Matches in SemOpenAlex for { <https://semopenalex.org/work/W2122296176> ?p ?o ?g. }
- W2122296176 endingPage "7162" @default.
- W2122296176 startingPage "7155" @default.
- W2122296176 abstract "The development of new HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel chemical entities of increased potency. Previous investigations in our laboratory resulted in the discovery of several novel series of arylazolylthioacetanilides as potent NNRTIs. In this study, based on the structure-based bioisosterism strategy, novel 1,2,4-triazin-6-yl thioacetamide derivatives were designed, synthesized and evaluated for their anti-HIV activity in MT-4 cells. Among them, the most promising compound was 8b15 with double-digit nanomolar activity against wild-type HIV-1 (EC(50)=0.018±0.007 μM) and moderate activity against the double mutant strain RES056 (EC(50)=3.3±0.1 μM), which indicated that 1,2,4-triazin-6-yl thioacetamide can be used as a novel scaffold to develop a new class of potent NNRTIs active against both wild-type and drug-resistant HIV-1 strains. In addition, preliminary structure-activity relationship (SAR) and molecular modeling results are also briefly discussed, which provide some useful information for the further design of novel NNRTIs." @default.
- W2122296176 created "2016-06-24" @default.
- W2122296176 creator A5016741562 @default.
- W2122296176 creator A5027734063 @default.
- W2122296176 creator A5031149051 @default.
- W2122296176 creator A5040662398 @default.
- W2122296176 creator A5059468550 @default.
- W2122296176 creator A5069927986 @default.
- W2122296176 creator A5081479819 @default.
- W2122296176 creator A5091214653 @default.
- W2122296176 creator A5091380652 @default.
- W2122296176 date "2012-12-01" @default.
- W2122296176 modified "2023-10-13" @default.
- W2122296176 title "Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs" @default.
- W2122296176 cites W1787470815 @default.
- W2122296176 cites W1977282539 @default.
- W2122296176 cites W1979203246 @default.
- W2122296176 cites W1984234311 @default.
- W2122296176 cites W1989331015 @default.
- W2122296176 cites W1991519292 @default.
- W2122296176 cites W1991670386 @default.
- W2122296176 cites W2006016090 @default.
- W2122296176 cites W2007088929 @default.
- W2122296176 cites W2013056086 @default.
- W2122296176 cites W2031081818 @default.
- W2122296176 cites W2032824735 @default.
- W2122296176 cites W2033255134 @default.
- W2122296176 cites W2036010588 @default.
- W2122296176 cites W2038775337 @default.
- W2122296176 cites W2045043030 @default.
- W2122296176 cites W2053818792 @default.
- W2122296176 cites W2062231842 @default.
- W2122296176 cites W2062744755 @default.
- W2122296176 cites W2063380198 @default.
- W2122296176 cites W2063825413 @default.
- W2122296176 cites W2072779381 @default.
- W2122296176 cites W2073415505 @default.
- W2122296176 cites W2079991727 @default.
- W2122296176 cites W2085313140 @default.
- W2122296176 cites W2103389647 @default.
- W2122296176 cites W2124496337 @default.
- W2122296176 cites W2132109825 @default.
- W2122296176 cites W2154386828 @default.
- W2122296176 cites W2173616003 @default.
- W2122296176 cites W2180699268 @default.
- W2122296176 doi "https://doi.org/10.1016/j.bmcl.2012.09.062" @default.
- W2122296176 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23084898" @default.
- W2122296176 hasPublicationYear "2012" @default.
- W2122296176 type Work @default.
- W2122296176 sameAs 2122296176 @default.
- W2122296176 citedByCount "44" @default.
- W2122296176 countsByYear W21222961762013 @default.
- W2122296176 countsByYear W21222961762014 @default.
- W2122296176 countsByYear W21222961762015 @default.
- W2122296176 countsByYear W21222961762016 @default.
- W2122296176 countsByYear W21222961762017 @default.
- W2122296176 countsByYear W21222961762018 @default.
- W2122296176 countsByYear W21222961762019 @default.
- W2122296176 countsByYear W21222961762020 @default.
- W2122296176 countsByYear W21222961762021 @default.
- W2122296176 countsByYear W21222961762022 @default.
- W2122296176 countsByYear W21222961762023 @default.
- W2122296176 crossrefType "journal-article" @default.
- W2122296176 hasAuthorship W2122296176A5016741562 @default.
- W2122296176 hasAuthorship W2122296176A5027734063 @default.
- W2122296176 hasAuthorship W2122296176A5031149051 @default.
- W2122296176 hasAuthorship W2122296176A5040662398 @default.
- W2122296176 hasAuthorship W2122296176A5059468550 @default.
- W2122296176 hasAuthorship W2122296176A5069927986 @default.
- W2122296176 hasAuthorship W2122296176A5081479819 @default.
- W2122296176 hasAuthorship W2122296176A5091214653 @default.
- W2122296176 hasAuthorship W2122296176A5091380652 @default.
- W2122296176 hasConcept C104317684 @default.
- W2122296176 hasConcept C114373084 @default.
- W2122296176 hasConcept C143065580 @default.
- W2122296176 hasConcept C185592680 @default.
- W2122296176 hasConcept C193042331 @default.
- W2122296176 hasConcept C202751555 @default.
- W2122296176 hasConcept C21951064 @default.
- W2122296176 hasConcept C2777752112 @default.
- W2122296176 hasConcept C55493867 @default.
- W2122296176 hasConcept C71240020 @default.
- W2122296176 hasConcept C74187038 @default.
- W2122296176 hasConceptScore W2122296176C104317684 @default.
- W2122296176 hasConceptScore W2122296176C114373084 @default.
- W2122296176 hasConceptScore W2122296176C143065580 @default.
- W2122296176 hasConceptScore W2122296176C185592680 @default.
- W2122296176 hasConceptScore W2122296176C193042331 @default.
- W2122296176 hasConceptScore W2122296176C202751555 @default.
- W2122296176 hasConceptScore W2122296176C21951064 @default.
- W2122296176 hasConceptScore W2122296176C2777752112 @default.
- W2122296176 hasConceptScore W2122296176C55493867 @default.
- W2122296176 hasConceptScore W2122296176C71240020 @default.
- W2122296176 hasConceptScore W2122296176C74187038 @default.
- W2122296176 hasIssue "23" @default.
- W2122296176 hasLocation W21222961761 @default.
- W2122296176 hasLocation W21222961762 @default.
- W2122296176 hasOpenAccess W2122296176 @default.