Mutagenic and antibacterial tests of newly synthesized sulfa drugs

Abstract

Seven derivatives of sulfa drugs including N (4)-acetyl sulfanilamide, N-methyl sulfanilamide, M-diethyl sulfanilamide, N (4) sulfanilamide, N(4)-acetyl-N-methyl sulfanilamide, N(4)-acetyl-N-diethyl sulfanilamide, 2-N(4)-acetyl sulfanilyl-amidopyridine and 2-(p-nitrobenzenesulfonamido) pyridine which have an antifertility effect in experimentl animals were studied for mutagenic activity to Salmmonella typhimurium TA 98 and TA 100, a histidine revertant by Ames test and to S. typhimurium TM 677 8-azaguanine (8-AG) resistance by forward mutation assay both in the absence and presence of polychlorinated biphenyl (PCB)-induced rat-liver postmitochondrial supernatant (PMS). The results showed that all of the seven compounds were not mutagenic to S. typhimurium TA 98 and TA 100 by using Ames test in both systems. However, N-methyl sulfanila-mide, N(4)-acetyl-N-methyl-sulfanilamide and N(4)-acetyl-N-diethyl sulfanilamide showed mutagenic activity to S. typhimurium TM 677 8-AG resistance by usi forward mutation assay in both absence and presence of PCB-induced rat liver postmitochondrial supernatant, while N(4)-acetyl sulfanilamide, N-diethyl sulfanilamide and 2-(p-nitrobenzene sulfonamido) pyridine exerted their mutagenic activity only in the presence of S9, but 2-N(4)-acetyl sulfanilylamidopyridine, had no mutagenic effect in both system. These seven synthesized compounds together with another three synthesized compounds [2-(o-nitrobenzene sulfonamide) pyridine, 2-(p-toluene sulfonamido) pyridine, and N-2-pyridylsulfonamide] were also studied for antibacterial activity against six bacterial strains including Candida albican ATCC 10231, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Streptococcus faecalis and Salmonella typhi by using a standard disk diffusion method. The results showed that all of the ten compounds did not possess any antibacterial activity to all of the six bacterial strains in the testing conditions.