Design, Synthesis, Characterization and Biological Evaluation of Para-Amino Salicylic Acid (PAS) Analogues: An Approach to Repurpose

The ever-emerging microbial resistance has imposed great challenges for the medicinal chemist in designing newer chemical entities, which is a lengthy and time-consuming process. An alternate approach of repurposing older drugs can be undertaken to accelerate discovery some derivatives with lesser side effects. work reported present paper an extension idea drugs. study aimed synthesize series ester amide (P1-P28) Para-amino salicylic acid. antimicrobial evaluation all synthesized was performed via serial dilution method. Gram-positive bacteria: Staphylococcus aureus Bacillus subtilis Gram-negative Escherichia coli Pseudomonas aeruginosa were used antibacterial activity, Candida albicans antifungal activity. Ciprofloxacin (antibacterial) Fluconazole (antifungal) standard antioxidant (ester derivatives, P1-P19) carried out by using DPPH scavenging method BHA (butylated hydroxy anisole) as reference. derivative 5-acetamido-2-(propyl carbamoyl) phenyl acetate (P22) most effective agent, may attributed presence 3-carbon aliphatic alkyl chain. At same time, 4-methoxy phenyl-4-amino-2-hydroxy benzoate (P15) 2-chloro (P16) displayed Ethyl-4-amino-2-hydroxy (P2) demonstrated potent free radical Further, spectroscopic characterization physicochemical have been found accord assigned structures.