A Brief Literature and Review of Patents on Thiazole Related Derivatives

Abstract

Background: Thiazole is widely investigated bioactive scaffold and dynamic tool in medicinal chemistry research. Significance of thiazole compounds are well documented as thiazole is an obligatory structure of number of currently available therapeutics. In spite of that, thiazole derivatives are endowed with myriad biological activities, such as antiviral, anticancer, antibacterial, antifungal, antimalarial, antiparkinsonian, anti-inflammatory activities and many more. Methods: In recent past, different approaches have been introduced for synthesis of thiazole and related compounds. Intrinsic molecular interaction between newly synthesized thiazole compounds and plethora of drug targets/enzymes has rendered discovery of new drug molecules with advances in modes of action. A renewed interest in therapeutic use of thiazole derivatives has been seen among the prospective researchers as exemplified by influx of huge scientific articles and patents. Some important patents of anti-infective and anticancer interest have been addressed appropriately and are presented in tables. Results: This review paper is a contemporary approach on therapeutic/applications of thiazole derivatives by summarizing important patents filed from 2000-2017. The main focus of these patents is on anti-infective and anticancer potential of thiazole based compounds. Conclusion: These approaches may provide valuable information for the further design of more active biological agents through various modifications and derivatizations.

Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance

“…Many heterocyclic compounds have been synthesized in the past decade in the attempt to obtain new antimicrobials, which would be able to treat infections caused by resistant bacterial strains. Herein we focused on synthetic molecules bearing the thiazole, benzothiazole, and thiazolidinone scaffolds, which are widely recognized as nuclei of great value for obtaining molecules endowed with various biological activities, 8 including analgesic, 9 anti-inflammatory, 9 antidiabetic, 10 antitumor, 11 and antimicrobial. 12 …”

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

“…19, Caco-2, MDA-MB-231, and A549 cell lines with the IC 50 values less than 3 μM which was found to be more potent than the reference compound cisplatin. Compound 236 (IC 50 : 0.3 µM) was found to exhibit excellent activity against SNB-19 cell line whereas, 237 (IC 50 : 0.3 µM) displayed prominent cytotoxicity against A549 carcinoma cells.…”

“…As the aforesaid S-containing heterocycles are in the limelight, reviews encompassing the applicability of individual templates have been published till date. [19][20][21][22][23][24][25][26][27][28][29] However, few reviews have been published covering a group of S-containing heterocycles on a single platform. Wang et al, 17 concentrated more specifically on the development of natural products possessing sulfur heteroatom.…”

“…As the aforesaid S ‐containing heterocycles are in the limelight, reviews encompassing the applicability of individual templates have been published till date 19–29 . However, few reviews have been published covering a group of S ‐containing heterocycles on a single platform.…”

α,α‐Dibromoketone precursors in the synthesis of some new thiazole derivatives: Thiazol‐2‐yl hydrazonobutanoates, thiazol‐2‐yl pyrazole‐4‐carboxylates and acids

“…However, due to handling problems associated with α‐bromoketones such as low melting, toxicity and lachrymosity, the use of α,α‐dibromoketones in modified HTS is appreciable. Synthesis of new derivatives of thiazoles is encouraged as (a) the wonder motif is endowed with remarkable biological activities particularly antimicrobial and antitumor, (b) there is continuous need for new antibiotics because the disease causing microbes become resistant to existing antibiotic arsenal . Combining thiazole with another five‐membered diheteroatomic N‐containing heterocycle, the pyrazole core in a single hybrid structure are expected to impart distinct and interesting structural and biological characteristics .…”