Among a large number of HIV-1 integrase (IN) inhibitors, the 8-hydroxy-[1, 6] naphthyridines
(ie, L-870,810) were one of the promising class of antiretroviral drugs developed by Merck …

HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential
for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of …

The medicinal chemistry and structure− activity relationships for a novel series of 7-benzyl-4-
hydroxy-1, 5-naphthyridin-2 (1 H)-one HIV-integrase inhibitors are disclosed. Substituent …

Previously, we discovered linomide analogues as novel HIV-1 integrase (IN) inhibitors.
Here, to make possible structure–activity relationships, we report on the design and …

A series of 2-hydroxy-1, 3-dioxoisoquinoline-4-carboxamides featuring an N-hydroxyimide
chelating functionality was evaluated for their inhibitory properties against human …

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 …

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 …

The use of a 1, 3, 4-oxadiazole in combination with an 8-hydroxy-1, 6-naphthyridine ring
system has been shown to deliver potent enzyme and antiviral activity through inhibition of …

In the present article, we describe SAR studies within a series of N-hydroxy-
dihydronaphthyridinone HIV integrase inhibitors that led to a candidate compound, PF …

4, 5-Dihyroxypyrimidine carboxamides, which evolved from a related series of HCV NS5b
polymerase inhibitors, have been optimized to provide selective HIV integrase strand …