Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

G Le, N Vandegraaff, DI Rhodes, ED Jones… - Bioorganic & medicinal …, 2010 - Elsevier
Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design
of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and …

Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring

SE Metobo, H Jin, M Tsiang, CU Kim - Bioorganic & medicinal chemistry …, 2006 - Elsevier
This communication details both the syntheses and biological evaluation of a novel class of
HIV-1 integrase inhibitors. When the quinoline moiety is replaced with the quinoxoline …

Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors

H Jin, RZ Cai, L Schacherer, S Jabri, M Tsiang… - Bioorganic & medicinal …, 2006 - Elsevier
A novel class of tri-cyclic HIV integrase inhibitors were designed based on conformational
analysis of 1, 6-naphthyridine carboxamide compound L-870810 and docking the designed …

The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore

BA Johns, JG Weatherhead, SH Allen… - Bioorganic & medicinal …, 2009 - Elsevier
A series of HIV-1 integrase inhibitors containing a novel metal binding motif consisting of the
8-hydroxy-1, 6-naphthyridine core and either an oxadiazole or triazole has been identified …

De novo design and synthesis of HIV-1 integrase inhibitors

MT Makhija, RT Kasliwal, VM Kulkarni… - Bioorganic & medicinal …, 2004 - Elsevier
Existing AIDS therapies are out of reach for most HIV-infected people in developing
countries and, where available, they are limited by their toxicity and their cost. New anti-HIV …

Effect of substitution on novel tricyclic HIV-1 integrase inhibitors

M Fardis, H Jin, S Jabri, RZ Cai, M Mish… - Bioorganic & medicinal …, 2006 - Elsevier
A series of novel tricyclic inhibitors of HIV-1 integrase enzyme was prepared. The effect of
substitution at C-6 of the 9-hydroxy-6, 7-dihydropyrrolo [3, 4-g] quinolin-8-one compounds …

Arylamide inhibitors of HIV-1 integrase

H Zhao, N Neamati, A Mazumder… - Journal of medicinal …, 1997 - ACS Publications
Based on data derived from a large number of HIV-1 integrase inhibitors, similar structural
features can be observed, which consist of two aryl units separated by a central linker. For …

Design and optimization of tricyclic phtalimide analogues as novel inhibitors of HIV-1 integrase

WG Verschueren, I Dierynck… - Journal of medicinal …, 2005 - ACS Publications
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 …

Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold

ED Jones, N Vandegraaff, G Le, N Choi, W Issa… - Bioorganic & medicinal …, 2010 - Elsevier
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold -
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Approaches to the synthesis of a novel, anti-HIV active integrase inhibitor

M Okello, M Nishonov, P Singh, S Mishra… - Organic & …, 2013 - pubs.rsc.org
The novel HIV-1 integrase inhibitor 1, discovered in our laboratory, exhibits potent anti-HIV
activity against a diverse set of HIV-1 isolates and also against HIV-2 and SIV. In addition …