Synthesis, antimycobacterial, cytotoxicity, anti‐inflammatory, in silico studies and molecular dynamics of pyrazole‐embedded thiazolidin‐4‐one hybrids

In the present investigation, we devolved and synthesized a new series of pyrazole‐embedded thiazolidin‐4‐one derivatives (9a–p) with the goal to produce promising antitubercular leads. The in vitro antimycobacterial activity of the synthesized compounds was tested against replicating and nonreplica...

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Published in:Archiv der Pharmazie (Weinheim) 2023-03, Vol.356 (3), p.e2200444-n/a
Main Authors: Kamat, Vinuta, Poojary, Boja, Puthran, Divyaraj, Das, Vishwa B., Kumar, Banoth K., Sankaranarayan, Murugesan, Shetye, Gauri, Ma, Rui, Franzblau, Scott G., Nayak, Suresh P.
Format: Article
Language:English
Subjects:
Alamar blue solution
Animals
antimycobacterial
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
anti‐inflammatory
Chlorocebus aethiops
Microbial Sensitivity Tests
Molecular Docking Simulation
Molecular Dynamics Simulation
Molecular Structure
Mycobacterium tuberculosis
Pyrazoles - pharmacology
Structure-Activity Relationship
thiazolidin‐4‐one
Vero Cells
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Summary:In the present investigation, we devolved and synthesized a new series of pyrazole‐embedded thiazolidin‐4‐one derivatives (9a–p) with the goal to produce promising antitubercular leads. The in vitro antimycobacterial activity of the synthesized compounds was tested against replicating and nonreplicating Mtb H37Rv strains. With MIC ranging from 3.03 to 22.55 µg/ml, five compounds (9a, 9c, 9d, 9e, and 9f) emerged as promising antitubercular agents. The active molecules were nontoxic to normal Vero cells. All the synthesized compounds were evaluated for in vitro anti‐inflammatory studies. Compounds 9a, 9b, 9c, 9h, and 9i exhibited excellent anti‐inflammatory efficacy. Docking study was performed to understand the binding pattern of the significantly active compound 9a with 1P44. A new series of pyrazole embedded thiazolidin‐4‐one derivatives (9a–p) were developed to produce promising antitubercular leads. The in vitro antimycobacterial activity of the synthesized compounds was tested against replicating and nonreplicating Mtb H37Rv strains. Five compounds (9a, 9c, 9d, 9e, and 9f) emerged as promising antitubercular agents while being nontoxic to normal Vero cells.
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.202200444