SOME REACTIONS WITH -(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 -(3,4-dimethylbenzoyl)-alpha-(indol-3-yl)propionic acid (2). The conde nsation of 2 with hydrazines affords the corresponding pyridazinones. Reactions of pyridazinones with N,N-p-(dimethylamino)benzaldehyde, ace tyl chloride, benzenesulfonyl chloride, monochloroacetic acid, ethyl c hloroformate gave the 4,5,6-trisubstituted pyridazinones and the N-sub stituted pyridazinone derivatives. Reactions of pyridazinones with POC l3 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 antibact erial screening revealed that some of the new compounds possess activi ty against Gram-positive, Gram-negative bacteria and fungi.