HIV-1 integrase catalyzes the insertion of viral DNA into the genome of the host cell.
Integrase inhibitor N-(4-fluorobenzyl)-8-hydroxy-1, 6-naphthyridine-7-carboxamide …

Introduction of a 5, 6-dihydrouracil functionality in the 5-position of N-(4-fluorobenzyl)-8-
hydroxy-[1, 6] naphthyridine-7-carboxamide 1 led to a series of highly active HIV-1 integrase …

A novel class of tetrahydro-pyrazinopyrimidine-2-carboxamides have been identified as HIV-
1 integrase inhibitors. Optimization of the initial lead culminated in the discovery of a series …

A series of 2-pyrrolidinyl-N-methyl pyrimidones HIV integrase inhibitors has been explored
leading to the identification of derivative 13, which showed high activity at inhibiting viral …

A series of novel 2-tbutyl-N-methyl pyrimidone HIV-1 integrase inhibitors have been
identified. Optimization of the initial lead resulted in compounds such as 9d and 14a, which …

The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of
Isentress™, represents a validated target for anti-retroviral therapy. Incorporation of the …

Integration of viral DNA into the host cell genome is an obligatory process for successful
replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is …

Human immunodeficiency virus type-1 integrase is an essential enzyme for effective viral
replication and hence a valid target for the design of inhibitors. We report here on the design …

A series of 5-amino derivatives of 8-hydroxy [1, 6]-naphthyridine-7-carboxamide exhibiting
sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of …

The human immunodeficiency virus type-1 (HIV-1) encodes three enzymes essential for viral
replication: a reverse transcriptase, a protease, and an integrase. The latter is responsible …