Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Yoshihiro YOKOMIZO"'
Autor:
Kenji Yoshikawa, Toshiharu Yoshino, Makoto Takemura, Akiyoshi Mochizuki, Toshiharu Ohta, Tsutomu Nagata, Kouichi Uoto, Yoshihiro Yokomizo, Hiroyuki Naito, Katsuhiro Kawakami, Hideyuki Kanno, Makoto Suzuki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2133-2140
We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substi
Autor:
Kenji Namba, Masami Ohtsuka, Yoshihiro Yokomizo, Hironobu Nitanai, Kazuki Hoshino, Makoto Takemura, Ving J. Lee, Kiyoshi Nakayama, Jason Z. Zhang, Yoshida Kenichi, William J. Watkins, Hiroko Kanda
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:8506-8518
A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, derivatized at the 2-position with aromatic substituents, were synthesized by the Suzuki cross-coupling method and evaluated for their ability to potentiate the activity of the fluoroquinolone
Autor:
Yoshida Kenichi, William J. Watkins, Monica Palme, Aesop Cho, Katsuya Akimoto, Kazuki Hoshino, Ving J. Lee, Atsunobu Sakamoto, Jason Z. Zhang, Haruko Kawato, Kiyoshi Nakayama, Hiroko Ishida, Masami Ohtsuka, Yoshihiro Yokomizo, Noriko Kuru, Toshiharu Ohta, Junko Itoh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2493-2497
Exchange of the ethylene tether in a series of pyridopyrimidine-based MexAB-OprM specific efflux pump inhibitors to an amide bond stabilized the olefin of the acrylic acid moiety, preventing facile photoisomerization to the Z-isomer. Furthermore, the
Autor:
Aesop Cho, Yoshida Kenichi, Monica Palme, William J. Watkins, Atsunobu Sakamoto, Toshiharu Ohta, Noriko Kuru, Ving J. Lee, Masami Ohtsuka, Jun Watanabe, Haruko Kawato, Jason Z. Zhang, Hiroko Ishida, Kiyoshi Nakayama, Kazuki Hoshino, Yoshihiro Yokomizo, Kumi Yoshida
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:475-479
The addition of substituents to the pyridopyrimidine scaffold of MexAB-OprM specific efflux pump inhibitors was explored. As predicted by a pharmacophore model, the incorporation substituents at the 2-position improved potency. Piperidines were found
Autor:
Kumi Yoshida, Haruko Kawato, Yoshida Kenichi, William J. Watkins, Ving J. Lee, Yohei Ishida, Tsuyoshi Otani, Thomas E. Renau, Yoshihiro Yokomizo, Hiroko Ishida, Kazuki Hoshino, Masami Ohtsuka, Toshiharu Ohta, Yuichi Kurosaka, Kiyoshi Nakayama
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4205-4208
Problems of low solubility, high serum protein binding, and lack of efficacy in vivo in first generation MexAB-OprM specific efflux pump inhibitors were addressed. Through the use of pharmacophore modelling, the key structural elements for pump inhib
Autor:
Yoshida Kenichi, Shigeru Hosono, William J. Watkins, Haruko Kawato, Yoshihiro Yokomizo, Kiyoshi Nakayama, Kumi Yoshida, Toshiharu Ohta, Kazuki Hoshino, Roger Leger, Masami Ohtsuka, Ving J. Lee, Jason Z. Zhang, Yohei Ishida, Thomas E. Renau, Hiroko Ishida
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4201-4204
The identification of a series of compounds that specifically inhibit efflux by the MexAB-OprM pump system in Pseudomonas aeruginosa is described. Synthesis and in vitro structure-activity relationships (SARs) are outlined. Early leads lacked activit
Autor:
Yasuyuki TAKEDA, Keiichi KAWAGOE, Aki YOKOMIZO, Yoshihiro YOKOMIZO, Toru HOSOKAMI, Yoshimasa SHIMOTO, Yoshiaki TABUCHI, Yoshiyasu OGIHARA, Yuko HONDA, Keiko KAWARABAYASHI, Miki ISERI, Shuichi YOKOHAMA
Publikováno v:
Chemical and Pharmaceutical Bulletin. 47:755-771
In order to improve the biological characteristics of DA-3934 (5), a novel gastrin/cholecystokinin (CCK)-B receptor antagonist, phenoxyacetic acid derivatives replacing the N-methyl-N-phenylcarbamoylmethyl moiety of 5 with various alkyl chains have b
Publikováno v:
ChemInform. 24
In the presence of catalytic amounts of [1,2-benzenediolato(2-)-O,O′]oxotitanium and trimethylsilyl triflate, 1-O-trimethylsilyl-2,3,5-tri-O-benzyl-D-arabinofuranose stereoselectively reacts with various trimethylsilyl ethers to afford the correspo
Publikováno v:
Chemistry Letters. 21:1401-1404
In the presence of catalytic amounts of [1,2-benzenediolato(2-)-O,O′]oxotitanium and trimethylsilyl triflate, 1-O-trimethylsilyl-2,3,5-tri-O-benzyl-D-arabinofuranose stereoselectively reacts with various trimethylsilyl ethers to afford the correspo
Autor:
Kazuki Hoshino, Yoshida Kenichi, William J. Watkins, Atsunobu Sakamoto, Masami Ohtsuka, Kumi Yoshida, Yoshihiro Yokomizo, Yuichiro Imamura, Kiyoshi Nakayama, Hironobu Nitanai, Hiroko Kanda, Makoto Takemura, Ving J. Lee, Jason Z. Zhang, Noriko Kuru, Kenji Namba
Publikováno v:
Bioorganicmedicinal chemistry. 15(22)
A series of 4-oxo-4 H -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 fluoroquinol