One-Pot Synthesis of Thiazoles via Hantzsch Thiazole Reaction and Their Antimicrobial Activity

Yogi, Prabhunath; Ashid, Mohammad; Hussain, Nasir; Khan, Saba; Joshi, Ajit

doi:10.14233/ajchem.2016.19603

Cited by 9 publications

(6 citation statements)

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“…Microwave‐assisted synthesis was also used but reduction in time was not great. These hybrids have exhibited a good anti‐bacterial activity when compared to Ciprofloxacin and better antifungal activity against C. albicans and A. fumigatus than Fluconazole [331] …”

Section: Reactivity Of 24‐thiazolidinedionementioning

confidence: 99%

Chemistry and Applications of Functionalized 2,4‐Thiazolidinediones

et al. 2023

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Thiazolidinedione (TZD) is one of the privileged heterocyclic rings and has shown many biological applications in medicinal chemistry and drug discovery. This review covers the synthetic approaches of TZD and its derivatives, different synthetic techniques for affording the desired regioselectivity and stereoselectivity, and the techniques that would enhance reaction conditions such as microwave, one‐pot, or ultrasound synthesis. It focuses on synthetic challenges of glitazones and the transformation of other heterocycles to TZD. Moreover, the chemical and biological behavior of TZD through the substitution in the N3 position, modification of the C5 position, annealing in complex heterocyclic systems, and hybridization with other pharmacologically attractive moieties are discussed. All reactions mentioned are provided as possible with different reaction conditions, mechanisms, derivatives scope, yield and clarified by applications of such reactions in the construction of potential medicinal agents. The review also answers questions about rapid racemization of glitazones, their toxicity, considering TZD as pan‐assay interference compounds (PAINS) or not, and the influence of saturation of 5‐position of TZD in their biological activities. This review is a comprehensive guide to make informed decisions for construction of TZD derivatives with biological potentials.

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Section: Reactivity Of 24‐thiazolidinedionementioning

confidence: 99%

Chemistry and Applications of Functionalized 2,4‐Thiazolidinediones

et al. 2023

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“…Antibacterial activity of the compounds was determined by the well diffusion method [24]. The microbial cultures were grown at 37 °C for 18 h and then diluted by sterile saline (0.9% w/v) solution to obtain a cell suspension of 105 CFU/ml.…”

Section: Antibacterial Activitymentioning

confidence: 99%

Biopolymer Catalysed Synthesis of 6-methyl-4-phenylcarbamoyl-1, 2, 3, 4- Tetrahydropyrimidine-2-ones and Evaluation of their Anti-bacterial and Anti-tubercular Activities

Chabukswar

Pawar

Handore

et al. 2019

CBC

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Background: An efficient one-pot biocatalysed ultrasound assisted synthesis of dihydropyrimidinones/ thiones has been developed under solvent free conditions. Materials and Methods: The use of biodegradable, non toxic, agar-powder as a catalyst provide advantages like high yield, simple operation, mild reaction condition with short reaction time. 1,2,3,4- tetrahydropyrimidine-2-ones/thiones formed were characterized by mass and 1H NMR spectroscopy. Results: The dihydropyrimidinones substituted with electron donating groups like fluorine, hydroxy along with thienyl groups exhibited good antibacterial activity. The compounds exhibited favorable binding interactions with mycobacterium target protein H37Rv. Conclusion: 4-methoxy substituted dihydropyrimidinones derivative showed significant antituberculosis activity.

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“…48 Microwave assisted synthesis of 4-phenyl-1,3-thiazole derivatives 54 from the reaction of isatin 1, 2-bromoethanones 52 and thiosemicarbazide 53 has been accomplished (Scheme 18). 49 The synthesized compounds were tested for their antimicrobial activities. © ARKAT USA, Inc Scheme 18 2,4-Dinitrophenol (DNP) facilitated the three component reaction of isatins 1, cyclic-amines 55 and alkynes 8 to prepare the mono-functionalized α-alkynyl-3-amino-2-oxindole derivatives 56 (Scheme 19).…”

Section: Scheme 15mentioning

confidence: 99%