1579938-33-2Relevant academic research and scientific papers
Synthesis and antibacterial and cytotoxic activities of new N-3 substituted thiazolidine-2,4-dione derivatives bearing the pyrazole moiety
Desai, Nisheeth C.,Satodiya, Hitesh M.,Kotadiya, Ghanshyam M.,Vaghani, Hasit V.
, p. 523 - 532 (2014/07/21)
Two new series of N-3 substituted thiazolidine-2,4-dione derivatives bearing the pyrazole moiety (5a-j and 7a-j) were synthesized and assessed in vitro for their efficacy as antibacterial agents against gram-positive and gram-negative bacterial strains. Among the tested compounds, 7b, 7c, 7i, and 7j were found to be active against gram-positive bacteria (Staphylococcus aureus and Streptococcus pyogenes) with minimum inhibitory concentration (MIC) values in the range of 6.25-25 μg/mL, and some compounds were also tested against methicillin-resistant S. aureus (MRSA). Compounds 7c and 7j inhibited the growth of MRSA at MIC values of 6.25 and 12.5 μg/mL, respectively. The influence of the lipophilicity (C log P) on the biological profile (MIC) of the prepared products was also discussed. From the standpoint of structure-activity relationship studies, it was observed that the lipophilic profiles of the compounds were crucial for their antibacterial activities. Further, the results of the MTT cytotoxicity studies on a human cervical cancer cell line (HeLa) and a mouse embryonic fibroblast cell line (NIH 3T3) suggested that compounds 7b, 7c, 7i, and 7j were endowed with low levels of cytotoxicity. Two new series of N-3 substituted thiazolidine-2,4-dione derivatives bearing the pyrazole moiety were assessed in vitro for their efficacy as antibacterial agents. Compounds 7b, 7c, 7i, and 7j were found to be active against Staphylococcus aureus and Streptococcus pyogenes. Compounds 7c and 7j also inhibited the growth of methicillin-resistant S. aureus. The lipophilicity profiles of the compounds were found to be crucial for their antibacterial activities.
