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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
1999-2-10
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pubmed:abstractText |
Based on X-ray crystallographic analysis of MKC-442/human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) complex, analogues in which the N1-substituent is replaced with omega-functionalized alkyl groups were designed to improve the affinity for the enzyme. Synthesis of these compounds was carried out starting from MKC-442 by a sequence of reactions (N3-protection, removal of N1-ethoxymethyl group, alkylation, and N3-deprotection). The compounds were evaluated for anti-HIV activity. Structure-activity relationships are discussed in terms of the possible interaction with the enzyme.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0956-3202
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pubmed:author |
pubmed-author:BabbLL,
pubmed-author:FujimotoKK,
pubmed-author:HayashiMM,
pubmed-author:HopkinsA LAL,
pubmed-author:JonesE YEY,
pubmed-author:MiyasakaTT,
pubmed-author:RecAA,
pubmed-author:StammersD KDK,
pubmed-author:StuartD IDI,
pubmed-author:TanakaHH,
pubmed-author:WalkerR TRT
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pubmed:issnType |
Print
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pubmed:volume |
9
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
325-32
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pubmed:dateRevised |
2009-8-19
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pubmed:meshHeading |
pubmed-meshheading:9875411-Allosteric Site,
pubmed-meshheading:9875411-Anti-HIV Agents,
pubmed-meshheading:9875411-Antiviral Agents,
pubmed-meshheading:9875411-Cell Line,
pubmed-meshheading:9875411-HIV Reverse Transcriptase,
pubmed-meshheading:9875411-HIV-1,
pubmed-meshheading:9875411-Hydrogen Bonding,
pubmed-meshheading:9875411-Mass Spectrometry,
pubmed-meshheading:9875411-Models, Molecular,
pubmed-meshheading:9875411-Molecular Structure,
pubmed-meshheading:9875411-Reverse Transcriptase Inhibitors,
pubmed-meshheading:9875411-Uracil,
pubmed-meshheading:9875411-Virus Replication
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pubmed:year |
1998
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pubmed:articleTitle |
Allosteric inhibitors against HIV-1 reverse transcriptase: design and synthesis of MKC-442 analogues having an omega-functionalized acyclic structure.
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pubmed:affiliation |
School of Pharmaceutical Sciences, Showa University, Tokyo, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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