[Development of new enzyme inhibitors for the treatment of AIDS[ ]

Two different approaches can be used to discover new lead structures for further drug design. Till now, de novo drug design, however, has not led to compounds active against HIV. The more classical approach, based on screening programmes, has led to the discovery of three different enzyme inhibitors active against HIV: transition state analogues (protease inhibitors), antimetabolites (azidothymidine and analogues as reverse transcriptase inhibitors), and TIBO and its congeners (reversible reverse transcriptase inhibitors).