Fragment-to-hit-to-lead discovery of a novel pyridylurea scaffold of ATP competitive dual targeting type II topoisomerase inhibiting antibacterial agents

Journal of Medicinal Chemistry

Volumn 56, Issue 21, 2013, Pages 8712-8735

  Basarab, Gregory S ^a   Manchester, John I ^a   Bist, Shanta ^a   Boriack Sjodin, P Ann ^a,b   Dangel, Brian ^a   Illingworth, Ruth ^a   Sherer, Brian A ^a,c   Sriram, Shubha ^a   Uria Nickelsen, Maria ^a,d   Eakin, Ann E ^a,e  

^a ASTRAZENECA   (United Kingdom)

^b EPIZYME INC   (United States)

^c EMD Serono Research Institute   (United States)

^d PFIZER INC   (United States)

^e NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (3,3' BIPYRIDINE 6 YL) 3 ETHYLUREA; 1 (4 BROMO 5 IODOPYRIDIN 2 YL) 3 ETHYLUREA; 1 (4 CHLOROPYRIDIN 2 YL) 3 ETHYLUREA; 1 (4 CYANOPYRIDIN 2 YL) 3 ETHYLUREA; 1 (5 BROMO 4 CHLOROPYRIDIN 2 YL) 3 ETHYLUREA; 1 (5 BROMO 4 CYANOPYRIDIN 2 YL) 3 ETHYLUREA; 1 ETHYL 3 [5' (5 OXO 4,5 DIHYDRO 1,3,4 OXADIAZOL 2 YL) 4 [4 (TRIFLUOROMETHYL)THIAZOL 2 YL] 3,3' BIPYRIDIN 6 YL]UREA; 4 BROMO 5 IODOPYRIDIN 2 AMINE; ANTIINFECTIVE AGENT; DNA TOPOISOMERASE INHIBITOR; DNA TOPOISOMERASE IV INHIBITOR; ETHYL 2 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL] 1,3 BENZOTHIAZOLE 7 CARBOXYLATE; ETHYL 2 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL] 1,3 THIAZOLE 4 CARBOXYLATE; ETHYL 4' BROMO 6' (3 ETHYLUREIDO) 3,3' BIPYRIDINE 5 CARBOXYLATE; ETHYL 4' CHLORO 6' (3 ETHYLUREIDO) 3,3' BIPYRIDINE 5 CARBOXYLATE; ETHYL 6' [[(ETHYLAMINO)CARBONYL]AMINO] 3,3' BIPYRIDINE 5 CARBOXYLATE; GYRASE INHIBITOR; METHYL 2 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL] 1,3 THIAZOLE 5 CARBOXYLATE; METHYL 2 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL]BENZOATE; METHYL 3 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL]BENZOATE; METHYL 4 [6 [[(ETHYLAMINO)CARBONYL]AMINO]PYRIDIN 3 YL]BENZOATE; N (3,4' BIPYRIDIN 2' YL) N' ETHYLUREA; N (4 BROMOPYRIDIN 2 YL) N' ETHYLUREA; N (5' BROMO 3,4' BIPYRIDIN 2' YL) N' ETHYLUREA; N ETHYL N' (4 PHENYLPYRIDIN 2 YL)UREA; N ETHYL N' [5 (4,4,5,5 TETRAMETHYL 1,3,2 DIOXABOROLAN 2 YL)PYRIDIN 2 YL]UREA; NOVOBIOCIN; PYRIDYLUREA DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; UREA DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBACTERIAL ACTIVITY; ARTICLE; BACTERIAL COUNT; CONTROLLED STUDY; DNA SYNTHESIS; DRUG CLEARANCE; DRUG EFFICACY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HAEMOPHILUS INFLUENZAE; HUMAN; HUMAN TISSUE; HYDROGEN BOND; INFECTION; LIPOPHILICITY; MALE; MEMBRANE PERMEABILITY; MINIMUM INHIBITORY CONCENTRATION; MORAXELLA CATARRHALIS; MOUSE; NONHUMAN; PLASMA PROTEIN BINDING; STAPHYLOCOCCUS AUREUS; STREPTOCOCCUS PNEUMONIAE;

ADENOSINE TRIPHOSPHATE; ANIMALS; ANTI-BACTERIAL AGENTS; BACTERIA; DISEASE MODELS, ANIMAL; DNA TOPOISOMERASES, TYPE II; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; MICE; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; STAPHYLOCOCCAL INFECTIONS; STRUCTURE-ACTIVITY RELATIONSHIP; TOPOISOMERASE II INHIBITORS; UREA;

EID: 84887882612     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401208b     Document Type: Article

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