Exploration of biological potency of carboxylic acid derivatives: Designing, synthesis, characterizations and molecular docking study

摘要

The carboxylic acid functional group plays a fundamental role in the biochemistry of living systems as well as in drug design by enhancing the hydrophilicity of drugs as well as their polarity which in turn affect their bioavailability. Two new carboxylic acid derivatives with molecular formula C15H12N2O6, (1) and C11H12N2O6 (2) were successfully confirmed by different instrumental techniques. Confirmation by FT-IR and H-1 NMR techniques was proved by the presence of the OH peak (3289 cm(-1) & 3264 cm(-1) and 12.20 ppm & 12.12 ppm, respectively). Biological potency of the compounds was explored in term of bacterial, cancer and leishmania treatment. Furthermore the interaction with Salmon sperm DNA (SS-DNA) was also explored resulting in an intercalative binding mode. From the preliminary in vitro antibacterial activity, it is found that the synthesized compounds have higer effect against some tested pathogens as compared to the recommended standard antibiotics. The anticancer potency against H-157 (lung carcinoma) and BHK-21 (kidney fibroblast) cell lines of the both compounds is relatively smaller compared to that of the vincristine while a significant anti-leishmanial potency against leishmania major was observed. The intercalative binding mode was further confirmed by Molecular docking study. (C) 2020 Elsevier B.V. All rights reserved.