Abstract:
:(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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Finke PE,Oates B,Mills SG,MacCoss M,Malkowitz L,Springer MS,Gould SL,DeMartino JA,Carella A,Carver G,Holmes K,Danzeisen R,Hazuda D,Kessler J,Lineberger J,Miller M,Schleif WA,Emini EAdoi
10.1016/s0960-894x(01)00492-9subject
Has Abstractpub_date
2001-09-17 00:00:00pages
2475-9issue
18eissn
0960-894Xissn
1464-3405pii
S0960-894X(01)00492-9journal_volume
11pub_type
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