Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan

Bioorganic and Medicinal Chemistry

Volumn 14, Issue 6, 2006, Pages 1978-1992

  Kamei, Katsuhide ^a   Maeda, Noriko ^a   Nomura, Kayoko ^a   Shibata, Makoto ^a   Katsuragi Ogino, Ryoko ^a   Koyama, Makoto ^a   Nakajima, Mika ^a   Inoue, Teruyoshi ^a   Ohno, Tomochika ^a   Tatsuoka, Toshio ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

1,4 benzoxazepine; 5 HT1A; Anti ischemia; Neuroprotective; Piclozotan; SUN N4057

Indexed keywords

1 METHYL 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,2 DIHYDRO 4H 1,4 BENZODIAZEPIN 3,5 DIONE; 1,4 BENZOXAZEPINE DERIVATIVE; 2 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 4,5 DIHYDRO 2H BENZAZEPIN 1,3 DIONE; 2,2 DIMETHYL 3 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 2,3 DIHYDRO 1,3 BENZOXAZIN 4 ONE; 3 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,3 3H BENZOXAZINE 2,4 DIONE; 3 CHLORO 4 [4 [3 (2 PYRIMIDINYL)PIPERIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 (2 PYRIDINYL) 1,2,3,6 TETRAHYDROPYRIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 (2 PYRIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 (2 PYRIMIDINYL) 1,2,3,6 TETRAHYDROPYRIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 (2 PYRIMIDINYL)PIPERIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 HYDROXY 4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [4 HYDROXY 4 (2 PYRIMIDINYL)PIPERIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 CHLORO 4 [4 [5 (2 PYRIMIDINYL) 1,2,3,6 TETRAHYDROPYRIDIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 3 METHYL 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,2 DIHYDRO 4H 1,4 BENZODIAZEPIN 3,5(2H,4H) DIONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,2 DIHYDRO 4H 1,4 BENZOXAZEPIN 5 ONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOTHIAZEPIN 3,5(2H,4H) DIONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 3,5(2H,4H) DIONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 1,4 BENZOXAZEPIN 5(4H) ONE; 4 [4 [4 (2 PYRIMIDINYL)PIPERAZIN 1 YL]BUTYL] 4,5 DIHYDRO 1,4 BENZOXAZEPIN 3(2H) ONE; AMINOPHENAZONE; BUSPIRONE; IPSAPIRONE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; SEROTONIN AGONIST; TANDOSPIRONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING ASSAY; BRAIN ISCHEMIA; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; IC 50; IN VITRO STUDY; MALE; MIDDLE CEREBRAL ARTERY OCCLUSION; NEUROPROTECTION; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BRAIN; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; ISCHEMIC ATTACK, TRANSIENT; MALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEUROPROTECTIVE AGENTS; OXAZEPINES; RATS; RATS, WISTAR; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN AGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA;

EID: 32044452397     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2005.10.046     Document Type: Article

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