Synthesis, characterization and in-vitro anti-inflammatory activity of some substituted 1,2,3,4 tetrahydropyrimidine derivatives

Abstract

Background & aim

Pyrimidines represent a broad class of compounds, which have received considerable attention due to their wide range of biological activities such as, anti-inflammatory, COX inhibitor, anticancer, antiallergic and analgesic. On the basis of exhaustive literature review and PASS predictions, it has been found that substituted 1,2,3,4 tetrahydropyrimidine derivatives have good potential to exhibit in vitro anti-inflammatory activity.

Method

The toxicity and pharmacological activities of synthesized compounds were studied with the help of softwares. The non-toxic compounds, which are having Pa (Probable activity), value more than 0.3 & less than 0.5 were synthesized. A novel procedure for synthesis of substituted 1,2,3,4-tetrahydropyrimidine was reported by the reaction of urea (0.01 mmol) and bis(methylthio)methylenemalononitrile (0.01 mmol). Substituted 1, 2, 3, 4-tetrahydropyrimidine possess a replaceable active methylthio group at the 6th position, which was substituted with selected nucleophiles to get final compounds.

Result

All synthesized compounds were characterized by IR, ¹H-NMR, MS and elemental analysis. All compounds were screened for in-vitro anti-inflammatory activity by inhibition of protein denaturation method using diclofenac as a standard drug. The results revealed that almost all the tested compounds showed potent in-vitro anti-inflammatory activity.

Conclusion

The obtained results for anti-inflammatory prove the necessity for further investigation to clarify the features underlying the anti-inflammatory potential of tested compounds. Substituted 1, 2, 3, 4-tetrahydropyrimidine derivatives have potential to design lead for anti-inflammatory activity.