2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3, 4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): A potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A

Bioorganic and Medicinal Chemistry

Volumn 19, Issue 18, 2011, Pages 5490-5499

  Nishio, Yukihiro ^a   Kimura, Hidenori ^a   Sawada, Naoyuki ^a   Sugaru, Eiji ^a   Horiguchi, Masakuni ^a   Ono, Michiko ^a   Furuta, Yudai ^a   Sakai, Mutsuko ^a   Masui, Yumi ^a   Otani, Misato ^a   Hashizuka, Takahiko ^a   Honda, Yayoi ^a   Deguchi, Jiro ^a   Nakagawa, Tsutomu ^a   Nakahira, Hiroyuki ^a  

^a DAINIPPON SUMITOMO PHARMA CO LTD   (Japan)

Author keywords

DPP IV inhibitors; Mechanism based inactivation

Indexed keywords

2 [[6 (3 AMINO 3 METHYLPIPERIDINE 1 YL) 1,3 DIMETHYL 2,4 DIOXO 1,2,3,4 TETRAHYDRO 5H PYRROLO [3,2 D] PYRIMIDINE 5 YL]METHYL] 4 FLUOROBENZONITRILE; CYTOCHROME P450 3A; DIPEPTIDYL PEPTIDASE IV INHIBITOR; DSR 12727; GLUCOSE; PEPTIDASE; UNCLASSIFIED DRUG;

ADVERSE DRUG REACTION; AREA UNDER THE CURVE; ARTICLE; CURTIUS REARRANGEMENT; DISTRIBUTION VOLUME; DOG; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME ACTIVITY; ENZYME INACTIVATION; ENZYME INHIBITION; ENZYME KINETICS; GENOTOXICITY; GLUCOSE BLOOD LEVEL; GLUCOSE TOLERANCE; HAPLORHINI; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PHARMACOLOGICAL PARAMETERS; RAT; TOXICITY TESTING;

ANIMALS; BLOOD GLUCOSE; CYTOCHROME P-450 CYP3A; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; GLUCOSE TOLERANCE TEST; HAPLORHINI; HUMANS; MALE; MOLECULAR CONFORMATION; PYRAZOLES; PYRIMIDINES; RATS; RATS, ZUCKER; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS;

RATTUS;

EID: 80052571269     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.07.042     Document Type: Article

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