Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides

Journal of Medicinal Chemistry

Volumn 48, Issue 1, 2005, Pages 71-90

  Doherty, Elizabeth M ^a   Fotsch, Christopher ^a   Bo, Yunxin ^a   Chakrabarti, Partha P ^a   Chen, Ning ^a   Gavva, Narender ^a   Han, Nianhe ^a   Kelly, Michael G ^b   Kincaid, John ^b   Klionsky, Lana ^a   Liu, Qingyian ^a   Ognyanov, Vassil I ^a   Tamir, Rami ^a   Wang, Xianghong ^a   Zhu, Jiawang ^a   Norman, Mark H ^a   Treanor, James J S ^a  

^a AMGEN INC   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

3 (4 TERTBUTYLPHENYL) N (2,3 DIHYDROBENZO[B][1,4]DIOXIN 6 YL)ACRYLAMIDE; 3 [2 (PIPERIDIN 1 YL) 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL] N (QUINOLIN 7 YL)ACRYLAMIDE; 3 [2 MORPHOLINO 6 (TRIFLUOROMETHYL)PYRIDIN 3 YL] N (QUINOLIN 7 YL)ACRYLAMIDE; ACRYLAMIDE DERIVATIVE; CALCIUM ION; CAPSAICIN; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CALCIUM TRANSPORT; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG POTENCY; DRUG SYNTHESIS; IC 50; MALE; NONHUMAN; PH; RAT; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOCHEMISTRY; BIOLOGICAL AVAILABILITY; CALCIUM; CAPSAICIN; CHO CELLS; CINNAMATES; CRICETINAE; CRICETULUS; HUMANS; HYDROGEN-ION CONCENTRATION; INHIBITORY CONCENTRATION 50; ION CHANNELS; MALE; RATS; RATS, SPRAGUE-DAWLEY; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; TRPV CATION CHANNELS;

EID: 19944428963     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm049485i     Document Type: Article

References (61)

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