SOME REACTIONS WITH BETA-(3,4-DIMETHYLBENZOYL)-ALPHA-(INDOL-3-YL)PROPIONIC ACID AND SCREENING OF THEIR ANTIBACTERIAL ACTIVITIES

Beta-(3,4-dimethylbenzoyl)acrylic acid (I) reacts with indole to give beta-(3,4-dimethylbenzoyl)-alpha-(indol-3-yl)propionic acid (2). The condensation of 2 with hydrazines affords the corresponding pyridazinones. Reactions of pyridazinones with N,N-p-(dimethylamino)benzaldehyde, acetyl chloride, benzenesulfonyl chloride, monochloroacetic acid, ethyl chloroformate gave the 4,5,6-trisubstituted pyridazinones and the N-substituted pyridazinone derivatives. Reactions of pyridazinones with POCl3 and P2S5 gave the chloro- and the thiopyridazine derivatives, which are subjected to further studies with anthranilic acid, p-anisidine, sodium azide, hydrazine hydrate and benzylamine. The in-vitro antibacterial screening revealed that some of the new compounds possess activity against Gram-positive, Gram-negative bacteria and fungi.