Sudhakar R. Bhusare

Novel thiazolopyrimidine derivatives (4a-l) were efficiently synthesized via the cyclo-condensation reactions of 2-(3-dimethylamino) acryloyl) phenyl 4-methylbenzene sulfonates with 2,3-dihydro-4-phenylthiazol-2-amines under microwave irradiation in ethanol catalyzed by iodine and the synthesized compounds were evaluated for their in vitro antimicrobial and anti-inflammatory activities. Among the newly synthesized compounds, 4d, 4h and 4l have exhibited potent antibacterial activity where as other derivatives 4b and 4j have showed moderate activity in comparison to standard drug amphcillin. The derivatives, 4d and 4l have displayed potent antifungal activity when their activity data was compared with standard drug norcadine. Some of the selected compounds were also screened for their anti-inflammatory activity and the results are compared with standard drug indomethacin. Among the derivatives, 4j possessed potent anti-inflammatory activity while 4b, 4f and 4k have exhibited moderate activity.

An effective and economical protocol was developed for the synthesis of 3-substituted indoles by one-pot three-component coupling reaction of a substituted salicylaldehyde, N-methylaniline and indole using [Hmim] HSO4 as a catalyst. All the synthesized derivatives were evaluated for inhibition of cancer cell. The initial assays indicated that some of the newly synthesized compounds displayed significantly good inhibition activities against human breast cancer cell (MCF7), cell lines compared with the control (Adriamysin), which might be developed as novel lead scaffold for potential anticancer agents.

An efficient and rapid synthesis of some new pyrazoles, isoxazole, benzoxazepine and benzothiazepine derivatives is described. The synthesized compounds were investigated for their anti-inflammatory and antimicrobial activities and some of them showed potent anti-inflammatory and anti-microbial activities.