Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 20, 2012, Pages 6019-6033

  Clark, Rachel L ^a   Clements, Carol J ^a   Barrett, Michael P ^b   MacKay, Simon P ^a   Rathnam, Rajendra P ^c   Owusu Dapaah, George ^a   Spencer, John ^c,d   Huggan, Judith K ^a  

^a UNIVERSITY OF STRATHCLYDE   (United Kingdom)

^b UNIVERSITY OF GLASGOW   (United Kingdom)

^c UNIVERSITY OF GREENWICH   (United Kingdom)

^d UNIVERSITY OF SUSSEX   (United Kingdom)

Author keywords

Benzodiazepines; Trypanosomiasis

Indexed keywords

1 (2 PHENYL)BENZYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 (4 METHOXYBENZYL) 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 (4 PHENYL)BENZYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 (4 PHENYL)BENZYL 6 CHLORO 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 (CYCLOPROPYLMETHYL) 2H 3,1 BENZOXAZINE 2,4(1H) DIONE; 1 (CYCLOPROPYLMETHYL) 6 CHLORO 2H 3,1 BENZOXAZINE 2,4(1H) DIONE; 1 ALLYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 ALLYL 4 (CYCLOHEXYLMETHYL) 1 PROPYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,5 DIONE; 1 ALLYL 6 CHLORO 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 BENZYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 BENZYL 6 CHLORO 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 BUTYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 BUTYL 6 CHLORO 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 1 ETHYL 2H 3,1 BENZOXAZINE 2,4(1H) DIONE; 1 METHYL 2H 3,1 BENZOXAZINE 2,4(1H) DIONE; 1 PROPYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 4 (CYCLOHEXYLMETHYL) 1 ETHYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,4 DIONE; 4 (CYCLOHEXYLMETHYL) 1 METHYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,4 DIONE; 4 (CYCLOHEXYLMETHYL) 1 PROPYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,5 DIONE; 6 CHLORO 1 (2 PHENYL)BENZYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 6 CHLORO 1 ETHYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 6 CHLORO 1 METHYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 6 CHLORO 1 PROPYL 1H BENZO[D][1,3]OXAZINE 2,4 DIONE; 7 CHLORO 4 (CYCLOHEXYLMETHYL) 1 ETHYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,4 DIONE; 7 CHLORO 4 (CYCLOHEXYLMETHYL) 1 METHYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,4 DIONE; 7 CHLORO 4 (CYCLOHEXYLMETHYL) 1 PROPYL 3,4 DIHYDRO 1H BENZO[E][1,4]DIAZEPINE 2,5 DIONE; ANTITRYPANOSOMAL AGENT; BENZODIAZEPIN 2 ONE DERIVATIVE; QUINAZOLINE 2,4 DIONE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AFRICAN TRYPANOSOMIASIS; ALKYLATION; ARTICLE; CELL PROLIFERATION; DRUG DESIGN; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; LIPOPHILICITY; MELTING POINT; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PHYSICAL CHEMISTRY; STRUCTURE ACTIVITY RELATION; TRYPANOSOMA BRUCEI;

ANIMALS; BENZODIAZEPINES; HUMANS; MICROBIAL SENSITIVITY TESTS; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMIASIS, AFRICAN;

TRYPANOSOMA BRUCEI;

EID: 84866944696     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.08.049     Document Type: Article

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