Raltegravir: first in class HIV integrase inhibitor

Z Temesgen, DS Siraj - Therapeutics and clinical risk management, 2008 - Taylor & Francis
On October 16, 2007, the US Food and Drug Administration (FDA) approved raltegravir for
treatment of human immunodeficiency virus (HIV)-1 infection in combination with other …

HIV‐1 integrase inhibitors: 2005–2006 update

R Dayam, R Gundla, LQ Al‐Mawsawi… - Medicinal Research …, 2008 - Wiley Online Library
Abstract HIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome,
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …

[HTML][HTML] HSV-1 Glycoprotein D and Its Surface Receptors: Evaluation of Protein–Protein Interaction and Targeting by Triazole-Based Compounds through In Silico …

R Bivacqua, I Romeo, M Barreca, P Barraja… - International Journal of …, 2023 - mdpi.com
Protein–protein interactions (PPI) represent attractive targets for drug design. Thus, aiming
at a deeper insight into the HSV-1 envelope glycoprotein D (gD), protein–protein docking …

The hunt for HIV-1 integrase inhibitors

M Lataillade, MJ Kozal - AIDS Patient Care & STDs, 2006 - liebertpub.com
Currently, there are three distinct mechanistic classes of antiretrovirals: inhibitors of the HIV-
1 reverse transcriptase and protease enzymes and inhibitors of HIV entry, including receptor …

Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

LF Zeng, Y Wang, R Kazemi, S Xu, ZL Xu… - Journal of Medicinal …, 2012 - ACS Publications
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 …

One‐Pot Synthesis of 2, 3, 6‐Trisubstituted Pyridines by Phosphine‐Catalyzed Annulation of γ‐Vinyl Allenoates with Enamino Esters Followed by DDQ‐Promoted …

X Li, W Cai, Y Huang - Advanced Synthesis & Catalysis, 2022 - Wiley Online Library
A one‐pot strategy for constructing trisubstituted pyridine derivatives had been established
via phosphine‐catalyzed annulation and DDQ oxidative aromatization reactions. This …

Targeting HIV-1 integrase with strand transfer inhibitors

Y Li, S Xuan, Y Feng, A Yan - Drug Discovery Today, 2015 - Elsevier
Highlights•Overview of structural and functional properties of HIV-1 integrase
(IN).•Classifying the HIV-1 integrase strand transfer inhibitors (INSTIs) into ten …

Retroviral integrase: Structure, mechanism, and inhibition

DO Passos, M Li, R Craigie, D Lyumkis - The enzymes, 2021 - Elsevier
The retroviral protein Integrase (IN) catalyzes concerted integration of viral DNA into host
chromatin to establish a permanent infection in the target cell. We learned a great deal about …

Inhibiting HCMV pUL89-C Endonuclease with Metal-Binding Compounds: Miniperspective

AD Jagtap, RJ Geraghty, Z Wang - Journal of medicinal chemistry, 2023 - ACS Publications
Human cytomegalovirus (HCMV) infects individuals of all ages and establishes a lifelong
latency. Current antiviral drugs are suboptimal in efficacy and safety and ineffective against …

Microwave-assisted one-pot two-step imine formation–hetero-Diels–Alder–detosylation/aromatization sequence: direct access to dibenzo [b, h][1, 6] naphthyridines

G Jan, A Kumar, M Karuppasamy, D Rajput… - Organic & …, 2022 - pubs.rsc.org
A microwave-assisted, copper-catalyzed, one-pot, two-step reaction is established to access
functionalized [1, 6] naphthyridines in high yields (up to 96%) starting from 2-(N …