Use of an additional hydrophobic binding site, the Z site, in the rational drug design of a new class of stronger trypanothione reductase inhibitor, quaternary alkylammonium phenothiazines

Journal of Medicinal Chemistry

Volumn 43, Issue 16, 2000, Pages 3148-3156

  Khan, M O F ^a,c   Austin, S E ^a   Chan, C ^a   Yin, H ^a   Marks, D ^a   Vaghjiani, S N ^a   Kendrick, H ^b   Yardley, V ^b   Croft, S L ^b   Douglas, K T ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b LONDON SCHOOL OF HYGIENE AND TROPICAL MEDICINE   (United Kingdom)

^c UNIVERSITY OF DHAKA   (Bangladesh)

Author keywords

[No Author keywords available]

Indexed keywords

[3 (2 CHLORO 4A,10A DIHYDROPHENOTHIAZIN 10 YL)PROPYL](3,4 DICHLOROBENZYL)DIMETHYLAMMONIUM; CHLORPROMAZINE; PHENOTHIAZINE DERIVATIVE; TRYPANOTHIONE REDUCTASE; UNCLASSIFIED DRUG;

AFRICAN TRYPANOSOMIASIS; AMASTIGOTE; ARTICLE; CHAGAS DISEASE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING SITE; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; IN VITRO STUDY; LEISHMANIA DONOVANI; LEISHMANIASIS; NONHUMAN; STRUCTURE ACTIVITY RELATION; TRYPANOSOMA BRUCEI; TRYPANOSOMA CRUZI;

ANIMALS; ANTIPARASITIC AGENTS; BINDING SITES; CHLORPROMAZINE; DRUG DESIGN; ENZYME INHIBITORS; INHIBITORY CONCENTRATION 50; LEISHMANIA DONOVANI; LIGANDS; MACROPHAGES, PERITONEAL; MICE; MODELS, MOLECULAR; NADH, NADPH OXIDOREDUCTASES; PHENOTHIAZINES; QUATERNARY AMMONIUM COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMA CRUZI;

EID: 0034632778     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000156+     Document Type: Article

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