SCOPUS 정보 검색 플랫폼

Volumn 19, Issue 17, 2011, Pages 5238-5246

Structure-guided design and synthesis of P 1′ position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors

(8) Tagad, Harichandra D a Hamada, Yoshio a Nguyen, Jeffrey Tri a Hidaka, Koushi a Hamada, Takashi a Sohma, Youhei a Kimura, Tooru a Kiso, Yoshiaki a,b

a KYOTO PHARMACEUTICAL UNIVERSITY (Japan)

b NAGAHAMA INSTITUTE OF BIO SCIENCE AND TECHNOLOGY (Japan)

Author keywords

Secretase; Alzheimer's disease; Bioisosteres; Pentapeptides; Phenylcycloalkylamines

Indexed keywords

1 PHENYLCYCLOALKYLAMINE DERIVATIVE; BETA SECRETASE 1; BETA SECRETASE INHIBITOR; KMI 1830; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOHEXYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOHEXYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOPENTYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOPENTYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLETHYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLETHYLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (2 PHENYLPROPAN 2 YLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [1 [3 HYDROXY 4 OXO 1 PHENYL 4 (2 PHENYLPROPAN 2 YLAMINO)BUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [1 [4 (1 BENZYL 4 PHENYLPIPERIDIN 4 YLAMINO) 3 HYDROXY 4 OXO 1 PHENYLBUTAN 2 YLAMINO] 3 CYCLOHEXYL 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [1 [4 (1 BENZYL 4 PHENYLPIPERIDIN 4 YLAMINO) 3 HYDROXY 4 OXO 1 PHENYLBUTAN 2 YLAMINO] 3 CYCLOHEXYL 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [1 [4 (1 BENZYL 4 PHENYLPIPERIDIN 4 YLAMINO) 3 HYDROXY 4 OXO 1 PHENYLBUTAN 2 YLAMINO] 4 METHYL 1 OXOPENTAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOHEXYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOHEXYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLCYCLOPENTYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLETHYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1 PHENYLOPENTYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (1PHENYLETHYLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (2 PHENYLPROPAN 2 YLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPAN 2 YLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 5 FLUORO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDINE 4 CARBOXAMIDE; N [2 AMINO 3 [1 [3 CYCLOHEXYL 1 [3 HYDROXY 4 OXO 1 PHENYL 4 (2 PHENYLPROPAN 2 YLAMINO)BUTAN 2 YLAMINO] 1 OXOPROPANYLAMINO] 3 METHYL 1 OXOBUTAN 2 YLAMINO] 3 OXOPROPYL] 2,5 DIHYDROXYBENZAMIDE; UNCLASSIFIED DRUG;

ARTICLE; COMPUTER MODEL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; MOLECULAR DOCKING; STRUCTURE ACTIVITY RELATION;

AMINES; AMYLOID PRECURSOR PROTEIN SECRETASES; ASPARTIC ACID ENDOPEPTIDASES; DRUG DESIGN; HUMANS; PEPTIDES; PROTEASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84860398295 PISSN: 09680896 EISSN: 14643391 Source Type: Journal
DOI: 10.1016/j.bmc.2011.07.002 Document Type: Article

Times cited : (17)

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