Abstract

Background: Nitrogen-rich heterocycles have occupied a special place in medicinal chemistry due to their exceptional biological activities. In that, thiazolo azapurines and pyrimido thiazolo azapurines are compounds of interest with their medicinal properties.

Objective: The objective is to synthesize novel substituted thiazolo azapurines and pyrimido thiazolo azapurines and evaluate their biological activities.

Methods: Herein, we have demonstrated the efficient synthesis of thiazole fused triazolo[4,5-d]pyrimidin- 7-ones starting from the easily accessible feedstock chemical cyano acetamide. The reaction proceeds under mild reaction conditions with diversified substrate scope.

Results: Notably, the obtained compounds are further derivatized under various sets of conditions to give the corresponding nitrogen-rich tetracyclic core. All synthesized compounds were tested against four pathogenic microorganisms and some of the compounds were found potent with good inhibition.

Conclusion: We have synthesized a diversely substituted nitrogen-rich thiazolo azapurines and pyrimido thiazolo azapurines and evaluated them for their anti-bacterial activity. All synthesized compounds were tested against four pathogenic microorganisms, and some of the compounds were found to be potent with good inhibition.

Keywords: Fused thiazole, azapurines, triazoles, pyrimidine, antibacterial activity, antimycobacterial activity, cyano, acetamide, isopropylazide.