MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate.

MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate. Research Abstract Details 

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MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate. Abstract Text:

Ken-Ichi Yoshida,Kiyoshi Nakayama,Masami Ohtsuka,Noriko Kuru,Yoshihiro Yokomizo,Atsunobu Sakamoto,Makoto Takemura,Kazuki Hoshino,Hiroko Kanda,Hironobu Nitanai,Kenji Namba,Kumi Yoshida,Yuichiro Imamura,Jason Z Zhang,Ving J Lee,William J Watkins,Ken-Ichi Yoshida,Kiyoshi Nakayama,Masami Ohtsuka,Noriko Kuru,Yoshihiro Yokomizo,Atsunobu Sakamoto,Makoto Takemura,Kazuki Hoshino,Hiroko Kanda,Hironobu Nitanai,Kenji Namba,Kumi Yoshida,Yuichiro Imamura,Jason Z Zhang,Ving J Lee,William J Watkins,Ken-Ichi Yoshida,Kiyoshi Nakayama,Masami Ohtsuka,Noriko Kuru,Yoshihiro Yokomizo,Atsunobu Sakamoto,Makoto Takemura,Kazuki Hoshino,Hiroko Kanda,Hironobu Nitanai,Kenji Namba,Kumi Yoshida,Yuichiro Imamura,Jason Z Zhang,Ving J Lee,William J Watkins,

A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, substituted at the 2-position with piperidines bearing quaternary ammonium salt side chains, were synthesized and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the beta-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Attachment of the charged entity using an N-ethylcarbamoyloxy linker led to the discovery of the highly soluble compound 22 (D13-9001), which maintained good potency in vitro and displayed excellent activity in vivo in a rat pneumonia model of P. aeruginosa.

MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate. Publishing Authors By Initials

K Yoshida,K Nakayama,M Ohtsuka,N Kuru,Y Yokomizo,A Sakamoto,M Takemura,K Hoshino,H Kanda,H Nitanai,K Namba,K Yoshida,Y Imamura,JZ Zhang,VJ Lee,WJ Watkins,K Yoshida,K Nakayama,M Ohtsuka,N Kuru,Y Yokomizo,A Sakamoto,M Takemura,K Hoshino,H Kanda,H Nitanai,K Namba,K Yoshida,Y Imamura,JZ Zhang,VJ Lee,WJ Watkins,K Yoshida,K Nakayama,M Ohtsuka,N Kuru,Y Yokomizo,A Sakamoto,M Takemura,K Hoshino,H Kanda,H Nitanai,K Namba,K Yoshida,Y Imamura,JZ Zhang,VJ Lee,WJ Watkins,

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MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 7087-97

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 22

MONTH: 08

YEAR: 2007

MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate. Information

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LANGUAGE: eng

NlmUniqueID: 9413298

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Grant and Affiliation Information for MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate.

AFFILIATION: Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd, 16-13, Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan.

Country: England

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MEDLINETA: Bioorg Med Chem

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