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Journal articles on the topic 'Thiazoles'

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Published: 4 June 2021

Last updated: 25 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

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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3

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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4

Hosseini, Akram Karbalaee, and Azadeh Tadjarodi. "Luminescent MOFs Based on Thiazolo[5,4-d]thiazole as a Chemosensor for the Detection of Environmental Contaminants." Journal of Nanotechnology and Nanomaterials 5, no. 1 (2024): 1–6. http://dx.doi.org/10.33696/nanotechnol.5.047.

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Luminescent metal-organic frameworks (LMOFs) are considered special candidates for the sensation and detection of particular analytes. Thiazolo[5,4-d]thiazoles (TTZs) are an ideal type of heterocycles for fluorophores with π-bridge moieties demonstrating structure-function characteristics. LMOFs with excellent sensing properties can be constructed by incorporating heterocyclic aromatic thiazolo[5,4-d]thiazole into the framework. This study has elaborated on LMOFs containing thiazolo[5,4-d]thiazole unit for the detection of environmental contaminants, such as toxic anions, aromatic compounds, a

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5

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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6

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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7

Turov, Kostyantyn. "Anticancer evaluation of di- and trifunctional substituted 1,3-thiazoles." Ukr. Bioorg. Acta 2020, Vol. 15, N1 15, no. 1 (2020): 2–11. http://dx.doi.org/10.15407/bioorganica2020.01.002.

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Anticancer activity of a series of polyfunctional substituted 1,3-thiazoles has been studied within the international scientific program “NCI-60 Human Tumor Cell Lines Screen”. Screening was performed in vitro on 60 cell lines of lungs, kidneys, CNS, ovaries, prostate, and breast cancer, epithelial cancer, leukemia, and melanoma. The most effective compounds were those with a piperazine substituent at C2 of the 1,3-thiazole cycle: 1-(4-((4-methylphenyl)-sulfonyl)-2-phenyl-1,3-thiazol-5-yl)piperazine (average lg GI50 = -5.87, lg TGI = -5.54, lg LC50 = -5.21), 1-(2-(3,5-dimethyl-1H-pyrazol-1-yl)

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8

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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9

Arshad, Mohammed F., Aftab Alam, Abdullah Ayed Alshammari, et al. "Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents." Molecules 27, no. 13 (2022): 3994. http://dx.doi.org/10.3390/molecules27133994.

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For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor–acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemica

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10

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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11

Nguyễn, Thiên Thuý Trang, Jean-François Longevial, and Stéphanie Hesse. "Synthesis of Thiazolo[5,4-d]thiazoles in an Eco-Friendly L-Proline–Ethylene Glycol Mixture." Molecules 30, no. 4 (2025): 938. https://doi.org/10.3390/molecules30040938.

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The hazardousness of solvents used in synthetic organic chemistry is well established. In this context, it is relevant to search for safer and greener alternatives. Within the last decades, deep eutectic solvents have been considered as possible and promising alternatives. Consequently, this study aims at using deep eutectic solvents to synthesize an emerging class of heteroaromatic compounds named thiazolo[5,4-d]thiazoles, for which interest is growing in the field of organics, electronics, and biology. To address this challenge, we developed a straightforward synthetic protocol consisting of

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12

Singh, Inder P., Shiv Gupta, and Sanjay Kumar. "Thiazole Compounds as Antiviral Agents: An Update." Medicinal Chemistry 16, no. 1 (2020): 4–23. http://dx.doi.org/10.2174/1573406415666190614101253.

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Background: Thiazole is a good nucleus owing to its various pharmaceutical applications. Thiazole containing compounds (thiazoles) have shown various biological activities like antioxidant, analgesic, antibacterial, anticancer, antiallergic, antihypertensive, antiinflammatory, antimalarial, antifungal and antipsychotic. The scaffold is present in more than 18 FDA approved drugs and also in more than 70 experimental drugs. Only a few reviews are available in the literature despite its great medicinal importance. During the course of time, this scaffold has been studied extensively for its antiv

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13

Alsharif, Zakeyah A., and Mohammad A. Alam. "Modular synthesis of thiazoline and thiazole derivatives by using a cascade protocol." RSC Advances 7, no. 52 (2017): 32647–51. http://dx.doi.org/10.1039/c7ra05993k.

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14

Liu, Yi, Yuguo Du, Zhi Li та ін. "Efficient One-Pot Synthesis of 2,4-Disubstituted Thiazoles and Dimeric Thiazoles Directly from Acyl Chlorides and β-Azido Disulfides". Synthesis 49, № 21 (2017): 4876–86. http://dx.doi.org/10.1055/s-0036-1590810.

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A simple and effective one-pot cascade procedure to provide 2,4-disubstituted thiazoles and symmetrical dimeric thiazoles directly from commercially available acid chlorides and β-azido disulfides in moderate to high yields is described. This cascade transformation consists of disulfide cleavage, thiocarbonylation, phosphine-promoted intramolecular Staudinger/aza-Wittig reaction and dehydrogenation to form the corresponding thiazoles. The application of our methodology is demonstrated by the concise two-step synthesis of anticancer agent SMART and its O-linked dimer in 64% and 46% overall yiel

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15

H. El-Feky, Hesham, Talaat Y. Mohammed, Alaa S. Amin, and Mohammed A. Kassem. "Rapid extraction and separation of mercury in water and food samples based on micelles and azo-thiazoles complexation before determination by UV-Vis spectrophotometer." Analytical Methods in Environmental Chemistry Journal 6, no. 04 (2023): 19–36. http://dx.doi.org/10.24200/amecj.v6.i04.258.

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A simple and sensitive procedure has been established for analyzing mercury (II) ions spectrophotometrically in the presence of micellar medium using three azo-thiazoles complexing reagents: 2-amino-6-(thiazole-2-yldiazenyl)-3-pyridinol (C8H7N5OS), 8-hydroxy-7-(thiazole-2-yldiazenyl) quinoline-5-sulfonic acid (C12H8N4O4S2), and 1-hydroxy-4-(thiazole-2-yldiazenyl)-2-naphthoic acid (C14H9N3O3S). H1 NMR spectra validated the three azo thiazoles synthesized material. Tween 80 (polysorbate 80) and cetyltrimethylammonium bromide (C19H42BrN as molecular biology) are micellar mediums to enhance sensit

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16

Mhaske, Sadhana Dhondibhau. "Synthesis and Antimicrobial Study of Thiophene Clubbed Thiazolyl Carbohydrazides." Oriental Journal Of Chemistry 37, no. 4 (2021): 858–63. http://dx.doi.org/10.13005/ojc/370412.

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Thiophene containing thiazolyl carbohydrazide on reaction with various aryl isothiocynates yields thiosemicarbazides which were transformed into 1,2,4- substituted thiazoles by Hantzsch synthesis and characterized by spectral methods. Most of the synthesized new thiosemicarbazides are found to be promisingly effective against tested bacterial strains and exhibited moderate activitytested fungal strains. Most of the 1, 2,4- substituted thiazoles are weakly active against test organisms.

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17

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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18

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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19

Rashdan, Huda R. M., Mohamed El-Naggar, and Aboubakr H. Abdelmonsef. "Synthesis, Molecular Docking Studies and In Silico ADMET Screening of New Heterocycles Linked Thiazole Conjugates as Potent Anti-Hepatic Cancer Agents." Molecules 26, no. 6 (2021): 1705. http://dx.doi.org/10.3390/molecules26061705.

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Thiazoles are important scaffolds in organic chemistry. Biosynthesis of thiazoles is considered to be an excellent target for the design of novel classes of therapeutic agents. In this study, a new series of 2-ethylidenehydrazono-5-arylazothiazoles 5a–d and 2-ethylidenehydrazono-5-arylazo- thiazolones 8a–d were synthesized via the cyclocondensation reaction of the appropriate hydrazonyl halides 4a–d and 7a–d with ethylidene thiosemicarbazide 3, respectively. Furthermore, the thiosemicarbazide derivative 3 was reacted with different bromoacetyl compounds 10–12 to afford the respective thiazole

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20

Abu-Melha, Sraa. "Synthesis, Modeling Study and Antioxidants Activity of New Heterocycles Derived from 4-Antipyrinyl-2-Chloroacetamidothiazoles." Applied Sciences 8, no. 11 (2018): 2128. http://dx.doi.org/10.3390/app8112128.

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The present work reports the preparation of twelve new heterocyclic scaffolds containing an antipyrinyl-thiazole hybrid through the reaction of 4-antipyrinyl-2-chloroacetamido-thiazoles 1 and 6 with various types of nucleophiles, namely; ethyl thioglycolate, 2-mercaptobenzothiazole, 2-mercaptobenzoxazole, ammonium thiocyanate, malononitrile, and salicylaldehyde. The constructed compounds were characterized by conventional spectroscopic techniques (IR, 1H NMR, 13C NMR, and mass analysis). A DFT method (material studio package) was used to predict the geometry, bond lengths, bond angles, and dip

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21

Kumar, Arun, Govind Singh, and Rajiv Tonk. "In vitro Antibacterial, ADME and Toxicity Screening of Newly Synthesized 4-(Substituted phenyl)-2-(2-chloroquinolin-3-yl)thiazoles." Asian Journal of Chemistry 36, no. 5 (2024): 1199–206. http://dx.doi.org/10.14233/ajchem.2024.31700.

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A series of novel thiazole (Va-o) compounds were synthesized following multi-step synthetic process. Using analytical methods like nuclear magnetic resonance, mass spectrometry and FTIR, the elucidation of the structure of the synthesized compounds was performed. All the 15 novel thiazoles were assessed for their antibacterial activity. The synthesized thiazoles were examined for inhibitory antibacterial activity against a panel Gram-positive strain viz. Staphylococcus aureus (NCTC 65710), Streptococcus pyogenes (MTCC-442), Bacillus subtilis (NCIM 2250) and Gram-negative bacteria Pseudomonas a

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22

Andreani, Aldo, Mirella Rambaldi, and Alessandra Locatelli. "Herbicidal activity of 5-haloimidazo[2,1-b]thiazoles." Collection of Czechoslovak Chemical Communications 56, no. 11 (1991): 2430–35. http://dx.doi.org/10.1135/cccc19912430.

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23

Swaroop, Toreshettahally R., Kanchugarakoppal S. Rangappa, Maralinganadoddi P. Sadashiva, Kuppalli R. Kiran, Narasimhamurthy Rajeev та Seegehalli M. Anil. "Cyclization of Active Methylene Isocyanides with α-Oxodithioesters Induced by Base: An Expedient Synthesis of 4-Methylthio/Ethoxycarbonyl-5-acylthiazoles". Synthesis 52, № 09 (2020): 1444–50. http://dx.doi.org/10.1055/s-0039-1690821.

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Cyclization of tosylmethyl isocyanide with α-oxodithioesters in the presence of KOH is reported for the synthesis of 4-methylthio-5-acylthiazoles. Similarly, ethyl isocyanoacetate underwent cyclization with α-oxodithioesters to form 4-ethoxycarbonyl-5-acylthiazoles in the presence of DBU/EtOH. Mechanisms for the formation of thiazoles are proposed. These thiazoles can also be obtained by Takeda reaction, in which thiazole-4,5-anhydride is acylated with aromatic compounds followed by esterification; however, that approach requires two steps and suffers from the formation of a regioisomeric mixt

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24

Luo, Puying, Qiuping Ding, Yuanyuan Ping, and Jianan Hu. "Regioselective ortho-trifluoromethylthiolation of 2-arylbenzo[d]thiazole via tandem substrate-assisted C–H iodination and trifluoromethylthiolation." Organic & Biomolecular Chemistry 14, no. 10 (2016): 2924–29. http://dx.doi.org/10.1039/c6ob00005c.

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A mild and efficient tandem benzo[d]thiazole directed C–H iodination and trifluoromethylthiolation for the synthesis ofortho-trifluoromethylthiolated 2-arylbenzo[d]thiazoles have been developed using AgSCF<sub>3</sub>as a coupling partner.

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25

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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26

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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27

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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28

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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29

Luo, Laichun, Lanlan Meng, Qi Sun, Zemei Ge, and Runtao Li. "Novel synthesis of thiazolo/thienoazepine-5,8-diones from dihalo cyclic 1,3-diketones and mercaptonitrile salts." RSC Adv. 4, no. 13 (2014): 6845–49. http://dx.doi.org/10.1039/c3ra46606j.

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An efficient approach to thiazolo[4,5-b]azepine-5,8-diones and thieno[3,2-b]azepine-5,8-diones has been developed via a domino synthesis of multifunctionalized thiazoles/thiophenes and further intramolecular cyclization.

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30

Zhang, Peng-Li, Gopala Lavanya, Yang Yu, Bo Fang, and Cheng-He Zhou. "Identification of a novel antifungal backbone of naphthalimide thiazoles with synergistic potential for chemical and dynamic treatment." Future Medicinal Chemistry 13, no. 23 (2021): 2047–67. http://dx.doi.org/10.4155/fmc-2021-0162.

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Aim: The high incidence and prevalence of fungal infections call for new antifungal drugs. This work was to develop naphthalimide thiazoles as potential antifungal agents. Results & methodology: These compounds showed significant antifungal potency toward some tested fungi. Especially, naphthalimide thiazole 4h with excellent anti- Candida tropicalis efficacy possessed good hemolysis level, low toxicity and no obvious resistance. Deciphering the mechanism showed that 4h interacted with DNA and disrupted the antioxidant defense system of C. tropicalis. Compound 4h also triggered membrane de

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Borysiuk, Olha, Vasyl Zhylko, Lesya Saliyeva, et al. "Synthesis and biological activity of 2-arylidene-5,6-dihydroimidazo[2,1-b]thiazoles and 6,7-dihydro-5h-[1,3]thiazolo[3,2-a]pyrimidines." ScienceRise: Pharmaceutical Science, no. 2 (54) (April 30, 2025): 22–28. https://doi.org/10.15587/2519-4852.2025.326521.

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The aim. The present study is devoted to searching for potential biologically active agents among functionalized imidazo[2,1-b]thiazoles and thiazolo[3,2-a]pyrimidines. Materials and methods. The interaction of preparatively available 5,6-dihydroimidazo[2,1-b]thiazolone and 6,7-dihydro-2H-thiazolo[3,2-a]pyrimidinone with several substituted benzaldehydes in boiling acetic acid in the presence of anhydrous sodium acetate leads to new 2-arylidene-substituted 5,6-dihydroimidazo[2,1-b]thiazoles and 6,7-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidines as potential pharmacological agents. Their antimicrob

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32

Chiacchio, Ugo, Giuseppina Visentin, Ettore Perrone, et al. "D3-Thiazolines, D4-Thiazolines and Thiazoles from Penem Antibiotics." HETEROCYCLES 33, no. 2 (1992): 859. http://dx.doi.org/10.3987/com-91-s96.

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Thanh, Nguyen Dinh. "Synthesis of Peracetylatedβ-D-Glucopyranosyl Thioureas from Substituted 2-Aminobenzo-1ʹ, 3ʹ-thiazoles". E-Journal of Chemistry 9, № 1 (2012): 55–62. http://dx.doi.org/10.1155/2012/615601.

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Some peracetylated glucopyranosyl thioureas containing a heterocyclic ring system, benzo-1,3-thiazole have been prepared by the condensation reaction of tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate and corresponding substituted 2-amino-(6-substituted)benzo-1,3-thiazoles. Investigated heating conditions showed that the solventless microwave-assisted method gave higher yields of these thioureas.

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34

Behmaram, Bahareh, Naser Foroughifar, Neda Foroughifar, and Sara Hallajian. "Synthesis of Some Derivatives of 4-phenyl-1,3-dihydro-2H-imidazole-2-thion Using Ionic Liquid as Catalyst and Evaluation of Their Antimicrobial Activity." International Journal of Chemistry 9, no. 2 (2017): 45. http://dx.doi.org/10.5539/ijc.v9n2p45.

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The synthesis of some 1,3-diazoles and thiazoles was realized in different conditions:a) In the presence of PTSA or sulfuric acid as catalyst we obtained only diazole products(4a-d).b) In basic medium such as DABCO or sodium hydroxide and ionic liquid afforded thiazoles.c) Both products, diazoles and thiazoles were collected when using methanol as catalyst and solvent.All structures were confirmed by IR, 1H NMR and 13C NMR spectroscopy. The antibacterial activity of some synthesized compounds was investigated against Escherichia Coli (ATCC: 25922) and Serratia marcescens (ATCC: 13880) as gram

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35

Gümüş, Mehmet, Mehmet Yakan, and İrfan Koca. "Recent advances of thiazole hybrids in biological applications." Future Medicinal Chemistry 11, no. 15 (2019): 1979–98. http://dx.doi.org/10.4155/fmc-2018-0196.

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Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity. Hybrid structures are formed by the combination of different groups of chemical reactivity and biological activity characteristics. In this review, we highlight recent developments related to hybrid str

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Mokry, Cornelia, and Horst Hartmann. "Preparation and properties of 2-Dialkylamino-5-haloacetyl-thiazoles and 4-(2-Dialkylamino-5-thiazolyl)-thiazoles." Journal f�r Praktische Chemie/Chemiker-Zeitung 340, no. 4 (1998): 375–80. http://dx.doi.org/10.1002/prac.19983400413.

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M, N. JOSHI, S. BHAGWAT V, and A. PARVAH I. "Synthesis of 3'[4-Aryl-2-thiazoly1]-6'-aryl- imidazo[2,1-b]thiazoles as Possible Antibacterials." Journal of Indian Chemical Society Vol. 70, Jul 1993 (1993): 647–48. https://doi.org/10.5281/zenodo.5917960.

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Chemistry Department, Parle College, Dixit Road, Vile Parle (Last), Bombay-400 057<strong> </strong> <em>Manuscript received 20 October 1992, revised 4 January 1993<strong>, </strong>accepted 4 February 1993</em> Synthesis of 3'[4-Aryl-2-thiazolyl]-6'-aryl- imidazo[2,1-b]thiazoles as Possible Antibacterials                    

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Abu-Zaied, Mamdouh A., and Galal H. Elgemeie. "Thiazoles in glycosylation reactions: Novel synthesis of thiazole thioglycosides." Heteroatom Chemistry 28, no. 6 (2017): e21404. http://dx.doi.org/10.1002/hc.21404.

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39

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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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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Özbey, Süheyla, and Asiye Meriç. "3,4-Di-p-tolyl-6,7-dihydroimidazo[2,1-b][1,3]thiazole." Acta Crystallographica Section E Structure Reports Online 62, no. 7 (2006): o2717—o2719. http://dx.doi.org/10.1107/s160053680602099x.

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The title compound, C19H18N2S, is a member of a new series of 2,3-dihydroimidazo[2,1-b][1,3]thiazoles and was obtained from 4,5-di-p-tolyl-1,3-dihydroimidazole-2-thione and 1-bromo-2-chloroethane. The thiazole ring adopts an envelope conformation; the plane through N, S and two C atoms makes a dihedral angle of 2.35 (3)° with the fused imidazole ring. The tolyl groups are essentially planar.

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Abdelrazek, Fathy M., Sobhi M. Gomha, Mohamed E. B. Shaaban, et al. "One-Pot Three-Component Synthesis and Molecular Docking of Some Novel 2-Thiazolyl Pyridines as Potent Antimicrobial Agents." Mini-Reviews in Medicinal Chemistry 19, no. 6 (2019): 527–38. http://dx.doi.org/10.2174/1389557518666181019124104.

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Background: Thiazoles and pyridines are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential antimicrobial activity. Objective: In the efforts to develop suitable antimicrobia drugs, medicinal chemists have focused on thiazole derivatives. A novel series of 2-thiazolyl pyridines was prepared in a one-pot three-component reaction using 2-bromoacetyl pyridine as a starting precursor. Method: Structure of the synthesized compounds was elucidated by spectral data (FT-IR, 1H NMR, 13C NMR, and mass) and elemental analyses. The prepared compounds were scree

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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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VISENTIN, G., E. PERRONE, D. BORGHI та ін. "ChemInform Abstract: δ3-Thiazolines, δ4-Thiazolines, and Thiazoles from Penem Antibiotics." ChemInform 23, № 49 (2010): no. http://dx.doi.org/10.1002/chin.199249074.

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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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Elmore, J. Stephen, Donald S. Mottram, Michael Enser, and Jeff D. Wood. "Novel Thiazoles and 3-Thiazolines in Cooked Beef Aroma." Journal of Agricultural and Food Chemistry 45, no. 9 (1997): 3603–7. http://dx.doi.org/10.1021/jf970066m.

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47

Panchani, Nayan M., and Hitendra S. Joshi. "Catalyst Free and Energy Economical Synthesis of Thiazole Derivatives Bearing Azo Imine Linkage with Imidazole as Antimicrobial Agents." Letters in Drug Design & Discovery 16, no. 3 (2019): 284–90. http://dx.doi.org/10.2174/1570180815666180627155443.

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Background:Several strategies have been reported for the synthesis of thiazole derivatives.Methods:However, many of these methods suffer from several drawbacks. Several modifications have been made to counter these problems. Here, we have synthesized a new series of 2-(2-((1HImidazol- 4-yl)methylene)hydrazinyl)-4-(4-substitutedphenyl)thiazoles without using the catalyst at room temperature.Results:The structures of synthesized compounds have been confirmed by spectral analysis, such as Mass, IR, 1H NMR and 13C NMR. All synthesized compounds were screened for in vitro antibacterial activity aga

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Taylor, Rupert G. D., Joseph Cameron, Iain A. Wright, et al. "Thiazole-induced rigidification in substituted dithieno-tetrathiafulvalene: the effect of planarisation on charge transport properties." Beilstein Journal of Organic Chemistry 11 (July 10, 2015): 1148–54. http://dx.doi.org/10.3762/bjoc.11.129.

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Two novel tetrathiafulvalene (TTF) containing compounds 1 and 2 have been synthesised via a four-fold Stille coupling between a tetrabromo-dithienoTTF 5 and stannylated thiophene 6 or thiazole 4. The optical and electrochemical properties of compounds 1 and 2 have been measured by UV–vis spectroscopy and cyclic voltammetry and the results compared with density functional theory (DFT) calculations to confirm the observed properties. Organic field effect transistor (OFET) devices fabricated from 1 and 2 demonstrated that the substitution of thiophene units for thiazoles was found to increase the

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Satheesh, Sandhya, Akhila Radha, Krishnapriya Girija, Kallikat Rajasekharan та Priya Maheswari. "Hindered phenolic aminothiazoles - synthesis, α-glucosidase, α-amylase inhibitory and antioxidant activities". Journal of the Serbian Chemical Society 82, № 10 (2017): 1087–95. http://dx.doi.org/10.2298/jsc161005084s.

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Base-catalysed heterocyclization of either N-aryl-N'-[imino(nitroamino) methyl]thioureas or N-aryl-N'-cyanothioureas by reaction with 2-bromo- 1-(2,6-di-t-butyl-4-hydroxyphenyl)ethanone afforded 4-amino-2-(arylamino)- -5-(3,5-di-t-butyl-4-hydroxybenzoyl)thiazoles, designed as molecular hybrids of hindered phenolic and 2-aminothiazole moieties. These compounds were screened for their inhibition activity on carbohydrate hydrolyzing enzymes. Thus, [4-amino-2-(phenylamino)-5-thiazolyl](3,5-di-t-butyl-4-hydroxyphenyl)- methanone exhibited ?-glucosidase inhibition activity with an IC50 value of 117

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50

Zhylko, Vasyl, Lesya Saliyeva, Nataliia Slyvka, et al. "Synthesis, antimicrobial and antioxidant activity evaluation, DFT-calculation, and docking studies of 3-aryl-5,6-dihydroimidazo[2,1-b][1,3]thiazoles." Current Chemistry Letters 14, no. 1 (2025): 107–18. http://dx.doi.org/10.5267/j.ccl.2024.9.002.

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A number of 3-aryl-5,6-dihydroimidazo[2,1-b][1,3]thiazoles were synthesized by cyclocondensation of imidazolidine-2-thione with phenacyl bromides, and their antimicrobial and antioxidant activity was evaluated. Bioscreening confirmed the moderate antibacterial activity against the reference strains of bacteria Staphylococcus aureus, Escherichia coli and Proteus vulgaris and excellent antifungal activity against Candida albicans. It was found that 3-(4-chlorophenyl)-5,6-dihydroimidazo[2,1-b]thiazole 4h (MIC = 15.625 μg/ml) has twice the antifungal effect compared to the control drug Furacilin.

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