Amino acid and peptide esters of abacavir: synthesis and activity against human immunodeficiency virus type 1 in cell culture.

Autor: Stankova, Ivanka, Stanoeva, Kamelia, Hinkov, Anton, Alexiev, Ivailo, Genova-Kalou, Petya, Chayrov, Radoslav, Argirova, Radka
Zdroj: Medicinal Chemistry Research; Dec2012, Vol. 21 Issue 12, p4053-4059, 7p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index