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Volumn 21, Issue 24, 2013, Pages 7578-7583
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Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4- methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases
a
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Author keywords
2 Amino 5 oxadiazolyl thiazole; Collagen induced arthritis (CIA) model; Phosphoinositide 3 kinase ; The Ames test
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Indexed keywords
1 (N' HYDROXYCARBAMIMIDOYL)PIPERIDIN 3 YLACETATE;
1 CYANOPIPERIDIN 3 YLACETATE;
2 (ACETYLAMINO) 4 METHYL 1,3 THIAZOLE 5 CARBOXYLIC ACID;
2 AMINO 4 METHYL 1,3 THIAZOLE 5 CARBOXYLIC ACID;
5 (3 TERT BUTYL 1,2,4 OXADIAZOL 5 YL) 4 METHYL 1,3 THIAZOL 2 AMINE;
ACETAMIDE DERIVATIVE;
N [4 METHYL 5 [3 (2,2,2 TRIFLUOROETHYL) 1,2,4 OXADIAZOL 5 YL] 1,3 THIAZOL 2 YL]ACETAMIDE;
N [4 METHYL 5 [3 (MORPHOLIN 4 YL) 1,2,4 OXADIAZOL 5 YL] 1,3 THIAZOL 2 YL]ACETAMIDE;
N [4 METHYL 5 [3 (TETRAHYDROFURAN 3 YL) 1,2,4 OXADIAZOL 5 YL] 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 (3 TERT BUTYL 1,2,4 OXADIAZOL 5 YL) 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (1 HYDROXY 2 METHYLPROPAN 2 YL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (2 HYDROXY 2 METHYLPROPYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (2 HYDROXY 2,2 DIMETHYLBUTYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (2 HYDROXYETHYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (3 HYDROXY 2,2 DIMETHYLPROPYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (3 HYDROXY 3 METHYLBUTYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (3 HYDROXYPIPERIDIN 1 YL) 1,2 4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (3 HYDROXYROPYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (3 METHOXY 2,2 DIMETHYLPROPYL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
N [5 [3 (4 HYDROXY 2 METHYLBUTAN 2 YL) 1,2,4 OXADIAZOL 5 YL] 4 METHYL 1,3 THIAZOL 2 YL]ACETAMIDE;
PHOSPHATIDYLINOSITOL 3 KINASE GAMMA;
PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR;
TASP 0415914;
TERT BUTYL 3 (ACETYLOXY)PIPERIDINE 1 CARBOXYLATE;
UNCLASSIFIED DRUG;
ANIMAL CELL;
ANIMAL EXPERIMENT;
ANIMAL MODEL;
ANIMAL TISSUE;
AREA UNDER THE CURVE;
ARTHRITIS;
ARTICLE;
CONTROLLED STUDY;
DOSE RESPONSE;
DRUG EFFICACY;
DRUG EXPOSURE;
DRUG IDENTIFICATION;
DRUG POTENCY;
DRUG SCREENING;
DRUG STABILITY;
DRUG STRUCTURE;
DRUG SYNTHESIS;
ENZYME INHIBITION;
HUMAN;
HUMAN CELL;
HUMAN TISSUE;
IC 50;
IN VIVO STUDY;
LIVER CELL;
LIVER MICROSOME;
MACROPHAGE;
MALE;
MAXIMUM PLASMA CONCENTRATION;
MOUSE;
NONHUMAN;
RAT;
STRUCTURE ACTIVITY RELATION;
MUS;
2-AMINO-5-OXADIAZOLYL THIAZOLE;
COLLAGEN INDUCED ARTHRITIS (CIA) MODEL;
PHOSPHOINOSITIDE 3-KINASE Γ;
THE AMES TEST;
ADMINISTRATION, ORAL;
ANIMALS;
ARTHRITIS, EXPERIMENTAL;
CLASS IB PHOSPHATIDYLINOSITOL 3-KINASE;
COLLAGEN;
DISEASE MODELS, ANIMAL;
DOSE-RESPONSE RELATIONSHIP, DRUG;
DRUG DISCOVERY;
ENZYME INHIBITORS;
MALE;
MICE;
MICE, INBRED DBA;
MOLECULAR STRUCTURE;
OXADIAZOLES;
STRUCTURE-ACTIVITY RELATIONSHIP;
THIAZOLES;
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EID: 84888428277
PISSN: 09680896
EISSN: 14643391
Source Type: Journal
DOI: 10.1016/j.bmc.2013.10.042 Document Type: Article |
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Times cited : (24)
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References (24)
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