Discovery of potent and specific dihydroisoxazole inhibitors of human transglutaminase 2

Journal of Medicinal Chemistry

Volumn 57, Issue 21, 2014, Pages 9042-9064

  Klöck, Cornelius ^a   Herrera, Zachary ^a   Albertelli, Megan ^a   Khosla, Chaitan ^a,b  

^a STANFORD UNIVERSITY   (United States)

^b Stanford University   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACYLTRANSFERASE INHIBITOR; CK 805; CK 996; ERW 1041E; ISOXAZOLE DERIVATIVE; PROTEIN GLUTAMINE GAMMA GLUTAMYLTRANSFERASE 2; QUINOLIN 3 YLMETHYL 2 [(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL] 2 METHYLPYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [2 [(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)AMINO] 2 OXOETHYL]PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL)CARBAMOYL] 4 (2 HYDROXYBENZAMIDO)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL)CARBAMOYL] 4 (2 HYDROXYPHENYL)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 (3 CHLOROPHENYL)PYRROLIDINE 1 CARBOXYALTE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 (3 HYDROXYPHENYL)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 (4 CHLOROPHENYL)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 (5 FLUORO IH INDOL 3 YL)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 (PROP 2 YN 1 YLOXY)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 FLUOROPYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 METHOXYPYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL] 4 PHENYLPYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHY]CARBAMOYL] 4 (3 HYDROXYBENZAMIDO)PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL] 4 PHENYL 2,5 DIHYDRO 1H PYRROLE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL]AZETIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL]PIPERIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 3 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL] 3,4 DIHYDRO 1H PYRIDO[3,4 B]INDOLE 2 (9H) CARBOXYLATE; QUINOLIN 3 YLMETHYL 3 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5YL)METHYL]CARBAMOYL]PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 4 AMINO 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL]PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 4 BENZAMIDO 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL]PYRROLIDINE 1 CARBOXYLATE; QUINOLIN 3 YLMETHYL 4 BENZYL 2 [[(3 BROMO 4,5 DIHYDROISOXAZOL 5 YL)METHYL]CARBAMOYL]PYRROLIDINE 1 CARBOXYLATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZH 118; ZH 147A; ENZYME INHIBITOR; GUANINE NUCLEOTIDE BINDING PROTEIN; PROTEIN GLUTAMINE GAMMA GLUTAMYLTRANSFERASE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CROSS REACTION; DRUG POTENCY; DRUG SELECTIVITY; DRUG TOLERABILITY; ELECTROPHILICITY; HUMAN; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; HALF LIFE TIME; ISOLATION AND PURIFICATION; METABOLISM; SYNTHESIS;

ANIMALS; BIOLOGICAL AVAILABILITY; ENZYME INHIBITORS; GTP-BINDING PROTEINS; HALF-LIFE; HUMANS; ISOXAZOLES; MICE; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSGLUTAMINASES;

EID: 84923808396     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501145a     Document Type: Article

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