التفاصيل البيبلوغرافية
| العنوان: |
2,3,5‐Trisubstituted Thiazolidinone Derivatives as Potential Antimicrobial and Antitubercular Agents and In Silico Studies. |
| المؤلفون: |
Nefisath, P., Kumar, Vasantha, Shashiprabha, Patil, Shashank M., Ramu, Ramith, S, Shradha, Dasappa, Jagadeesh Prasad |
| المصدر: |
ChemistrySelect; 5/13/2024, Vol. 9 Issue 18, p1-16, 16p |
| مصطلحات موضوعية: |
ANTITUBERCULAR agents, MYCOBACTERIUM tuberculosis, ANTI-infective agents, ESCHERICHIA coli, MOLECULAR docking, ASPERGILLUS fumigatus |
| مستخلص: |
A series of novel 2,3,5‐trisubstituted thiazolidinone derivatives was designed and synthesized. Compounds were tested for their antimicrobial and antitubercular activities. Compounds 3‐(2,4‐difluorobenzyl)‐5‐[(5‐methylfuran‐2‐yl)methylidene]‐2‐(phenylimino)‐1,3‐thiazolidin‐4‐one (5 c) and 3‐(2,4‐difluorobenzyl)‐2‐((3‐fluorophenyl)imino)‐5‐((Z)‐4‐hydroxybenzylidene) thiazolidin‐4‐one (6 f) exhibited remarkable antimicrobial activity against Klebsiella pneumoniae and Escherichia coli respectively. All compounds except 3‐(2,4‐difluorobenzyl)‐5‐((3‐(4‐fluorophenyl)‐1‐phenyl‐1H‐pyrazol‐4‐yl)methylene)‐2‐(phenylimino)thiazolidin‐4‐one (5 a) and (6 f) exposed excellent antitubercular activity in comparison with the standard drugs against H37RV strain of Mycobacterium tuberculosis (ATCC No‐ 27294). In addition, molecular docking and dynamic simulations studies were performed with E. coli Mur B (EMB) (PDB ID: 2Q85), Aspergillus fumigatus sterol 14‐alpha demethylase (ASD) (PDB ID: 4UYM) and Mycobacterium tuberculosis pantothenate synthetase (MPS) (PDB ID: 3IVX) proteins against all compounds and the most potent compound (5 c) displayed higher binding proficiency. These compounds may serve as lead compounds for further optimization to achieve promising therapeutic properties. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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