About: 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents

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About: 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents
Creator	Balzarini, Jan Seley-Radtke, Katherine Pannecouque, Christophe Temburnikar, Kartik Gurskaya, Galina Ivanov, Alexander Ivanova, Olga Kochetkov, Sergey Novikov, Mikhail Ozerov, Alexander Valuev-Elliston, Vladimir
Source	Elsevier; Medline; PMC
abstract	Abstract Non-nucleoside reverse transcriptase inhibitors (NNRTI) are key components in highly active antiretroviral therapy for treating HIV-1. Herein we present the synthesis for a series of N1-alkylated uracil derivatives bearing ω-(2-benzyl- and 2-benzoylphenoxy)alkyl substituents as novel NNRTIs. These compounds displayed anti-HIV activity similar to that of nevirapine and several of them exhibited activity against the K103N/Y181C RT mutant HIV-1 strain. Further evaluation revealed that the inhibitors were active against most nevirapine-resistant mono- and di-substituted RTs with the exception of the V106A RT. Thus, the candidate compounds can be regarded as potential lead compounds against the wild-type virus and drug-resistant forms.
has issue date	2011-10-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2011.08.025
bibo:pmid	21903401
has license	els-covid
sha1sum (hex)	eb2e1f738d39b3edeeea7a341f49f3f929af9fc2
schema:url	https://doi.org/10.1016/j.bmc.2011.08.025
resource representing a document's title	1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents
has PubMed Central identifier	PMC7127633
has PubMed identifier	21903401
schema:publication	Bioorganic & Medicinal Chemistry
resource representing a document's body	covid:eb2e1f738d39b3edeeea7a341f49f3f929af9fc2#body_text
is schema:about of	named entity '282' named entity 'NNRTI' named entity 'COMPONENTS' named entity 'HIV-1' named entity 'POTENTIAL' named entity 'EVALUATION' named entity 'RESISTANT' named entity 'NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS' named entity 'THESE' named entity 'TYPE VIRUS' named entity 'NOVEL' named entity 'PRESENT' named entity 'CANDIDATE' named entity 'DISPLAYED' named entity 'MONO' named entity 'LEAD COMPOUNDS' named entity 'ACTIVE' named entity 'ACTIVITY' named entity 'ANTI-HIV-1 AGENTS' named entity 'RTS' named entity '282' named entity 'SERIES' named entity 'MUTANT' named entity 'BENZOYL' named entity 'REVEALED' named entity 'SIMILAR' named entity 'ANTI-HIV ACTIVITY' named entity 'HIGHLY ACTIVE ANTIRETROVIRAL THERAPY' named entity 'NEVIRAPINE' named entity 'SYNTHESIS' named entity 'INHIBITORS' named entity 'EXCEPTION' named entity 'URACIL' named entity 'KEY' named entity 'TREATING' named entity 'FORMS' named entity 'BEARING' named entity 'WILD-TYPE' named entity 'DRUG' named entity 'STRAIN' covid:arg/eb2e1f738d39b3edeeea7a341f49f3f929af9fc2 named entity 'reverse transcriptase' named entity 'virus' named entity 'inhibitors' named entity 'revealed' named entity 'compounds' named entity 'active' named entity 'HIV-1' named entity 'nevirapine' named entity 'highly active antiretroviral therapy' named entity 'ethyl' named entity 'wild-type virus' named entity 'atom' named entity 'potency' named entity 'Tris-HCl' named entity 'RNA polymerase' named entity 'medicinal chemists' named entity 'dNTP' named entity 'nucleoside' named entity 'uracil' named entity 'virus' named entity 'halogens' named entity 'HIV' named entity 'binding pocket' named entity 'recombinant enzyme' named entity 'enzyme' named entity 'protease inhibitors' named entity 'wild-type' named entity 'K I' named entity 'K I' named entity 'HIV integrase'

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