Synthesis and biological evaluation of 4-thiazolidinone derivatives as antitubercular and antimicrobial agents

Samadhiya, Pushkal; Sharma, Ritu; Srivastava, S. K.

doi:10.1016/j.arabjc.2010.11.015

Cited by 38 publications

(16 citation statements)

References 11 publications

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“…The structure–activity relationship investigation revealed that compounds with nitro group in the benzene ring of R 1 and R 2 substituents exhibited much stronger activity than compounds with chloro or bromo group in the same position. At the same time, compounds with chloro or bromo group were more active than compounds with electron‐donating groups such as methoxyl and methyl groups (Samadhiya, Sharma, Srivastava, & Srivastava, ).…”

Section: Five‐membered Ring Compoundsmentioning

confidence: 99%

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Wang

et al. 2020

Drug Development Research

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Tuberculosis (TB), a chronic infectious disease, is one of the greatest risks to human beings and 10 million people were diagnosed with TB and 1.6 million died from this disease in 2017. In addition, with the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB), the TB situation has become even worse, which has aggravated the mortality and spread of this disease.To overcome this problem, research into novel antituberculosis agents with enhanced activities against MDR-TB, reduced toxicity, and shortened duration of therapy is of great importance. Fortunately, many novel potential anti-TB drug candidates with five-membered rings, which are most likely to be effective against sensitive and resistant strains, have recently entered clinical trials. Different five-membered rings such as furans, pyranoses, thiazoles, pyrazolines, imidazoles, oxazolidinone, thiazolidins, isoxazoles, triazoles, oxadiazoles, thiadiazoles, and tetrazoles have been designed, prepared, and evaluated for their antimycobacterial activity against Mycobacterium tuberculosis. In this article, we highlight the recent advances made in the discovery of novel five-membered ring compounds and focus on their antitubercular activities, toxicity, structure-activity relationships, and mechanisms of action. K E Y W O R D Santi-TB drug, antitubercular activities, five-membered ring, MDR-TB, tuberculosis

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Section: Five‐membered Ring Compoundsmentioning

confidence: 99%

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Wang

et al. 2020

Drug Development Research

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“…Samadhiya et al [34] made an attempt to design by conventional as well as microwave strategies from 2-amino-5-nitrothiazole as a starting material to synthesize N-[2-2(substituted phenyl)-4-oxo-5-(substituted benzylidene)-1,3-thiazolidineiminoethyl]-2-amino-5-nitrothiazole.…”

Section: Scheme 1: Synthesis Of Thiazolementioning

confidence: 99%

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

P¹,

M²,

Santhanalakshmi³

et al. 2019

Asian J Pharm Clin Res

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In the new millennium, we have novel biological targets which are defined at the molecular level, which have incredible success in comprehending human illness. On the other hand, the drug design processes are largely including pharmaceutical research study, scientific intuition, reaction and expertise to drive. Final thoughts attracted from this analysis can perform crucial function shaping the way our team believe concerning existing as well as future projects. With its origins rooted in natural synthesis as well as medicinal chemistry, heterocyclic compounds are existed themselves as a fundamental department of organic chemistry. IUPAC defined “cyclic compounds possessing ring members with atoms of at least two distinct elements" 1. Heterocyclic ring structures are core substances made up of components aside from carbon, where one of the most usual substituents is oxygen, nitrogen as well as sulphur 2, 3. According to the heteroatom(s) existing in the ring structure, heterocyclic could be recorded as oxygen, nitrogen or sulfur based and within each and every class of compound is based on the size of the ring structure, determined by the total number of atoms 4. The type and size of the ring structures, as one with the substituent groups of the core scaffold, impact is strongly on the physico-chemical properties 5. Heating responses with conventional devices, such as oil bath and also home heating mantles, are not only slow, yet additionally it produces a hot surface area on the reaction vessel where reagents, items and substrates are frequently disintegrate after at some time. Microwave power alternatively, is brought right into the chemical reactor from another location and travels through the walls of the response vessel, warming the catalysts and solvents directly. Microwave dielectric heating drives chain reactions by manipulating the benefit of the potential of some solids and liquids to change electromagnetic radiation into warm. Recently, a new technique has actually concerned the leading edge of chemical investigation, that is, microwave dielectric heating. In a similar method to the introduction of the isomantle, this technical advancement will no question need an adjustment in the drug store's mind set. In the future, the drug store will make use of fast blasts of microwave power to heat and also increase chemical reactions, as opposed to an alternate application in the very first circumstances for the mantle or hot plate. High-speed synthesis with microwaves has actually attracted a significant quantity of rate of interest in most recent years 6. Considering that, the very first reports on the usage of microwave home heating by Gedye and also Giguere / Majetich groups in speeding up organic chemical conversion in 1986, far more than 2,000 write-ups have been released in the area of Microwave Assisted Organic Synthesis 7, 8.

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“…For years many medicinal chemists are in search of biologically active alkaloids containing substituted amine ring systems for their whole or partial synthesis. As by considering the medicinal and biological importance of thiazolidinone moiety, we initiated a program to synthesize thiazolidi- none derivatives as an antitubercular agent by preparing hybrid molecules having the similar features of reported potent antitubercular agents [19] (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Synthesis of (Z)-5-(substituted benzylidene)-2-((substituted phenyl) amino)thiazol-4(5H)-one analogues with antitubercular activity

Shelke

Pansare

Sarkate

et al. 2019

Journal of Taibah University for Science

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We initiated a program to synthesize thiazolidinone derivatives as antitubercular agent by preparing hybrid molecules having the similar features of reported potent antitubercular agents. We desire to state the advancement and execution of a methodology allowing for the synthesis of some new (Z)-5-(substituted benzylidene)-2-((substituted phenyl) amino)thiazol-4(5H)-one analogues with antitubercular activity. A highly efficient protocol was developed for the synthesis with excellent yields as well as evaluated in vitro for their antimycobacterial activity against Mycobacterium tuberculosis MTB H37Ra and M. bovis BCG strains. Among these synthesized compounds 6a, 6c, 6e, 6f and 6i showed marginal antitubercular activity in the series along with no significant cytotoxicity against the MCF-7 and A549 human cancer cell lines. ARTICLE HISTORY

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Synthesis and biological evaluation of 4-thiazolidinone derivatives as antitubercular and antimicrobial agents

Cited by 38 publications

References 11 publications

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Opportunities and challenges of using five‐membered ring compounds as promising antitubercular agents

Green Synthesis, Biological Evaluation and DFT Calculations of Thiazolidinone Derivatives – A Review

Synthesis of (Z)-5-(substituted benzylidene)-2-((substituted phenyl) amino)thiazol-4(5H)-one analogues with antitubercular activity

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