Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: Discovery of an orally active GCP II inhibitor

Journal of Medicinal Chemistry

Volumn 46, Issue 10, 2003, Pages 1989-1996

  Majer, Pavel ^a   Jackson, Paul F ^a   Delahanty, Greg ^a   Grella, Brian S ^a   Ko, Yao Sen ^a   Li, Weixing ^a   Liu, Qun ^a   Maclin, Keith M ^a   Poláková, Jana ^a   Shaffer, Kathryn A ^a   Stoermer, Doris ^a   Vitharana, Dilrukshi ^a   Yanjun Wang, Eric ^a   Zakrzewski, Anthony ^a   Rojas, Camilo ^a   Slusher, Barbara S ^a   Wozniak, Krystyna M ^a   Burak, Eric ^a   Limsakun, Tharin ^a   Tsukamoto, Takashi ^a  

^a GUILFORD PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (3 MERCAPTOPROPYL)PENTANEDIOIC ACID; 2 (HYDROXYPENTAFLUOROPHENYLMETHYLPHOSPHINOYLMETHYL)PENTANEDIOIC ACID; 2 (PHOSPHONOMETHYL)PENTANEDIOIC ACID; 5 MERCAPTOPENTANOIC ACID; CARBENE; ENZYME INHIBITOR; GAMMA GLUTAMYL HYDROLASE; GLUTAMATE CARBOXYPEPTIDASE II INHIBITOR; GLUTARIC ACID DERIVATIVE; PHOSPHONIC ACID DERIVATIVE; PROPIONIC ACID; THIOL DERIVATIVE; UNCLASSIFIED DRUG; VALERIC ACID DERIVATIVE; ZINC;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COMPETITIVE INHIBITION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG EFFICACY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME SUBSTRATE; IC 50; MOLECULAR INTERACTION; MOLECULAR RECOGNITION; NEUROPATHIC PAIN; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANALGESICS; ANIMALS; BIOLOGICAL AVAILABILITY; CARBOXYPEPTIDASES; CONSTRICTION, PATHOLOGIC; ENZYME INHIBITORS; GLUTAMATE CARBOXYPEPTIDASE II; GLUTARATES; HEAT; HYPERALGESIA; MALE; PAIN; PERIPHERAL NERVOUS SYSTEM DISEASES; RATS; RATS, SPRAGUE-DAWLEY; SCIATIC NERVE; STRUCTURE-ACTIVITY RELATIONSHIP; SULFHYDRYL COMPOUNDS;

EID: 0038748474     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020515w     Document Type: Article

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