Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency
virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced …

ABSTRACT Introduction: The Multidimensional quantitative structure− activity relationship
(multidimensional-QSAR) method is one of the most popular computational methods …

HIV-1 integrase is one of the three most important enzymes required for viral replication and
is therefore an attractive target for anti retroviral therapy. We herein report the design and …

AIDS caused by the infection of HIV is a prevalent problem today. Rapid development of
drug resistance to existing drug classes has called for the discovery of new targets. Within …

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 application of bioisosteres in drug discovery is a well-established design concept that
has demonstrated utility as an approach to solving a range of problems that affect candidate …

HIV integrase became an important target for drug development more than twenty years
ago. However, progress has been hampered by the lack of assays suitable for high …

HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the
emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery …

Inhibition of HIV replication initially targeted viral enzymes, which are exclusively expressed
by the virus and not present in the human cell. The development of reverse transcriptase …

ABSTRACT Reaction of 2, 2, 6, 6-tetramethylpiperidin-4-one (1) with different aromatic
aldehydes afforded the diarylidenes 2a-f. Compound 1 reacted in one-pot reaction with …