Discovery of (1 S,2 R,3 R)-2,3-dimethyl-2-phenyl-1- sulfamidocyclopropanecarboxylates: Novel and highly selective aggrecanase inhibitors

Journal of Medicinal Chemistry

Volumn 54, Issue 8, 2011, Pages 2839-2863

  Shiozaki, Makoto ^a   Maeda, Katsuya ^a   Miura, Tomoya ^a   Kotoku, Masayuki ^a   Yamasaki, Takayuki ^a   Matsuda, Isamu ^a   Aoki, Kenta ^a   Yasue, Katsutaka ^a   Imai, Hiroto ^a   Ubukata, Minoru ^a   Suma, Akira ^a   Yokota, Masahiro ^a   Hotta, Takahiro ^a   Tanaka, Masahiro ^a   Hase, Yasunori ^a   Haas, Julia ^b   Fryer, Andrew M ^b   Laird, Ellen R ^b   Littmann, Nicole M ^b   Andrews, Steven W ^b   Josey, John A ^b   Mimura, Takayuki ^a   Shinozaki, Yuichi ^a   Yoshiuchi, Hiromi ^a   Inaba, Takashi ^a   more..

^a JAPAN TOBACCO INC   (Japan)

^b ARRAY BIOPHARMA INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2,3 DIMETHYL 2 PHENYL 1 SULFAMIDOCYCLOPROPANECARBOXYLATE DERIVATIVE; AGGRECANASE; AGGRECANASE 1; AGGRECANASE 2; AMINO ACID; CARBOXYLIC ACID DERIVATIVE; CYCLOPROPANE DERIVATIVE; ENZYME INHIBITOR; HETEROCYCLIC COMPOUND; HYDROXAMIC ACID DERIVATIVE; PIPERIDINE; SULFANILAMIDE DERIVATIVE; UNCLASSIFIED DRUG; CYCLOPROPANE; PROTEINASE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; NONHUMAN; OSTEOARTHRITIS; RAT; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECT; IC 50; MOUSE; MOUSE MUTANT; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; CRYSTALLOGRAPHY, X-RAY; CYCLOPROPANES; DRUG DISCOVERY; ENDOPEPTIDASES; ENZYME INHIBITORS; INHIBITORY CONCENTRATION 50; MAGNETIC RESONANCE SPECTROSCOPY; MICE; MICE, KNOCKOUT; MODELS, MOLECULAR; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79955422907     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm101609j     Document Type: Article

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