Abstract:
:DPC168, a benzylpiperidine-substituted aryl urea CCR3 antagonist evaluated in clinical trials, was a relatively potent inhibitor of the 2D6 isoform of cytochrome P-450 (CYP2D6). Replacement of the cyclohexyl central ring with saturated heterocycles provided potent CCR3 antagonists with improved selectivity against CYP2D6. The favorable preclinical profile of DPC168 was maintained in an acetylpiperidine derivative, BMS-570520.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Pruitt JR,Batt DG,Wacker DA,Bostrom LL,Booker SK,McLaughlin E,Houghton GC,Varnes JG,Christ DD,Covington M,Das AM,Davies P,Graden D,Kariv I,Orlovsky Y,Stowell NC,Vaddi KG,Wadman EA,Welch PK,Yeleswaram S,Solomon KAdoi
10.1016/j.bmcl.2007.03.065subject
Has Abstractpub_date
2007-06-01 00:00:00pages
2992-7issue
11eissn
0960-894Xissn
1464-3405pii
S0960-894X(07)00368-Xjournal_volume
17pub_type
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