Synthesis and Biological Activity of Heterocycles from Chalcone

Abstract

The reaction between aromatic or heteroaromatic ortho-diamines and chalcone 1_a,b is a convenient and versatile method for the preparation of condensed 1,4-diazepines 2_a,b and 4_a,b. 2,4-Diaryl- 2,3-dihydro[1,5]benzothiazepines 5_a,b were obtained from the condensation of chalcone 1_a,b with 2-aminothiophenol in presence of catalytic amount of acid. The reaction of 2,3-diaminopyridine with chalcone dibromides 6_a,b afforded the corresponding enaminoketones 7_a,b, which cyclized to 6,8-diaryl-7,8-dihydro-9H-pyrido[4,5-b][1,4]diazepine 9_a,b under acid condition. All synthesized compounds were characterized using IR, ¹H NMR, ¹³C NMR, MS and elemental analysis. The compounds were screened for their antibacterial and antifungal activities. The synthesized compounds have shown activity against all the bacterial and fungal strains.