Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 16, 2011, Pages 4836-4843

  Yuan, Jing ^a   Simpson, Robert D ^a   Zhao, Wei ^a   Tice, Colin M ^a   Xu, Zhenrong ^a   Cacatian, Salvacion ^a   Jia, Lanqi ^a   Flaherty, Patrick T ^a   Guo, Joan ^a   Ishchenko, Alexey ^a   Wu, Zhongren ^a   McKeever, Brian M ^a   Scott, Boyd B ^a   Bukhtiyarov, Yuri ^a   Berbaum, Jennifer ^a   Panemangalore, Reshma ^a   Bentley, Ross ^b   Doe, Christopher P ^b   Harrison, Richard K ^a   McGeehan, Gerard M ^a   Singh, Suresh B ^a   Dillard, Lawrence W ^a   Baldwin, John J ^a   Claremon, David A ^a   more..

^a Vitae Pharmaceuticals   (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Biphenyl; Diphenyl ether; Hypertension; Renin inhibitors; Structure based design; X ray crystallography

Indexed keywords

BIPHENYL ETHER RENIN INHIBITOR; CYTOCHROME P450 3A4; DIPHENYL ETHER RENIN INHIBITOR; RENIN INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIHYPERTENSIVE ACTIVITY; ARTICLE; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; ENZYME INHIBITION; HUMAN; HYPERTENSION; IC 50; NONHUMAN; PROCESS OPTIMIZATION; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 CYP3A; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME INHIBITORS; HUMANS; HYPERTENSION; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PHENYL ETHERS; RATS; RATS, TRANSGENIC; RECOMBINANT PROTEINS; RENIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 79960897000     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.06.043     Document Type: Article

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