Microwave-assisted synthesis of bioactive tetrahydropyrimidine derivatives as antidiabetic agents

Abstract

Introduction: In drug discovery, pyrimidine analogues show good biological response and many drug moieties have pyrimidine core. Aim: On the basis of prior review, we synthesized a series of N-(substituted phenyl)-1,3,6-trimethyl-4-(4-((5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl)methoxy)phenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide parade a 1,3,4-oxadiazole core which were evaluated for in vitro antidiabetic screening. Materials and methods: The tetrahydropyrimidine derivatives have been synthesized by microwave irradiation method. It was carried out by Biginelli condensation of 1,3,4-oxadiazole based aldehyde, substituted acetoacetanilide and N,N’-dimethyl urea. All synthesized compounds were evaluated for antidiabetic screening. Results: By the results derived from antidiabetic activity, compounds 4a, 4e, 4g, and 4i show good inhibition compared to others because of electron withdrawing and hydroxyl groups. All results are compared with standard drug acarbose. Conclusions: In conclusion, a series of 1,3,4-oxadizole bearing tetrahydropyrimidine has been synthesized and evaluated for in vitro antidiabetic screening. The derivatives 4a, 4e, 4g, and 4i exhibited promising antidiabetic activity