Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Masayasu Kasai"'
Autor:
Shunkichi Tanaka, Hiroaki Shirahase, Nobuharu Kakeya, Kazuyoshi Kunishiro, Hiroshi Matsui, Masayasu Kasai
Publikováno v:
The Journal of Antibiotics. 64:233-242
To improve the oral absorption of meropenem (MEPM), we synthesized and evaluated a series of its double-promoiety prodrugs, in which lipophilic promoieties were introduced into carboxyl and pyrrolidinyl groups. Among these prodrugs, pivaloyloxymethyl
Autor:
Satoru Azukizawa, Masaki Fukui, Hiroaki Shirahase, Kazuya Otake, Hikaru Kamemoto, Kazuyoshi Kunishiro, Michiko Shibabayashi, Masayasu Kasai, Tomohiro Miike
Publikováno v:
Chemical and Pharmaceutical Bulletin. 59:1233-1242
Novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and (S)-7-(2-{2-[(E)-2-cyclopentylvinyl]-5-methyloxazol-4-yl}ethoxy)-2-[(2E,4E)-hexadienoyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14c) was identified as
Autor:
Hiroaki Shirahase, Kenji Takahashi, Satoru Azukizawa, Michiko Shibabayashi, Masaki Fukui, Kazuya Otake, Masayasu Kasai, Hikaru Kamemoto
Publikováno v:
Chemical and Pharmaceutical Bulletin. 59:876-879
2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome prolif
Autor:
Yoshimichi Shoji, Masayasu Kasai, Tomohiro Miike, Chisato Mukai, Masaru Ohta, Kazuyoshi Kunishiro, Kenji Takahashi, Hiroaki Shirahase, Mamoru Kanda
Publikováno v:
Chemical and Pharmaceutical Bulletin. 58:1066-1076
To find a novel acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor with anti-lipid peroxidative activity, a series of tetrahydroisoquinoline derivatives were synthesized and evaluated. A compound with a N-(4-hydroxy-2,3,5-trimethylphenyl)carbamoy
Autor:
Mamoru Kanda, Yoshimichi Shoji, Masayasu Kasai, Satoko Yogai, Masaru Ohta, Kazuyoshi Kunishiro, Kenji Takahashi, Yasuo Takeuchi, Hiroaki Shirahase
Publikováno v:
Bioorganic & Medicinal Chemistry. 17:6020-6031
A novel series of indoline-based acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors with a methanesulfonamide group at the 5-position were synthesized and their lipophilicity and biological activities were evaluated. Hepatic ACAT inhibitory and
Autor:
Yoshimichi Shoji, Mamoru Kanda, Kazuyoshi Kunishiro, Kazuyoshi Kurahashi, Masayasu Kasai, Kenji Takahashi, Hiroaki Shirahase, Masaru Ohta
Publikováno v:
Journal of Medicinal Chemistry. 51:4823-4833
A series of novel indoline derivatives with an ionizable moiety were synthesized to find a bioavailable acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor with antiperoxidative activity. [7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-y
Autor:
Hiroaki Shirahase, Tomohiro Miike, Kenji Takahashi, Chisato Mukai, Masayasu Kasai, Satoru Azukizawa, Mamoru Kanda, Kazuyoshi Kunishiro
Publikováno v:
Chemical and Pharmaceutical Bulletin. 56:335-345
A novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-Benzyl-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (10, KY-021) was iden
Autor:
Meiko Kitagawa, Tadakiyo Suzuki, Kenichi Nishimura, Minoru Toriya, Atsushi Sakai, Toshiyuki Kodama, Akiko Aoki, Seika Yamaguchi, Masayasu Kasai, Satoru Hatano, Taisuke Sugihara, Nobuhiro Mori, Akihisa Yoshimi, Toshio Nishijima
Publikováno v:
International Journal of Antimicrobial Agents. 19:439-442
Autor:
Minoru Toriya, Nobuhiro Mori, Akiko Aoki, Meiko Kitagawa, Seika Yamaguchi, Tadakiyo Suzuki, Toshio Nishijima, Kenichi Nishimura, Satoru Hatano, Toshiyuki Kodama, Akihisa Yoshimi, Taisuke Sugihara, Masayasu Kasai, Atsushi Sakai
Publikováno v:
International Journal of Antimicrobial Agents. 18:451-461
AS-924 is an oral prodrug of the antibiotic ceftizoxime (CTIZ), a parenteral use cephalosporin. This novel prodrug, produced by esterifying CTIZ with a lipophilic pivaloyloxymethyl (POM) group and introducing a water soluble L-alanyl group, is expect
Autor:
Hiroaki Shirahase, Nobuharu Kakeya, Satoru Hatano, Meiko Kitagawa, Akihisa Yoshimi, Masayasu Kasai, Kenichi Nishimura
Publikováno v:
The Journal of Antibiotics. 52:491-500
To improve the oral absorption of ceftizoxime (CZX), 7beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]- 3-cephem-4- carboxylic acid, we synthesized and evaluated a novel series of bifunctional prodrugs, in which L-alanine was introduced int