N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
Mikhail S. Novikov,Vladimir T. Valuev-Elliston,Denis A. Babkov,Maria P. Paramonova,Alexander V. Ivanov,Sergey A Gavryushov,Anastasia L. Khandazhinskaya,Sergey N. Kochetkov,Christophe Pannecouque,Graciela Andrei,Robert Snoeck,Jan Balzarini,Katherine L. Seley-Radtke +12 more
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TLDR
The synthesis of phenyloxyethyl and cinnamyl derivatives of substituted uracils found to exhibit potent activity against HIV-RT and HIV replication in cell culture confirmed that the 3-benzyluracil fragment in the NNRTI structure can be regarded as a functional analogue of the benzophenone pharmacophore typically found in NN RTIs.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2013-03-01 and is currently open access. It has received 29 citations till now.read more
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Patent
Acc inhibitors and uses thereof
TL;DR: In this paper, the authors provide compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same, as well as methods of obtaining the same.
Journal ArticleDOI
Synthesis, anti-varicella-zoster virus and anti-cytomegalovirus activity of quinazoline-2,4-diones containing isoxazolidine and phosphonate substructures
TL;DR: The synthesized isoxazolidine phosphonates cis-15/trans-15 having benzyl substituents both at N3 of the quinazoline-2,4-dione skeleton and at N2 of the isoxzolidine ring displayed some anti-cytomegalovirus potency but at the same time showed significant cytostatic activity for human embryonic lung fibroblasts as well as for other cell lines.
Journal ArticleDOI
Novel Thiazolidin-4-ones as Potential Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase.
Anthi Petrou,Phaedra Eleftheriou,Athina Geronikaki,Melpomeni G. Akrivou,Ioannis S. Vizirianakis +4 more
TL;DR: The evaluation of HIV-1 RT inhibitory activity revealed that seven compounds have significantly lower ΙC50 values than nevirapine (0.3 μΜ), and it was observed that the activity of compounds depends not only on the nature of substituent and it position in benzothiazole ring but also in the nature and position of substitUents in benzene ring.
Comparative global epidemiology of HIV infections and status of current progress in treatment
TL;DR: The status of current research progress for development of drugs for HIV treatment and near future projections have been included for new treatment possibilities along with discussion about existing drugs.
Dissertation
Design and modelling in early drug development in targeting HIV-1 reverse transcriptase and Malaria
TL;DR: In this article, the authors proposed a method to solve the problem of the "missing link" problem in the context of artificial neural networks (ANNs) and artificial intelligence networks.
References
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Journal ArticleDOI
Inhibition of HIV-1 Replication by a Nonnucleoside Reverse Transcriptase Inhibitor
Vincent J. Merluzzi,K. D. Hargrave,M. Labadia,Grozinger Karl G,Mark T. Skoog,Joe C. Wu,Cheng-Kon Shih,K. Eckner,S. Hattox,Julian Adams +9 more
TL;DR: Dipyridodiazepinones inhibition of HIV-1 replication in vitro as demonstrated by in situ hybridization, inhibition of protein p24 production, and the lack of syncytia formation in cultured human T cell lines and freshly isolated human peripheral blood lymphocytes.
Journal ArticleDOI
L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase.
Steven D. Young,Susan F. Britcher,Tran Lekhanh O,Payne Linda S,William C. Lumma,Terry A. Lyle,Joel R. Huff,P. S. Anderson,David B. Olsen,S S Carroll +9 more
TL;DR: A new class of NNRTIs, the 1, 4-dihydro-2H-3, 1-benzoxazin-2-ones, was developed and L-743, 726 (DMP-266), a member of this class, was chosen for clinical evaluation because of its in vitro properties.
Journal ArticleDOI
TMC125, a Novel Next-Generation Nonnucleoside Reverse Transcriptase Inhibitor Active against Nonnucleoside Reverse Transcriptase Inhibitor-Resistant Human Immunodeficiency Virus Type 1
Koen Andries,Hilde Azijn,Theo Thielemans,Donald Ludovici,Michael Joseph Kukla,Jan Heeres,Paul Adriaan Jan Janssen,Corte Bart De,Johan Vingerhoets,Rudi Pauwels,Marie-Pierre de Béthune +10 more
TL;DR: The emerging clinical candidate, TMC125, was highly active against wild-type HIV-1 and showed some activity against HIV-2 and retained activity against 97% of 1,081 recent clinically derived recombinant viruses resistant to at least one of the currently marketed NNRTIs.
Journal ArticleDOI
Rapid purification of homodimer and heterodimer HIV-1 reverse transcriptase by metal chelate affinity chromatography.
TL;DR: In this paper, the authors modified an Escherichia coli vector expressing 66-kDa HIV-1 reverse transcriptase (p66) so that it simultaneously expressed this and the pol-coded protease.
Journal ArticleDOI
The HIV-1 reverse transcription (RT) process as target for RT inhibitors.
TL;DR: The structure‐function relationship of the HIV‐1 reverse transcriptase is highlighted, which is of great importance for a better understanding of resistance development, a major problem in anti‐AIDS therapies.