|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
18
|
|
pubmed:dateCreated |
2001-9-10
|
|
pubmed:abstractText |
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50=10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Sep
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:CarellaAA,
pubmed-author:CarverGG,
pubmed-author:DanzeisenRR,
pubmed-author:DeMartinoJ AJA,
pubmed-author:EminiE AEA,
pubmed-author:FinkeP EPE,
pubmed-author:GouldS LSL,
pubmed-author:HazudaDD,
pubmed-author:HolmesKK,
pubmed-author:KesslerJJ,
pubmed-author:LinebergerJJ,
pubmed-author:MacCossMM,
pubmed-author:MalkowitzLL,
pubmed-author:MillerMM,
pubmed-author:MillsS GSG,
pubmed-author:OatesBB,
pubmed-author:SchleifW AWA,
pubmed-author:SpringerM SMS
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
17
|
|
pubmed:volume |
11
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2475-9
|
|
pubmed:dateRevised |
2005-11-17
|
|
pubmed:meshHeading |
pubmed-meshheading:11549450-Animals,
pubmed-meshheading:11549450-Anti-HIV Agents,
pubmed-meshheading:11549450-Butanes,
pubmed-meshheading:11549450-Cells, Cultured,
pubmed-meshheading:11549450-Cricetinae,
pubmed-meshheading:11549450-Drug Design,
pubmed-meshheading:11549450-Drug Evaluation, Preclinical,
pubmed-meshheading:11549450-HIV-1,
pubmed-meshheading:11549450-Humans,
pubmed-meshheading:11549450-Inhibitory Concentration 50,
pubmed-meshheading:11549450-Neutrophils,
pubmed-meshheading:11549450-Piperidines,
pubmed-meshheading:11549450-Receptors, CCR5,
pubmed-meshheading:11549450-Structure-Activity Relationship
|
|
pubmed:year |
2001
|
|
pubmed:articleTitle |
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. paul_finke@merck.com
|
|
pubmed:publicationType |
Journal Article
|
