Structure-based design, synthesis and preliminary evaluation of selective inhibitors of dihydrofolate reductase from Mycobacterium tuberculosis

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 13, 2007, Pages 4552-4576

  El Hamamsy, Mervat H R I ^a   Smith, Anthony W ^a   Thompson, Andrew S ^a   Threadgill, Michael D ^a  

^a University of Bath   (United Kingdom)

Author keywords

Dihydrofolate reductase; Glycerol; Mycobacterium tuberculosis; Pyrimidine 2,4 diamine; Structure based drug design

Indexed keywords

1 (4 BROMOPHENYL) 1 CYANO 7 HYDROXY 2 METHOXYHEPT 1 ENE; 1 (4 CHLOROPHENYL) 1 CYANO 2 METHOXYBUT 1 ENE; 1 (4 CHLOROPHENYL) 1 CYANO 7 HYDROXY 2 METHOXYHEPT 1 ENE; 1 CYANO 1 (3,4 DICHLOROPHENYL) 7 HYDROXY 2 METHOXYHEPT 1 ENE; 1 CYANO 7 HYDROXY 2 METHOXY 1 PHENYLHEPT 1 ENE; 2,3, O ISOPROPYLIDENE DEXTRO ERYTHRONOLACTONE; 5 (3,4 DICHLOROPHENYL) 6 (1,2,3 TRIHYDROXYPROPYL)PYRIMIDINE 2,4 DIAMINE; 5 (3,4 DICHLOROPHENYL) 6 (3,4,5 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (3,4 DICHLOROPHENYL) 6 (5 HYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 BROMOPHENYL) 6 (1,2,3 TRIHYDROXYPROPYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 BROMOPHENYL) 6 (3,4,5 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 BROMOPHENYL) 6 (5 HYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 CHLOROPHENYL) 6 (1,2,3 TRIHYDROXYPROPYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 CHLOROPHENYL) 6 (3,4,5 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 CHLOROPHENYL) 6 (5 HYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 (4 CHLOROPHENYL) 6 ETHYLPYRIMIDINE 2,4 DIAMINE(PYRIMETHAMINE); 5 ARYL 6 (1,2,3 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE DERIVATIVE; 5 ARYL 6 (3,4,5 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE DERIVATIVE; 5 ARYL 6 (5 HYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE DERIVATIVE; 5 PHENYL 6 (1,2,3 TRIHYDROXYPROPYL)PYRIMIDINE 2,4 DIAMINE; 5 PHENYL 6 (3,4,5 TRIHYDROXYPENTYL)PYRIMIDINE 2,4 DIAMINE; 5 PHENYL 6 (3,4,5 TRIHYDROXYPHENYL)PYRIMIDINE 2,4 DIAMINE; 6 (5 HYDROXYPENTYL) 5 PHENYLPYRIMIDINE 2,4 DIAMINE; BENZYL CYANIDE DERIVATIVE; DIHYDROFOLATE REDUCTASE INHIBITOR; ETHYL 4 BENZYLOXYMETHYL 2,2 DIMETHYL 1,3 DIOXOLANE 4 PROPANOIC ACID; GLYCEROL; PYRIMIDINE 2,4 DIAMINE DERIVATIVE; TETRAHYDROOXEPIN 2 ONE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ACYLATION; ANTIBIOTIC RESISTANCE; ARTICLE; BINDING SITE; CELL DEATH; CLINICAL EVALUATION; DRUG ACTIVITY; DRUG BINDING; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; GROWTH INHIBITION; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; PROTEIN MOTIF; SACCHAROMYCES; TUBERCULOSIS;

ANTITUBERCULAR AGENTS; BINDING SITES; FOLIC ACID ANTAGONISTS; GLYCEROL; HUMANS; INDICATORS AND REAGENTS; MAGNETIC RESONANCE SPECTROSCOPY; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MYCOBACTERIUM AVIUM COMPLEX; MYCOBACTERIUM TUBERCULOSIS; SACCHAROMYCES CEREVISIAE; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROFOLATE DEHYDROGENASE;

MYCOBACTERIUM TUBERCULOSIS; SACCHAROMYCES CEREVISIAE;

EID: 34248660823     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2007.04.011     Document Type: Article

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