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Volumn 21, Issue 24, 2011, Pages 7489-7495

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

Author keywords

Amino piperidines; Antibacterial; Bacterial type IIA topoisomerase; In vivo efficacy; Pharmacokinetics

Indexed keywords

AMINO PIPERIDINE DERIVATIVE; ANTIINFECTIVE AGENT; BACTERIAL TYPE IIA TOPOISOMERASE; CIPROFLOXACIN; DNA TOPOISOMERASE; NOVOBIOCIN; PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 81255208413     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.09.117     Document Type: Article
Times cited : (47)

References (26)
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    • 78549260109 scopus 로고    scopus 로고
    • (b) For the syntheses of these compounds and experimental details for the reactions in this paper see WO2002056882
    • (b) For the syntheses of these compounds and experimental details for the reactions in this paper see: Davies, D. T.; Jones, G. E.; Markwell, R. E.; Miller, W.; Pearson, N. D. WO2002056882; Chem. Abstr. 2002, 137, 125092.
    • (2002) Chem. Abstr. , vol.137 , pp. 125092
    • Davies D., .T.1    Jones G., .E.2    Markwell R., .E.3    Miller, W.4    Pearson, N.D.5
  • 26
    • 33846263060 scopus 로고    scopus 로고
    • All animal experiment protocols were approved by the Animal Care and Use Committee at GlaxoSmithKline Pharmaceuticals (PA, USA). The pharmacokinetics of compound 8 was studied in male Sprague-Dawley rats, male Beagle dogs and male cynomolgus monkeys following single intravenous and oral administration. Absolute oral bioavailability was estimated using a cross-over study design (n = 3). Blood samples were assayed using protein precipitation followed by LCMS/MS analysis and the concentration-time data were analyzed by non-compartmental methods (WinNonlin, v3.2). The in vitro plasma protein binding and microsomal intrinsic clearance were determined as described in Xiang, H.; McSurdy-Freed, J.; Moorthy, G. S.; Hugger, E.; Bambal, R.; Han, C.; Ferrer, S.; Gargallo, D.; Davis, C. B. J. Pharm. Sci. 2006, 95, 2657.
    • (2006) J. Pharm. Sci. , vol.95 , pp. 2657
    • Xiang, H.1    McSurdy-Freed, J.2    Moorthy G., .S.3    Hugger, E.4    Bambal, R.5    Han, C.6    Ferrer, S.7    Gargallo, D.8    Davis, C.B.9


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.