Aminothienopyridazine inhibitors of tau aggregation: Evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo properties

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 14, 2012, Pages 4451-4461

  Ballatore, Carlo ^a,b   Crowe, Alex ^b   Piscitelli, Francesco ^a   James, Michael ^b   Lou, Kevin ^a   Rossidivito, Gabrielle ^a   Yao, Yuemang ^b   Trojanowski, John Q ^b   Lee, Virginia M Y ^b   Brunden, Kurt R ^b   Smith III, Amos B ^a  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

Alzheimer's disease; Aminothienopyridazine; K18PL; Tau aggregation inhibitor; Tauopathy

Indexed keywords

5 AMINO 3 (2 CHLOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLIC ACID; 5 AMINO 3 (4 FLUOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLIC ACID; 5 AMINO CYCLOPROPYL 3 (4 FLUOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXAMIDE; AMINOTHIENOPYRIDAZINE DERIVATIVE; ETHYL 1 (2 CHLOROPHENYL) 5 CYANO 4 METHYL 6 OXO 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 1 (3 CHLOROPHENYL) 5 CYANO 4 METHYL 6 OXO 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 2 [2 (3 CHLOROPHENYL)HYDRAZONO] 3 OXOBUTANOATE; ETHYL 2 [2 (4 CHLOROPHENYL)HYDRAZONO] 3 OXOBUTANOATE; ETHYL 2 [2 (4 FLUOROPHENYL)HYDRAZONO] 3 OXOBUTANOATE; ETHYL 2 [2 (4 HYDROXOPHENYL)HYDRAZONO] 3 OXOBUTANOATE; ETHYL 2 [2 (4 ISOPROPYLPHENYL)HYDRAZONO] 3 OXOBUTANOATE; ETHYL 3 OXO 2 [2 [4 (TRIFLUOROMETHOXY)PHENYL]HYDRAZONO]BUTANOATE; ETHYL 3 OXO 2 [2 [4 (TRIFLUOROMETHYL)PHENYL]HYDRAZONO]BUTANOATE; ETHYL 5 AMINO 3 (2 CHLOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO [3,4 5]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (2 CHLOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (3 CHLOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (4 CHLOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (4 FLUOROPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (4 HYDROXYPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 3 (4 ISOPROPYLPHENYL) 4 OXO 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 4 OXO 3 [4 (TRIFLUOROMETHOXY)PHENYL] 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 AMINO 4 OXO 3 [4 (TRIFLUOROMETHYL)PHENYL] 3,4 DIHYDROTHIENO[3,4 D]PYRIDAZINE 1 CARBOXYLATE; ETHYL 5 CYANO 1 (4 FLUOROPHENYL) 4 METHYL 6 OXO 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 5 CYANO 1 (4 HYDROXYPHENYL) 4 METHYL 6 OXO 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 5 CYANO 1 (4 ISOPROPYLPHENYL) 4 METHYL 6 OXO 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 5 CYANO 4 METHYL 6 OXO 1 [4 (TRIFLUOROMETHOXY)PHENYL] 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; ETHYL 5 CYANO 4 METHYL 6 OXO 1 [4 (TRIFLUOROMETHYL)PHENYL] 1,6 DIHYDROPYRIDAZINE 3 CARBOXYLATE; PYRIDAZINE DERIVATIVE; TAU PROTEIN; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; CONTROLLED STUDY; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; ENZYME INHIBITION; FEMALE; FERTILIZATION IN VITRO; IN VIVO STUDY; MOUSE; NONHUMAN; PROTEIN AGGREGATION; REVIEW; STRUCTURE ACTIVITY RELATION;

MUS;

EID: 84863202528     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.05.027     Document Type: Article

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