Journal ArticleDOI
Thiazoles: having diverse biological activities
Shiv Jee Kashyap,Vipin Kumar Garg,Pankaj Sharma,Nitin Kumar,Rupesh Dudhe,Jitendra Kumar Gupta +5 more
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TLDR
This review presents the up to date development on the design and development of different thiazole derivatives.Abstract:
In the last few decades, a lot of work has been done on thiazole ring to find new compounds related to this scaffold to act as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective, and antitumor or cytotoxic drug molecules with lesser side effects. This review presents the up to date development on the design and development of different thiazole derivatives.read more
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Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals
TL;DR: This review reports on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals, and reports detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.
Journal ArticleDOI
Polycationic Synergistic Antibacterial Agents with Multiple Functional Components for Efficient Anti-Infective Therapy
TL;DR: The present work provides an efficient strategy for the rational design of high‐performance antibacterial materials to fight biomedical device‐associated infections.
Journal ArticleDOI
Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles.
TL;DR: The structure activity relationship revealed that the presence of electron withdrawing groups at para position of phenyl ring remarkably enhanced the antibacterial activity of synthesized compounds.
Journal ArticleDOI
Single Continuous Near-Infrared Laser-Triggered Photodynamic and Photothermal Ablation of Antibiotic-Resistant Bacteria Using Effective Targeted Copper Sulfide Nanoclusters
TL;DR: This work took advantage of the excellent photothermal and photodynamic properties of copper sulfide nanoparticles upon NIR laser irradiation and thiazole derivative as a membrane-targeting cationic ligand toward bacteria to highlight the promise of the highly versatile multifunctional nanoantibiotics in bacterial infection.
Journal ArticleDOI
Synthesis of some new 2-(3-pyridyl)-4,5-disubstituted thiazoles as potent antimicrobial agents
TL;DR: 5-acetyl-4-methyl-2-(3-pyridyl)thiazole (5) exhibited twofold antibacterial activity of ampicillin in inhibiting the growth of Staphylococcus epidermidis and also showed equipotent antifungal activity with amphotricin B against Geotricum candidum.
References
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Journal ArticleDOI
Synthesis, antibacterial, antifungal and anti-HIV activities of Schiff and Mannich bases derived from isatin derivatives and N-[4-(4′-chlorophenyl)thiazol-2-yl] thiosemicarbazide
TL;DR: Isatin, its 5-chloro and 5-bromo derivatives have been reacted with N-[4-(4'-chlorophenyl)thiazol-2-yl] thiosemicarbazide to form Schiff bases and the N-Mannich bases of these compounds were synthesized by reacting them with formaldehyde and three secondary amines.
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Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
F W Bell,Cantrell As,Marita Högberg,Jaskunas,Johansson Nils Gunnar,C. L. Jordan,Kinnick,Peter Thomas Lind,J. M. Jun. Morin,Rolf Noreen +9 more
TL;DR: A novel series of potent specific HIV-1 inhibitory compounds is described and the identification of N-(2-pyridyl)-N'-(5-bromo-2- pyridol)-thiourea (62; LY300046.HCl) as a candidate for clinical evaluation is identified.
Journal ArticleDOI
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
William C. Patt,Harriet W. Hamilton,Taylor,Michael J. Ryan,D G Taylor,Cleo J. C. Connolly,Annette M. Doherty,Klutchko,Sircar I,Bruce A. Steinbaugh +9 more
TL;DR: A series of renin inhibitors was synthesized that contained a 2-amino-4-thiazolyl moiety at the P2 position that exhibited oral blood pressure lowering activity in high-renin normotensive monkeys and was selected for further evaluation in renal hypertensive monkeys on the basis of its superior efficacy and duration of action.
Journal ArticleDOI
Synthesis and antimicrobial activity of novel 2-thiazolylimino-5-arylidene-4-thiazolidinones.
TL;DR: The 5-arylidene derivatives showed an antibacterial efficacy considerably greater than that of the parent 2-(thiazol-2-ylimino)thiazolidin-4-one 3, suggesting that the substituted and unsubstituted 5- Darylidene moiety plays an important role in enhancing the antimicrobial properties of this class of compounds.
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N-(4-substituted-thiazolyl)oxamic acid derivatives, a new series of potent, orally active antiallergy agents.
TL;DR: A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model and one of the ethanolamine salts, N-[4-(1,4-benzodioxan-6-yl)-2-thiaxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.