Nucleoside substituted perhydro-1λ5-[1,3,2]diazaphospholo[1,5-a]pyridine-1-thione analogues: Synthesis and evaluation of antiviral and antimicrobial activities

Mavallur Varalakshmi and Chamarthi Nagaraju

Sri Venkateswara College of Engineering and Technology, Chittoor-517127, Andhra Pradesh, India

Department of Chemistry, Sri Venkateswara University, Tirupati-517501, Andhra Pradesh, India

Abstract: A new series of nucleoside substituted perhydro-1λ 5-[1,3,2]diazaphospholo[1,5-a]pyridine-3-thione derivatives 4(a-j) was synthesized by a one-pot two-step process. It involves the formation of key intermediate, 1-chloroperhydro-1λ 5-[1,3,2]diazaphospholo [1,5-a]pyridine-1-thione (3) and its subsequent reaction with various nucleosides to obtain the title products 4(a-j). Structures of all the newly synthesized compounds were elucidated by spectral analysis. Compound (4b) linked with zidovudine exhibited highest antiviral and antimicrobial activities as compared to other nucleoside derivatives.

Keywords:2(±)-Aminomethyl piperidine; thiophosphoryl chloride; nucleosides; antiviral activity; antimicrobial activity. ©2018 ACG Publication. All right reserved.