Synthesis of new 1,3,4-oxadiazole and benzothiazolylthioether derivatives of 4-arylmethylidene-3-substituted-isoxazol-5(4H)-one as potential antimycobacterial agents

AbstractA new series of 4-[(substituted benzylidene)-3-[(5-(pyridine-4-yl)-1,3,4-oxadiazole-2-ylthio)-methyl]isoxazol-5(4H)-one (6a –g) and 4-(substituted benzylidene)-3-((benzo[d]thiazol-2-ylthio)methyl)isoxazol-5(4H)-one(8a –g) was synthesized. All the synthesized compounds were screened for antitubercular activity againstMycobacterium tuberculosis H37Ra (ATCC 25177) andMycobacterium bovis BCG (ATCC 35743) and antibacterial activity againstEscherichia coli (NCIM 2576),Pseudomonas flurescence (NCIM 2059),Staphylococcus aureus (NCIM 2602),Bacillus subtilis (NCIM 2162). Amongst the synthesized 1,3,4-oxadiazole and benzothiazoyl thioether derivatives, compounds6b and8b showed excellent antimycobacterial activity and compounds6b,8a,8b, and8d showed excellent antibacterial activity against all tested antibacterial strains. The synthesized compounds were further evaluated for their cytotoxic activity against the HCT 116 and HeLa cancer cell lines. The 1,3,4-oxadiazole and benzothiazoyl thioether derivatives6a –g and8a –g did not show cytotoxicity.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research