Development of Triazoles and Triazolium Salts Based on AZT and Their Anti-Viral Activity against HIV-1.

ABSTRACT: We report herein a set of 3'-azido-3'-deoxythymidine (AZT) derivatives based on triazoles and triazolium salts for HIV-1 infection. The compounds were synthesized via click chemistry with Cu(I) and Ru(II) catalysts. Triazolium salts were synthesized by reaction with methyl iodide or methyl triflate in good yields. The antiviral activity of the compounds was tested using two methodologies: In method one the activity was measured on infected cells; in method two a pre-exposure prophylaxis experimental model was employed. For method one the activity of the compounds was moderate, and in general the triazolium salts showed a decreased activity in relation to their triazole precursors. With method two the antiviral activity was higher. All compounds were able to decrease the infection, with two

SUBMITTER: de Alencar DM 

PROVIDER: S-EPMC8588071 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature