Amino acid and peptide esters of abacavir: synthesis and activity against human immunodeficiency virus type 1 in cell culture
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Abacavir (ABC) is clinically associated with hypersensitivity reactions, risk for cardiovascular disease, etc. A possible way to minimize side effects is by modifying chemical structure. Three esters of ABC containing amino acid (glycine) and dipeptide esters (glycyl-glycine) were synthesized and their activity on HIV-1 III B replication in MT-4 cells was evaluated. One of the newly synthesized esters—Gly-ABC—demonstrates low-cytotoxicity and high-anti-HIV-1 activity in MT-4 cells, as well as low-mitochondrial toxicity and high-genetic barrier to resistance.
KeywordsCell culture Aminoacid and dipeptide esters of abacavir Anti-HIV activity Mitochondrial toxicity Sequencing of HIV-mutants
The financial support of contract VUL-304/07 of Ministry of Science and Education, Republic of Bulgaria, is highly appreciated.
Conflict of interest
The authors declare lack of conflict of interest.
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