Time-dependent diaryl ether inhibitors of InhA: Structure-activity relationship studies of enzyme inhibition, antibacterial activity, and in vivo efficacy

ChemMedChem

Volumn 9, Issue 4, 2014, Pages 776-791

  Pan, Pan ^a   Knudson, Susan E ^b   Bommineni, Gopal R ^a   Li, Huei Jiun ^a   Lai, Cheng Tsung ^a   Liu, Nina ^a   Garcia Diaz, Miguel ^a   Simmerling, Carlos ^a   Patil, Sachindra S ^c   Slayden, Richard A ^b   Tonge, Peter J ^a  

^a STONY BROOK UNIVERSITY   (United States)

^b Department of Environmental and Radiological Health Sciences   (United States)

^c Kanashi Biotech Pvt Ltd   (India)

Author keywords

diaryl ethers; enoyl ACP reductases; fatty acid biosynthesis; InhA; inhibitors; structure activity relationships; time dependent inhibition

Indexed keywords

ANTIINFECTIVE AGENT; DIARYL ETHER DERIVATIVE; INHIBIN A; INHIBIN A INHIBITOR; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; ENZYME INHIBITOR; ETHER DERIVATIVE; INHIBIN; INHIBIN-ALPHA SUBUNIT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBACTERIAL ACTIVITY; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; DRUG TARGETING; ENZYME INHIBITION; ENZYME INHIBITOR COMPLEX; FATTY ACID SYNTHESIS; IN VIVO STUDY; MOUSE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TUBERCULOSIS; ANIMAL; ANTAGONISTS AND INHIBITORS; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; MICROBIAL SENSITIVITY TEST; SYNTHESIS; TIME; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTI-BACTERIAL AGENTS; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; ETHERS; INHIBINS; MICE; MICE, INBRED C57BL; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MYCOBACTERIUM TUBERCULOSIS; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS; TUBERCULOSIS;

EID: 84898011360     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201300429     Document Type: Article

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