The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 658-665

  Graham, Thomas H ^a   Shen, Hong C ^a   Liu, Wensheng ^a   Xiong, Yusheng ^a   Verras, Andreas ^a   Bleasby, Kelly ^a   Bhatt, Urmi R ^a   Chabin, Renee M ^a   Chen, Dunlu ^a   Chen, Qing ^a   Garcia Calvo, Margarita ^a   Geissler, Wayne M ^a   He, Huaibing ^a   Lassman, Michael E ^a   Shen, Zhu ^a   Tong, Xinchun ^a   Tung, Elaine C ^a   Xie, Dan ^a   Xu, Suoyu ^a   Colletti, Steven L ^a   Tata, James R ^a   Hale, Jeffrey J ^a   Pinto, Shirly ^a   Shen, Dong Ming ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Amide; Angiotensin; Angiotensinase C; Benzimidazole; Bioisostere; Enzyme inhibitor; Medicinal chemistry; Melanocyte stimulating hormone; Metabolic syndrome; Obesity; P glycoprotein; P gP; PrCP; Prekallikrein; Prolylcarboxypeptidase

Indexed keywords

AMIDE; BENZYLAMINE DERIVATIVE; GLYCOPROTEIN P; PEPTIDE HYDROLASE INHIBITOR; PROLINE CARBOXYPEPTIDASE; PROLYLCARBOXYPEPTIDASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BRAIN; CELL MEMBRANE PERMEABILITY; CONTINUOUS INFUSION; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG PENETRATION; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; IN VIVO STUDY; MOUSE; NONHUMAN; OBESITY; PROTEIN TRANSPORT; SERUM; WEIGHT REDUCTION;

AMIDES; ANIMALS; BENZIMIDAZOLES; BIOLOGICAL TRANSPORT; BODY WEIGHT; BRAIN; CARBOXYPEPTIDASES; DISEASE MODELS, ANIMAL; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MODELS, CHEMICAL; OBESITY; P-GLYCOPROTEINS; PYRROLIDINES; TIME FACTORS;

EID: 84655162123     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.060     Document Type: Article

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