BORONIC ACID-DERIVATIVES TARGETING HIV-1

A series of novel boronic acid derivatives containing either a pyrimid ine or purine base was synthesized. The preparation involved the conde nsation of 4-bromobutyl boronic acid with the appropriate base. These acyclic nucleosides were designed as potential antiviral agents especi ally targeting the human immunodeficiency virus. Two analogues, 6-chlo ro-9-(4-dihydroxyborylbutyl)purine and 2,6-dichloro-9-(4-dihydroxybory lbutyl)purine, exhibited EC(5)0 values of 7.7 mu M, and 0.99 mu M, res pectively, in an HIV-1 syncytial plaque reduction assay.