Abstract
Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results.
 Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi.
 Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed.
 Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.
Highlights
Bacteria Mycobacterium tuberculosis is the causative organism for tuberculosis (TB)
By substituting different thiazolidinone moiety at C-3 andmethyl moiety at C-1 of 5-nitroisatin, a series of novel Schiff and Mannich bases of 5-nitroisatin analogs 5–19 were synthesized in this work
A sequence of novel 1-((dimethylamino) methyl)-3-(4-(3-(substitutedphenyl)-4-oxothiazolidin-2-yl) phenylimino)-5-nitroindolin-2-one derivatives 5–19 were prepared from isatin using a multistep synthesis
Summary
Bacteria Mycobacterium tuberculosis is the causative organism for tuberculosis (TB). Within diseases caused by single infectious agent TB is the second largest killer. According to the WHO, every year about 9 million people are affected by TB. 3 million people are missed by current health systems. TB is an airborne disease and is two types, i.e., latent TB and active TB [1]. Chronic cough with sputum containing blood, weight loss, fever, and night sweats is the characteristic symptoms of active TB. It is believed that about one-third of the world’s population has latent TB. Latent TB becoming active only in 10% cases, but the risk is much higher in people who have compromised immune systems, i.e., people living with HIV or malnutrition, or people who smoke [2]
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: Asian Journal of Pharmaceutical and Clinical Research
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
