydroimidazo[2,1-b]thiazoles and 6,7-dihydrothiazolo[3,2-a]pyrimidines with isatin derivatives. It was established that the condensation of the indicated reagents occurs selectively upon heating and without the use of a catalyst with the formation of addition products, 2-(2-oxoindolin-3-ylidene)-5,6-dihydroimidazo[2,1-b]thiazole-3(2H)-ones 6a–d and 2-(2-oxoindolin-3-ylidene)-6,7-dihydro-2H-thiazolo[3,2-a]pyrimidin-3(5H)-ones 7a–c, the structure of which was rigorously proven by 1H NMR (13C) spectroscopy and chromatography-

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14

Sinenko, Vitalii O., Oleksandr V. Los, Lyudmyla M. Potikha, and Volodymyr S. Brovarets. "Functionalized 1,3-thiazoles by combined halogen dance." Current Chemistry Letters 13, no. 4 (2024): 695–706. http://dx.doi.org/10.5267/j.ccl.2024.5.001.

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It has been reported that the halogen dance reaction can be used to synthesize polyfunctionalized 1,3-thiazoles. The transformation into target products was carried out by lithiation of 2-bromo-5-(1,3-dioxolan-2-yl)-1,3-thiazole with lithium diisopropylamide (LDA) followed by treatment with various electrophiles. The obtained compounds were then successfully applied to prepare novel 4,5-difunctional thiazole derivatives.

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15

Mohareb, Rafat M., Amr S. Abouzied, and Nermeen S. Abbas. "Synthesis and Biological Evaluation of Novel 4,5,6,7-Tetrahydrobenzo[D]-Thiazol-2- Yl Derivatives Derived from Dimedone with Anti-Tumor, C-Met, Tyrosine Kinase and Pim-1 Inhibitions." Anti-Cancer Agents in Medicinal Chemistry 19, no. 12 (2019): 1438–53. http://dx.doi.org/10.2174/1871520619666190416102144.

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Background: Dimedone and thiazole moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. Thiazole derivatives are a very important class of compounds due to their wide range of pharmaceutical and therapeutic activities. On the other hand, dimedone is used to synthesize many therapeutically active compounds. Therefore, the combination of both moieties through a single molecule to produce heterocyclic compounds will produce excellent anticancer agents. Objective: The present work repor

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16

Srilakshmi, Singagari, and Raja Sundararajan. "DESIGN, In-silico STUDIES, SYNTHESIS, CHARACTERIZATION, AND ANTICONVULSANT ACTIVITIES OF NOVEL THIAZOLE SUBSTITUTED OXAZOLE DERIVATIVES." Rasayan Journal of Chemistry 15, no. 01 (2022): 711–25. http://dx.doi.org/10.31788/rjc.2022.1516762.

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A potent antiepileptic drug was developed by synthesizing a set of novel thiazoles substituted oxazole derivatives using multi-step synthesis. FT-IR, 1H-NMR, Mass spectroscopy, and elemental analyses are employed to confirm the structure of compounds. Molinspiration online tool was used to predict the molecular properties and molecular docking was employed to predict the antiepileptic potency of the title analogs. MES and scPTZ tests were employed to determine the antiepileptic potency of thirteen prepared novel thiazole substituted oxazole derivatives. In addition, the neurotoxicity of the co

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17

Tokárová, Zita, Renáta Gašparová, Natália Kabaňová, Marcela Gašparová, and Róbert Balogh. "Hemetsberger–Knittel and Ketcham Synthesis of Heteropentalenes with Two (1:1), Three (1:2)/(2:1) and Four (2:2) Heteroatoms." Reactions 4, no. 2 (2023): 254–73. http://dx.doi.org/10.3390/reactions4020015.

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The synthetic methods leading to furo[3,2-b]pyrroles and thiazolo [5,4-d]thiazoles are reviewed herein. Furo-, thieno- and seleno [3,2-b]pyrroles are related to heteropentalenes, containing two heteroatoms in the entire structure, one each per core. The synthetic approach follows the Hemetsberger–Knittel protocol covering three reaction steps—the nucleophilic substitution of halogen-containing aliphatic carboxylic acid esters, Knoevenagel condensation and, finally, thermolysis promoting the intramolecular cyclocondensation to O,N-heteropentalene. The Hemetsberger–Knittel reaction sequence is a

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18

El-Hagrassey, Eman A., Ehab Abdel-Latif, and Gamal M. Abdel-Fattah. "Synthesis and efficiency of new pyridine, chromene and thiazole containing compounds as antimicrobial and antioxidant agents." Bulletin of the Chemical Society of Ethiopia 36, no. 1 (2022): 137–48. http://dx.doi.org/10.4314/bcse.v36i1.12.

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ABSTRACT. The versatile scaffold, N'-(2-cyanoacetyl)-2-hydroxybenzohydrazide (3) was utilized in the production of new pyridine, chromene and thiazole derivatives as antimicrobial and antioxidant agents. The synthetic strategy involves the treatment of precursor 3 with various arylidene-malononitrile and 3-aryl-2-cyanoacrylate compounds to furnish substituted pyridines 5 and 7. The interaction of 3 with salicylaldehyde and/or phenyl isothiocyanate followed by cyclization with chloroacetone produced the corresponding 2-imino-2H-chromene-3-carbohydrazide and (thiazol-2-ylidene-acetyl)-salicylic

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19

Omer, Rebaz A., Karzan M. Ahmed, Khdir A. Othman, et al. "New Thiazole Derivatives." ARO-THE SCIENTIFIC JOURNAL OF KOYA UNIVERSITY 12, no. 2 (2024): 10–22. http://dx.doi.org/10.14500/aro.11557.

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While bacterial superbugs have garnered much attention, the rise of antifungal resistance poses a growing threat. This study explores the potential of newly synthesized 2,5-Bis(3,4 Dialkoxy Phenyl) Thiazolo[5,4-d] Thiazoles (DATTn compounds) as antifungal agents. Notably, DATTn compounds demonstrated significant fungicidal activity against Candida albicans, a major fungal pathogen, whereas remaining largely ineffective against common bacterial strains, such as Staphylococcus aureus and Escherichia coli. In silico docking simulations using Schrödinger suites unveiled the molecular basis for thi

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20

Petrou, Anthi, Maria Fesatidou, and Athina Geronikaki. "Thiazole Ring—A Biologically Active Scaffold." Molecules 26, no. 11 (2021): 3166. http://dx.doi.org/10.3390/molecules26113166.

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Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature surve

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21

Urleb, Uro?, Richard Neidlein, and Walter Kramer. "Synthesis of Thiazole and Fused Thiazolo Derivatives." Helvetica Chimica Acta 76, no. 1 (1993): 431–40. http://dx.doi.org/10.1002/hlca.19930760127.

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22

Yamsani, Neeharika\, and Raja Sundararajan. "ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF NOVEL HETEROCYCLIC SUBSTITUTED THIAZOLE DERIVATIVES." Rasayan Journal of Chemistry 15, no. 01 (2022): 461–74. http://dx.doi.org/10.31788/rjc.2022.1516737.

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A set of new heterocyclic substituted thiazole derivatives were synthesized as powerful analgesic and antiinflammatory agents with minimal ulcer index. Spectroscopic and elemental analyses were employed to confirm the chemical structures of the prepared compounds. Molecular properties, ADME properties, drug-likeness scores, and toxicities of title compounds were predicted using insilico studies. In addition, title compounds were docked against two proteins namely, 3KK6 and 3LN1 using AutoDock 4.2. Tail-flick method and carrageenan-induced foot paw oedema methods were used to screen in vitro an

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23

Gobala Krishnan P, Gnanaprakash K, and Chandrasekhar KB. "Design, synthesis, characterization and antitubercular activity of some nov-el 2, 4-disubstituted thiazole derivatives." International Journal of Research in Pharmaceutical Sciences 10, no. 2 (2019): 1504–9. http://dx.doi.org/10.26452/ijrps.v10i2.729.

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Literature reviews reveal that thiazole and pyrazine carboxamide derivatives exhibit anticonvulsant, antimicrobial, anticancer and anti-tubercular activities due to the presence of –S-C=N- and-CO–NH- moiety. A series of thiazolyl pyrazine carboxamide derivatives (5a-j) were synthesized by condensation reaction between 2-amino, 4-substituted phenyl 2-amino thiazole and pyrazine 2-carboxylic acid. These synthesized thiazole derivatives (5a-j) were evaluated for their inhibitory activity against Mycobacterium tuberculosis (Mtb), H37Rv using microplate Alamar Blue assay (MABA). The compound, 5c an

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24

Agili, Fatimah. "Novel Thiazole Derivatives Containing Imidazole and Furan Scaffold: Design, Synthesis, Molecular Docking, Antibacterial, and Antioxidant Evaluation." Molecules 29, no. 7 (2024): 1491. http://dx.doi.org/10.3390/molecules29071491.

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Carbothioamides 3a,b were generated in high yield by reacting furan imidazolyl ketone 1 with N-arylthiosemicarbazide in EtOH with a catalytic amount of conc. HCl. The reaction of carbothioamides 3a,b with hydrazonyl chlorides 4a–c in EtOH with triethylamine at reflux produced 1,3-thiazole derivatives 6a–f. In a different approach, the 1,3-thiazole derivatives 6b and 6e were produced by reacting 3a and 3b with chloroacetone to afford 8a and 8b, respectively, followed by diazotization with 4-methylbenzenediazonium chloride. The thiourea derivatives 3a and 3b then reacted with ethyl chloroacetate

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25

Aly Ibrahim, Rehab, and Rafat M. Mohareb. "The anti-proliferative activities and morphological studies of 5,6-dihydrobenzo [d]thiazole derivatives synthesized from cyclohexan-1,3-dione." Bulletin of the Chemical Society of Ethiopia 39, no. 5 (2025): 967–86. https://doi.org/10.4314/bcse.v39i5.12.

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This study focused on the synthesis of various benzo[d]thiazole derivatives with different substituents, exploring their potential as anticancer agents. The key starting material was 2-amino-5,6-dihydrobenzo[d]thiazol-7(4H)-one (4), which was synthesized through the reaction of 2-bromocyclohexane-1,3-diketone with thiourea. Compound 4 was then used to create azine and azole derivatives based on the benzo[d]thiazole core structure. The cytotoxicity of all the synthesized compounds was evaluated against several cancer cell lines, with many demonstrating notable inhibitory activity. The compounds

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Popovych, M. V., Ya R. Shalai, V. P. Hreniukh, et al. "Effect of thiazole derivative complexed with nanoscale polymeric carriers on cellular ultrastructure of murine lymphoma cells in vivo." Studia Biologica 15, no. 2 (2021): 15–24. http://dx.doi.org/10.30970/sbi.1502.653.

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Background. A pronounced cytotoxic action of the thiazole derivatives complexed with polymeric carriers on tumor cells in vitro was reported earlier, while no cytotoxicity of these compounds was detected toward noncancerous cells. It was found that thiazole derivatives at concentrations of 10 and 50 µM affected lymphoma cell ultrastructure in vitro. The purpose of this work was to investigate the effect of thiazole derivative 8-methyl-2-Me-7-[trifluoromethyl-phenylmethyl]-pyrazolo-[4,3-e]-[1,3]- thiazolo-[3,2-a]-pyrimidin-4(2H)-one (PP2) and its complexes with polymeric carriers poly(VEP-co-GM

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Dighe, Rajendra Dnyandeo, Vinod A. Bairagi, Parag A. Pathade, and Yogesh T. Sonawane. "Virtual screening of synthesized thiazole derivatives for M. tuberculosis and dTDP-rhamnose inhibitors." Journal of Drug Delivery and Therapeutics 9, no. 1 (2019): 207–10. http://dx.doi.org/10.22270/jddt.v9i1.2324.

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To determine antimycobacterium and dTDP rhamnose inhibitor activity of the synthesized azetidinone, thiazolidinone derivatives of thiazole, we studied different derivatives for the activity. One pot synthesis of 2-amino-4-methylthiazole-5-carboxylic acid ethyl ester has been carried out and synthesized different derivative compounds. Compounds were tested for antimicrobial activity against different strains of microorganism and antitubercular activity against M. tuberculosis H37Rv. Compounds 7c, 7d, 7i, 8d, 8e, 8g and 8h, were showed antimicrobial activity against Staphylococcus aureus, Escher

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Hitesh, Hitesh Amrutlal. "Synthesis, Characterization and Antifungal Activity of Novel Thiazolo-Pyrimidine Fused Heterocycles." ECS Transactions 107, no. 1 (2022): 1165–72. http://dx.doi.org/10.1149/10701.1165ecst.

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In medicinal chemistry, nitrogen and sulphur containing heterocyclic compounds are well known for their therapeutic properties.(1) Among them thiazole and pyrimidine derivatives possess diverse pharmaceutical activities.(2,3) More particularly thiazolo-pyrimidine fused shows various therapeutically activities like, anticancer, antimicrobial, antibacterial effects, antiviral ,etc (4-7). Such type of fused heterocycles containing furan and naphthalene moieties has not been developed. Thus, the aim of the present work to study the novel fused thiazolo-pyrimidine derivatives, their characterizatio

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Kavaliauskas, Povilas, Birutė Grybaitė, Rita Vaickelionienė, et al. "Synthesis and Development of N-2,5-Dimethylphenylthioureido Acid Derivatives as Scaffolds for New Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens." Antibiotics 12, no. 2 (2023): 220. http://dx.doi.org/10.3390/antibiotics12020220.

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The growing antimicrobial resistance to last-line antimicrobials among Gram-positive pathogens remains a major healthcare emergency worldwide. Therefore, the search for new small molecules targeting multidrug-resistant pathogens remains of great importance. In this paper, we report the synthesis and in vitro antimicrobial activity characterisation of novel thiazole derivatives using representative Gram-negative and Gram-positive strains, including tedizolid/linezolid-resistant S. aureus, as well as emerging fungal pathogens. The 4-substituted thiazoles 3h, and 3j with naphthoquinone-fused thia

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Fizer, O. I., M. M. Fizer, A. O. Kryvoviaz, and M. V. Slivka. "INVESTIGATION OF THE INFLUENCE OF THE SUBSTITUTE IN THE THIRD POSITION ON THE ELECTRONIC STRUCTURE OF 1,3-THIAZOLO[2,3-c][1,2,4]TRIAZOLE." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 46, no. 2 (2022): 55–62. http://dx.doi.org/10.24144/2414-0260.2021.2.55-62.

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Condensed 1,2,4-triazole derivatives exhibit a wide range of biological activity. In particular, triazolam, alprazolam and estazolam, which contain [1,2,4]triazolo[4,3-a][1,4]benzodiazepine system, are used as tranquilizers. Brotizolam is another tranquilizer, a derivative of thieno[3,2-f][1,2,4]triazolo [4,3-a][1,4]diazepine. The oral hypoglycemic drug sitagliptin contains the [1,2,4]triazolo[4,3-a]pyrazine system. In addition, pesticides such as flumetsulam, metosulam, cloransulam, diclosulam, florasulam, are derivatives of [1,2,4]triazolo[1,5-a]pyrimidine, [1,2,4]triazolo[1,5-c]pyrimidine a

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31

Hua, Shuanghui, Jimin Moon, and Taeho Lee. "The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives." Molecules 30, no. 2 (2025): 430. https://doi.org/10.3390/molecules30020430.

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A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-d]pyrimidin-7(6H)-one structure was synthesized through efficient Thorpe–Ziegler and cyclization reactions. The thiazolo[4,5-d]pyrimidin-7(6H)-one derivative library with a diversity of three had a total of four synthesis steps and 57 compounds. In addition, the yield per synthesis step was 65–97%, which was very high. The developed synthesis method and compounds will be used to find compounds with biological activity through the thiazole derivative structu

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32

Kupczyk, Daria, Renata Studzińska, Rafał Bilski, Szymon Baumgart, Renata Kołodziejska та Alina Woźniak. "Synthesis of Novel 2-(Isopropylamino)thiazol-4(5H)-one Derivatives and Their Inhibitory Activity of 11β-HSD1 and 11β-HSD2 in Aspect of Carcinogenesis Prevention". Molecules 25, № 18 (2020): 4233. http://dx.doi.org/10.3390/molecules25184233.

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Glucocorticoid metabolism at the tissue level is regulated by two isoenzymes 11β-hydroxysteroid dehydrogenase (11β-HSD), which mutually convert biologically active cortisol and inactive cortisone. Recent research is focused on the role of 11β-HSD1 and 11β-HSD2 as autocrine factors of tumor cell proliferation and differentiation. Herein, we report the synthesis of novel 2-(isopropylamino)thiazol-4(5H)-one derivatives and their inhibitory activity for 11β-HSD1 and 11β-HSD2. The derivative containing the spiro system of thiazole and cyclohexane rings shows the highest degree of 11β-HSD1 inhibitio

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33

Tejashree, Deokule. "1,3,4-Thiadiazole and its Derivatives: A Versatile Moiety." Medicinal Chemistry 13, no. 1 (2023): 9. https://doi.org/10.37421/2161-0444.2023.13.660.

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The evaluation of thiazole's biological activity, such as antibacterial, antiprotozoal, antitubercular, antifungal and anthelmintic, with an emphasis on their potential medicinal applications, is desirable because the thiazole has an important component effect on the pharmacophores of a large number of medicinally significant molecules. We are particularly interested in investigating newly synthesized aminothiazoles, particularly 2-aminothiazole derivatives, a class of heterocyclic ring systems with antiviral, antimicrobial, anticancer and anti-inflammatory properties, respectively. Numerous h

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34

Sharma, Gyanendra Kumar, Gurvinder Pal Singh, Harsh Bhardwaj, et al. "Microwave-assisted synthesis of some new 2-(substituted phenyl)-3-(thiazol-2-yl)imidazo[4,5-b]indoles of biological interest." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 373. http://dx.doi.org/10.59467/ijhc.2024.34.373.

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In the present investigation, we have synthesized some new 2-(substituted phenyl)-3-(thiazol-2-yl) imidazo[4,5-b]indoles (1b-8b) of biological interest. In the last step of the synthesis, N-(substituted benzylidene)thiazole-2- amines (1a-8a) were reacted with isatin and ammonium acetate using silica gel as the solid support to yield the corresponding substituted thiazolyl imidazo indole derivatives (1b-8b). The reactions were carried out by two different techniques - conventional and microwave irradiation. The microwave irradiation method offers excellent yield, lesser reaction time, and eco-e

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35

Raslan, M. A., and S. M. Sayed. "Synthesis of some new thiazolo[3,2‐ a ]pyridine, bi‐thiazole‐thiazole , bi‐thiazole‐pyrazole and bi‐thiazole‐thiophene derivatives." Journal of Heterocyclic Chemistry 57, no. 7 (2020): 2862–74. http://dx.doi.org/10.1002/jhet.3995.

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36

Raut, Dattatraya G., Sandeep B. Patil, Prafulla B. Choudhari, et al. "POCl3 Mediated Syntheses, Pharmacological Evaluation and Molecular Docking Studies of Some Novel Benzofused Thiazole Derivatives as a Potential Antioxidant and Anti-inflammatory Agents." Current Chemical Biology 14, no. 1 (2020): 58–68. http://dx.doi.org/10.2174/2212796813666191118100520.

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Background: The present research work is focused on the development of alternative antioxidant and anti-inflammatory agents. The review of the literature reveals that many benzofused thiazole analogues have been used as lead molecules for the design and development of therapeutic agent, including anticancer, anti-inflammatory, antioxidant and antiviral. The synthesized benzofused thiazole derivatives are evaluated for in vitro antioxidant, anti-inflammatory activities and molecular docking study. Thus, the present research work aims to synthesize benzofused thiazole derivatives and to test the

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37

Drašar, Pavel, Vladimír Pouzar, Ivan Černý, George R. Pettit, and Miroslav Havel. "Synthesis and in vitro antimetabolic evaluation of some steroidal thiazoles." Collection of Czechoslovak Chemical Communications 54, no. 12 (1989): 3339–47. http://dx.doi.org/10.1135/cccc19893339.

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Steroidal thiazoles VI-XII have been synthesized. The starting bromoketones XVII and XX were prepared by bromination of pregnan-20-ones in position 21 with copper(II) bromide, and used for synthesis of the thiazole derivatives employing the Hantzch reaction. Preliminary biological evaluation of thiazoles I-XII against the P388 lymphocytic leukemia cell line showed growth inhibition values of ED50 2.9 and 7 μg/ml for thiazoles II and VII, respectively.

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38

Mohareb, Rafat M., Abeer A. Mohamed, and Rehab A. Ibrahim. "Uses of chalcone acetophenone to synthesis heterocyclic compounds with cytotoxic and c-Met kinase activities." Bulletin of the Chemical Society of Ethiopia 36, no. 1 (2022): 149–72. http://dx.doi.org/10.4314/bcse.v36i1.13.

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ABSTRACT. The aim of present study was the uses of a series of α,β-unsaturated carbonyl compounds (chalcones), in the synthesis of pyridine, pyran, thiophene, thiazole, together with their uses in heterocyclic synthesis. The work has resulted in the synthesis of a variety of 2,5-dihydropyridine, hydrazide-hydrazone, thiophene derivatives, coumarin, pyran and thiazolo[4,5-d]thiazole derivatives. The antitumor activities of the newly synthesized products were carried out against three cancer cell lines namely MCF-7, NCI-H460 and SF-268 and normal human cell line WI38. In addition, the inhibition

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39

Sultan Alwan, Ensaf, and Rafat Milad Mohareb. "Synthesis of bioactive heterocyclic compounds using camphor." Bulletin of the Chemical Society of Ethiopia 38, no. 4 (2024): 1069–76. http://dx.doi.org/10.4314/bcse.v38i4.20.

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The aim of the work was to synthesize novel heterocyclic compounds derived from camphor with antibacterial activity. The pyridazine, xanthene, pyranothiazole, pyridinothiazole, thiophene and pyrazole derivatives were produced from 4,11,11-trimethyl-9-phenyl-7-(2-phenylhydrazono)-3,4,5,6,7,9-hexahydro-1H-1,4-methanoxanthen-8(2H)-one (1). Thiophene derivatives 6a,b were produced according to the Gewald’s reaction for thiophene synthesis. On the other hand, pyranothiazol derivatives 8a,b were synthesized by the multicomponent reactions between xanthene derivative 5, benzaldehyde and ethylcyanoace

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40

Walmik, Prabhakar, Basavaraj S. Naraboli, Swathi B, and Somashekhar Ghanti. "DESIGN, SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES CONTAINING INDOL- THIAZOLYL- THIAZOLIDINONE DERIVATIVES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 3 (2018): 113. http://dx.doi.org/10.22159/ajpcr.2018.v11i3.22199.

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Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7- trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7- trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c).Methods: All the newly synthesized compounds were characterized by infrared, 1H, 13C nuclear magnetic resonance and mas

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41

Liu, Xiang-Wei, Jiang-Ling Shi, Jiang-Bo Wei, et al. "Diversified syntheses of multifunctionalized thiazole derivatives via regioselective and programmed C–H activation." Chemical Communications 51, no. 22 (2015): 4599–602. http://dx.doi.org/10.1039/c4cc10419f.

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The direct construction of 5-alkenylated thiazole derivatives from 2-/4-substituted thiazole derivatives or challenging thiazole via palladium-catalyzed regioselective 5-alkenylation has been realized.

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42

Vastag, Gy, E. Szöcs, A. Shaban, and E. Kálmán. "New inhibitors for copper corrosion." Pure and Applied Chemistry 73, no. 12 (2001): 1861–69. http://dx.doi.org/10.1351/pac200173121861.

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The study of the effectiveness of several potential copper corrosion inhibitors in acidic media was studied. The investigated thiazole derivative functional groups contain heterocyclic atoms such as nitrogen, sulfur, and oxygen. Thiazole derivatives, 5-benzylidene-2,4-dioxotetrahydro-1,3-thiazole (BDT) 5-(4¢-isopropylbenzylidene)-2,4-dioxotetrahydro-1,3-thiazole (IPBDT), 5-(3¢-thenylidene)-2,4-dioxotetrahydro-1,3-thiazole (TDT), and 5-(3¢,4¢-dimetoxybenzylidene)-2,4-dioxotetrahydro-1,3-thiazole (MBDT) were tested for copper corrosion inhibition properties. The electrolyte solution was 0.1 M Na

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43

Ramadan, El Sayed, Hamida M. Abdel Hamid, Sawsan A. Noureddin, and Khadija O. Badahdah. "Synthesis, characterization, and antitumor activity of some novel S-functionalized benzo[d]thiazole-2-thiol derivatives; regioselective coupling to the –SH group." Zeitschrift für Naturforschung B 73, no. 9 (2018): 647–54. http://dx.doi.org/10.1515/znb-2018-0078.

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AbstractSeveral 2-substituted sulfanyl benzo[d]thiazoles were regioselectively synthesized by the reaction of benzo[d]thiazole-2-thiol (1a) with a variety of reagents under different basic conditions. Some 2-(2,3-disubstituted propyl sulfanyl)benzo[d]thiazoles were obtained from 2-(allylthio)benzo[d]thiazole, which was prepared by the allylation of 1a with allyl bromide in the presence of sodium hydride in dry N,N-dimethylformamide. Reaction of 1a with various pyrazolyl-quinoxaline derivatives was also investigated. Better yields and shorter reaction time were achieved for the synthesis of som

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44

Zhang, Xiying, Xiaohua Liu, Jianlin Zhang, Dong Zhang, Lili Lin, and Xiaoming Feng. "Enantioselective [3 + 2] cycloaddition and rearrangement of thiazolium salts to synthesize thiazole and 1,4-thiazine derivatives." Organic Chemistry Frontiers 5, no. 13 (2018): 2126–31. http://dx.doi.org/10.1039/c8qo00370j.

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A highly efficient catalytic asymmetric [3 + 2] cycloaddition/rearrangement cascade of thiazolium N-ylides with various electron-deficient 2-π components was achieved, providing a convenient method to access hydropyrrolo-thiazole and hydropyrrolo-thiazine derivatives.

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45

Choi, Won-Sik, Seok-Woo Nam, Il-Doo Kim, et al. "Synthesis and Pesticidal Activities of 5-(2-Cyclopropylaminopyrimidin-4-yl)-4-(thiophenyl)thiazole Derivatives." Journal of Chemistry 2015 (2015): 1–6. http://dx.doi.org/10.1155/2015/241793.

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Pesticidal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluoro-phenyl)thiazol-2-yl]-1-methylpiperidine, designated as Comp I, have been determined against a mosquito larva,Culex pipiens pallens, and a phytopathogenic fungus,Phytophthora capsici. Comp I was used as the leading compound in this study. The compounds were synthesized by reacting them with two functional groups, 3-thiophenyl and 2-thiophenyl groups, instead of 4-chloro-2-fluorophenyl group in Comp I. Other functional groups such as 2-aminothiazole, 2-(1-methylpiperazin-4-yl)thiazole, and 2-(piperazin-4-yl)thi

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46

Lagoja, Irene M., Koen Nauwelaerts, Christine Bal-Mahieu, Michela Pasqualini, Christian Bailly, and Piet Herdewijn. "Synthesis and Leukemia Cell Growth Inhibition of a Series of 1,3-Dithiazolylbenzene Derivatives." Collection of Czechoslovak Chemical Communications 69, no. 7 (2004): 1491–98. http://dx.doi.org/10.1135/cccc20041491.

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By a slightly modified Hantzsch thiazole synthesis either 1,3-bis[(thiazol-2-yl)amino]benzene derivatives 2 or 1,3-bis[2-iminothiazol-3(2H)-yl]benzene derivatives 3 were exclusively obtained. The compounds can be distinguished by NMR spectroscopy. Compounds 2a-2d and 3a-3d were evaluated for their potential antitumor activity, DNA interaction, and for their activity against DNA and RNA viruses and against HIV-1 and HIV-2.

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47

Eldin, Sanaa M. "Reactions of Cyanothioacetamide Derivatives with 2-Hydrazinothiazol-4(5H)-one: Synthesis, Cyclization and Biological Evaluation of Several New Annelated Pyran, Thiazole, 1,2,4-Triazole and 1,2,4-Triazine Derivatives." Zeitschrift für Naturforschung B 54, no. 12 (1999): 1589–97. http://dx.doi.org/10.1515/znb-1999-1218.

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The thiocarboxamidocinnamonitriles (2) reacted with 2-hydrazinothiazol-4(5H)-one (3) to afford the corresponding pyrano[2,3-d]thiazoles (6). Compounds 6 were used for the synthesis of several new annelated pyran, thiazole, 1,2,4-triazole and 1,2,4-triazine derivatives via their reactions with chloroacetic acid, ethyl chloroformate, diethyl oxalate and acetylacetone. Structures were established based on elemental and spectral data studies. Some of the newly synthesized heterocyclic derivatives were tested for their antimicrobial activity.

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48

Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Thiophenyl Thiazole Based Novel Quinoxaline Derivatives." International Letters of Chemistry, Physics and Astronomy 51 (May 2015): 115–24. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.51.115.

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A new series of thiophenyl thiazole based novel quinoxaline derivatives 4a-4t have been synthesized by base catalysed condensation reaction. In which 6-substituted 2,3-dichloroquinoxaline 1a and 4-(thiophen-2-yl) thiazol-2-amine 2b reacted in basic condition to afford intermediate 3c which reacts with various aromatic amine to form final compounds. Easy experimental procedure, high yield, and selectivity are the imperative features of this method. The identity of all the compounds has been established by 1H NMR, 13C NMR, FT-IR, and elemental analysis.

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Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Thiophenyl Thiazole Based Novel Quinoxaline Derivatives." International Letters of Chemistry, Physics and Astronomy 51 (May 15, 2015): 115–24. http://dx.doi.org/10.56431/p-oioid3.

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A new series of thiophenyl thiazole based novel quinoxaline derivatives 4a-4t have been synthesized by base catalysed condensation reaction. In which 6-substituted 2,3-dichloroquinoxaline 1a and 4-(thiophen-2-yl) thiazol-2-amine 2b reacted in basic condition to afford intermediate 3c which reacts with various aromatic amine to form final compounds. Easy experimental procedure, high yield, and selectivity are the imperative features of this method. The identity of all the compounds has been established by 1H NMR, 13C NMR, FT-IR, and elemental analysis.

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Simiran, Singh Anila Mishra*. "Thiazole Derivatives in Diabetes Management: Recent Progress and Future Perspective." International Journal of Pharmaceutical Sciences 3, no. 5 (2025): 3020–27. https://doi.org/10.5281/zenodo.15458382.

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Objectives: This review explores the potential of thiazole derivatives as innovative anti-diabetic agents, emphasizing their structural diversity and effectiveness in Type-II diabetes mellitus.  Theoretical Framework: Diabetes mellitus (DM), characterized by chronic hyperglycemia, is a progressive metabolic disorder affecting millions worldwide. Heterocyclic compounds, mainly thiazole derivatives, have recently shown promise as novel anti-diabetic agents with the potential to target specific mechanisms in DM2. Method: This review focuses on findings from recent studies on thiazole derivat

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