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.
The ethanol extracts of flowers, young bud, mature leaves and stems of Calotropis procera (Ait). R. Br. (Asclepiadaceae) was screened for phytochemical properties, antimicrobial (agar dilution method) activity and effectiveness on third instar larvae of Anopheles stephansi. Qualitative estimation of alkaloids, carbohydrates, glycosides, saponins, proteins, fixed oils, starch, triterpenoid, phenolics and tannins showed their presence in almost all the plant part extracts. While, gum and mucilage were absent in all the plant extracts. Quantitative estimation of different parts of the plant extracts had large quantity of carbohydrate and tannin in flower while young buds had higher amount of phenolic compounds and oil. Mature leaves showed maximum activity against all the bacterial strain used in the study. The extracts of mature leaves showed highest activity of 100% mortality at 2000 ppm after 48 hours of incubation against 3rd instar larvae of A. stephansi. LD50 and LD90 values suggested that mature leaves of C. procera had higher mortality rate against larvae of A. stephansi.
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