Second-generation antibacterial benzimidazole ureas: Discovery of a preclinical candidate with reduced metabolic liability

Journal of Medicinal Chemistry

Volumn 57, Issue 21, 2014, Pages 8792-8816

  Grillot, Anne Laure ^a   Tiran, Arnaud Le ^a,b   Shannon, Dean ^a,c   Krueger, Elaine ^a   Liao, Yusheng ^a   Odowd, Hardwin ^a   Tang, Qing ^a   Ronkin, Steve ^a   Wang, Tiansheng ^a   Waal, Nathan ^a   Li, Pan ^a   Lauffer, David ^a   Sizensky, Emmanuelle ^a   Tanoury, Jerry ^a   Perola, Emanuele ^a   Grossman, Trudy H ^a,d   Doyle, Tim ^a   Hanzelka, Brian ^a   Jones, Steven ^a   Dixit, Vaishali ^a   Ewing, Nigel ^a   Liao, Shengkai ^a   Boucher, Brian ^a   Jacobs, Marc ^a   Bennani, Youssef ^a   Charifson, Paul S ^a   more..

^a VERTEX PHARMACEUTICALS   (United States)

^b INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

^c DE Synthetics   (Canada)

^d Tetraphase Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BENZIMIDAZOLE DERIVATIVE; LIVER PROTEIN; UREA; UREA DERIVATIVE; ANTIINFECTIVE AGENT; DNA TOPOISOMERASE (ATP HYDROLYSING); DNA TOPOISOMERASE IV; ENZYME INHIBITOR; GYRASE INHIBITOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIAL STRAIN; BLOOD SAMPLING; CHEMICAL PARAMETERS; CONTROLLED STUDY; COVALENT BOND; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; EPOXIDATION; HAPLORHINI; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MALE; METABOLITE; MINIMUM INHIBITORY CONCENTRATION; MOLECULE; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG DESIGN; METABOLISM; MICROBIAL SENSITIVITY TEST; SYNTHESIS;

ANIMALS; ANTI-BACTERIAL AGENTS; BENZIMIDAZOLES; DNA GYRASE; DNA TOPOISOMERASE IV; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; MICROBIAL SENSITIVITY TESTS; MICROSOMES, LIVER; STRUCTURE-ACTIVITY RELATIONSHIP; TOPOISOMERASE II INHIBITORS; UREA;

EID: 84923258321     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm500563g     Document Type: Article

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