Synthesis, characterization and in-vitro anti-microbial and anti-cancer activity of novel fused benzo-chromene derivatives

Abstract

An ecofriendly synthesis of (E) –N-(1-Substituted Phenyl)-3H –benzo[f]chromen-3 ylthioimidcarboxyacetohydrazides was carried out. The versatile use of benzo-chromenes has stimulated a considerable interest to explore the possible synthesis of novel fused compounds in which the benzo-chromene ring is fused with another biologically active molecule. An attempt was made to utilize this concept, that is the fusion of benzo-chromene with pyrimidin-4-one. Pyrimidin-4-one nucleus was chosen because it was found to possess various biological activities. The (E)-N-(1-SubstitutedPhenyl-3Hbenzo[f]chromenylthioimidcarboxyacetohydrazides  were formed when the starting materials Substituted Benzaldehyde, Napthalene-2-ol and Ethyl cyano acetate were treated with Potassium Iodide, Iodine and Potassium Carbonate. The Ethyl-3-amino-1-substituted phenyl-1H-benzo[f]chromene-2-carboxylates were further treated with DMS, DMSO, CS₂, and finally with Hydrazine Hydrate to afford (E)–N-(1-Substituted Phenyl)-3H–benzo (f) chromen-3-ylthioimidcarboxyacetohydrazides. The novel Synthesized Compounds were characterized by M.P, IR, ¹HNMR and Mass Spectrum. These synthesized compounds were subjected to anti-bacterial studies using few Gram-Positive, Gram-negative and fungal organisms. The standard drug used for anti-microbial activity is Ampicillin and Ketoconazole respectively. Also is tested for their anti-cancer activity by MTT assay method. The tested Compounds exhibited significant anti-microbial and anti-cancer activity.