Matches in SemOpenAlex for { <https://semopenalex.org/work/W2313179993> ?p ?o ?g. }
Showing items 1 to 99 of
99
with 100 items per page.
- W2313179993 endingPage "221" @default.
- W2313179993 startingPage "213" @default.
- W2313179993 abstract "Eleven chiral naphthyl thiourea (CNT) compounds were synthesized as non-nucleoside inhibitors (NNI) of the reverse transcriptase (RT) enzyme of HIV-1. Molecular modelling studies indicated that, because of the asymmetric geometry of the NNI binding pocket, the ‘R” stereoisomers would fit the NNI binding pocket of the HIV-1 RT much better than the corresponding ‘S” stereoisomers, as reflected by their 10 4 -fold lower Ki values. The ‘R” stereoisomers of all 11 compounds inhibited the recombinant RT in vitro with lower IC 50 values than their enantiomers. Of seven CNT compounds whose ‘R” stereoisomers exhibited nanomolar IC 50 values against recombinant RT, five were further evaluated for their ability to inhibit HIV-1 replication in human peripheral blood mononuclear cells (PBMC). All five ‘R” stereoisomers were active anti-HIV agents and inhibited the replication of the HIV-1 strains HTLV-IIIB (NNI-sensitive), A17 (NNI- resistant, Y181C mutant RT) and A17Var (NNI- resistant, Y181C plus K103N mutant RT), as well as primary HIV-1 isolates from AIDS patients in human PBMC at nanomolar concentrations, whereas their enantiomers were inactive. The lead compounds, 1R and 5R, were 3 log more potent than the standard NNI drug nevirapine against the NNI-resistant HIV-1 strains. Our data establish the stereochemistry as a major determinant of the potency of this new class of NNI." @default.
- W2313179993 created "2016-06-24" @default.
- W2313179993 creator A5016366257 @default.
- W2313179993 creator A5048956276 @default.
- W2313179993 creator A5091381226 @default.
- W2313179993 date "2001-08-01" @default.
- W2313179993 modified "2023-09-28" @default.
- W2313179993 title "Stereochemistry as a Major Determinant of the Anti-HIV Activity of Chiral Naphthyl Thiourea Compounds" @default.
- W2313179993 cites W153672433 @default.
- W2313179993 cites W1968224345 @default.
- W2313179993 cites W1976580962 @default.
- W2313179993 cites W1989357838 @default.
- W2313179993 cites W2027148086 @default.
- W2313179993 cites W2030901281 @default.
- W2313179993 cites W2056524306 @default.
- W2313179993 cites W2061482690 @default.
- W2313179993 cites W2072409481 @default.
- W2313179993 cites W2076578204 @default.
- W2313179993 cites W2086624794 @default.
- W2313179993 cites W2101963388 @default.
- W2313179993 cites W2107500997 @default.
- W2313179993 cites W2117784959 @default.
- W2313179993 cites W2130266760 @default.
- W2313179993 cites W2146411900 @default.
- W2313179993 cites W2156229229 @default.
- W2313179993 cites W2169046292 @default.
- W2313179993 cites W2319375073 @default.
- W2313179993 cites W2322443628 @default.
- W2313179993 cites W2333133071 @default.
- W2313179993 doi "https://doi.org/10.1177/095632020101200402" @default.
- W2313179993 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11771730" @default.
- W2313179993 hasPublicationYear "2001" @default.
- W2313179993 type Work @default.
- W2313179993 sameAs 2313179993 @default.
- W2313179993 citedByCount "16" @default.
- W2313179993 countsByYear W23131799932020 @default.
- W2313179993 crossrefType "journal-article" @default.
- W2313179993 hasAuthorship W2313179993A5016366257 @default.
- W2313179993 hasAuthorship W2313179993A5048956276 @default.
- W2313179993 hasAuthorship W2313179993A5091381226 @default.
- W2313179993 hasBestOaLocation W23131799931 @default.
- W2313179993 hasConcept C104317684 @default.
- W2313179993 hasConcept C129694887 @default.
- W2313179993 hasConcept C137061746 @default.
- W2313179993 hasConcept C143065580 @default.
- W2313179993 hasConcept C153574943 @default.
- W2313179993 hasConcept C156719811 @default.
- W2313179993 hasConcept C161790260 @default.
- W2313179993 hasConcept C178790620 @default.
- W2313179993 hasConcept C181199279 @default.
- W2313179993 hasConcept C185592680 @default.
- W2313179993 hasConcept C202751555 @default.
- W2313179993 hasConcept C2780538656 @default.
- W2313179993 hasConcept C40767141 @default.
- W2313179993 hasConcept C486523 @default.
- W2313179993 hasConcept C55493867 @default.
- W2313179993 hasConcept C67705224 @default.
- W2313179993 hasConcept C71240020 @default.
- W2313179993 hasConcept C86803240 @default.
- W2313179993 hasConceptScore W2313179993C104317684 @default.
- W2313179993 hasConceptScore W2313179993C129694887 @default.
- W2313179993 hasConceptScore W2313179993C137061746 @default.
- W2313179993 hasConceptScore W2313179993C143065580 @default.
- W2313179993 hasConceptScore W2313179993C153574943 @default.
- W2313179993 hasConceptScore W2313179993C156719811 @default.
- W2313179993 hasConceptScore W2313179993C161790260 @default.
- W2313179993 hasConceptScore W2313179993C178790620 @default.
- W2313179993 hasConceptScore W2313179993C181199279 @default.
- W2313179993 hasConceptScore W2313179993C185592680 @default.
- W2313179993 hasConceptScore W2313179993C202751555 @default.
- W2313179993 hasConceptScore W2313179993C2780538656 @default.
- W2313179993 hasConceptScore W2313179993C40767141 @default.
- W2313179993 hasConceptScore W2313179993C486523 @default.
- W2313179993 hasConceptScore W2313179993C55493867 @default.
- W2313179993 hasConceptScore W2313179993C67705224 @default.
- W2313179993 hasConceptScore W2313179993C71240020 @default.
- W2313179993 hasConceptScore W2313179993C86803240 @default.
- W2313179993 hasIssue "4" @default.
- W2313179993 hasLocation W23131799931 @default.
- W2313179993 hasLocation W23131799932 @default.
- W2313179993 hasOpenAccess W2313179993 @default.
- W2313179993 hasPrimaryLocation W23131799931 @default.
- W2313179993 hasRelatedWork W1570438659 @default.
- W2313179993 hasRelatedWork W1997500570 @default.
- W2313179993 hasRelatedWork W2019547910 @default.
- W2313179993 hasRelatedWork W2049991593 @default.
- W2313179993 hasRelatedWork W2064042198 @default.
- W2313179993 hasRelatedWork W2081812181 @default.
- W2313179993 hasRelatedWork W2102978189 @default.
- W2313179993 hasRelatedWork W2123056841 @default.
- W2313179993 hasRelatedWork W2313179993 @default.
- W2313179993 hasRelatedWork W2435146534 @default.
- W2313179993 hasVolume "12" @default.
- W2313179993 isParatext "false" @default.
- W2313179993 isRetracted "false" @default.
- W2313179993 magId "2313179993" @default.
- W2313179993 workType "article" @default.