Synthesis and Biological Evaluation of Novel Tetracyclic Benzothiazepines

Abstract

6-Arylidene-2,3-dimethyl-6,7,8,9-tetrahydro-benzocyclohepten-5-one 2a–l were obtained by the condensation of 2,3-dimethyl/3-methyl benzocyclohepten-5-one 1 with appropriate aromatic aldehydes, and upon condensation with 2-aminothiophenol in ethyl alcohol yielded 1,5-benzothiazepine derivatives 3a–l, respectively. Compounds 3d and 3h were found to possess antimicrobial activity when tested against B. Subtilis. Compounds 3i and 3j were found to possess moderate anti-inflammatory activity. Compound 3b was found to possess comparable antifungal activity when compared to clotrimazole against Trichomonas species.

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Keywords:

• Antibacterial, anti-inflammatory, and antifungal activities
• aromatic aldehydes
• benzocyclohepten-5-one
• 1,5-benzothiazepines