|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0019693,
umls-concept:C0086418,
umls-concept:C0087111,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0231491,
umls-concept:C0442027,
umls-concept:C0935763,
umls-concept:C1098714,
umls-concept:C1332700,
umls-concept:C1527415,
umls-concept:C1611588,
umls-concept:C1880355
|
|
pubmed:issue |
21
|
|
pubmed:dateCreated |
2001-10-4
|
|
pubmed:abstractText |
Structure-activity studies on piperidino-piperidine 3 led to the discovery of SCH 351125 (1), a selective CCR5 antagonist with potent activity against RANTES binding (K(i) = 2 nM), which possesses subnanomolar activity in blocking viral entry and has excellent antiviral potency versus a panel of primary HIV-1 viral isolates. Compound 1, which has good oral bioavailability in rats, dogs, and monkeys, is proposed as a potential therapeutic agent for the treatment of HIV-1 and has entered human clinical trials.
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|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
11
|
|
pubmed:volume |
44
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
3339-42
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:11585437-Administration, Oral,
pubmed-meshheading:11585437-Animals,
pubmed-meshheading:11585437-Anti-HIV Agents,
pubmed-meshheading:11585437-Biological Availability,
pubmed-meshheading:11585437-Cell Line,
pubmed-meshheading:11585437-Cyclic N-Oxides,
pubmed-meshheading:11585437-Dogs,
pubmed-meshheading:11585437-Drug Evaluation, Preclinical,
pubmed-meshheading:11585437-HIV-1,
pubmed-meshheading:11585437-Humans,
pubmed-meshheading:11585437-Leukocytes, Mononuclear,
pubmed-meshheading:11585437-Macaca fascicularis,
pubmed-meshheading:11585437-Piperazines,
pubmed-meshheading:11585437-Piperidines,
pubmed-meshheading:11585437-Pyridines,
pubmed-meshheading:11585437-Rats,
pubmed-meshheading:11585437-Receptors, CCR5,
pubmed-meshheading:11585437-Structure-Activity Relationship
|
|
pubmed:year |
2001
|
|
pubmed:articleTitle |
Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
|
|
pubmed:affiliation |
Chemical Research, Drug Safety and Metabolism, and Antiviral Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. anandan.palani@spcorp.com
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|
pubmed:publicationType |
Journal Article,
In Vitro
|
