Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Toshio Fujishita"'
Autor:
Hitoshi Murai, Tamio Fujiwara, Makoto Kodama, Chiaki Wakasa-Morimoto, Mark R. Underwood, Shigeru Miki, Scott A. Foster, Toshio Fujishita, Edward P. Garvey, Brian A. Johns, Yoshihiro Matsushita, Masanori Kobayashi, Koichiro Nakahara, Akihiko Sato, Takeshi Endoh, Tomokazu Yoshinaga, Eiichi Oosugi, Takahiro Seki, Akemi Suyama, Shinobu Kawauchi
Publikováno v:
Antiviral Research. 80:213-222
Resistance passage studies were conducted with five INIs (integrase inhibitors) that have been tested in clinical trials to date: a new naphthyridinone-type INI S/GSK-364735, raltegravir, elvitegravir, L-870,810 and S-1360. In establishing the passag
Autor:
Masayoshi Ogawa, Kunio Hayashi, Mariko Hara, Toshio Fujishita, Tsunetoshi Honma, Ryuichi Kiyama, Masafumi Fujimoto
Publikováno v:
Journal of Medicinal Chemistry. 38:2728-2741
Three-dimensional substructure searching (3D search), using the program MACCS-3D, was utilized for designing novel angiotensin II receptor antagonists which contain a bioisostere of the biphenylyltetrazole moiety of DuP 753. A 3D query was prepared f
Autor:
Mariko Hara, Tomoji Kawabata, Kunio Hayashi, Masaru Kawakami, Shigeyuki Nakajima, Ryuichi Kiyama, Masafumi Fujimoto, Toshio Fujishita
Publikováno v:
ChemInform. 26
A novel series of 6-alkyl-7-oxo-4,7-dihydropyrazolo[1,5-alpha]pyrimidine-3-carboxyli c acid derivatives was prepared as angiotensin II (AII) receptor antagonists. When evaluated in an in vitro binding assay using COS cells transfected with a cDNA enc
Autor:
Toshio Fujishita, Kazuo Kawasaki, Masami Eigyo, Takashi Sasatani, Nobuo Chomei, Makoto Adachi, Akira Matsushita, Susumu Takada, Shunji Murata
Publikováno v:
ChemInform. 27
2-Arylimidazo[4,5-c]quinolines and analogous fused imidazopyridines were synthesized and evaluated as benzodiazepine receptor ligands. Affinity to the receptors was greatly affected by the bulkiness of the aryl group at the 2-position, compared to th
Autor:
Takeshi Noshi, Chiaki Wakasa-Morimoto, Mikiko Kanamori-Koyama, Brian A. Johns, Tamio Fujiwara, Scott A. Foster, Mark R. Underwood, Masanori Kobayashi, Shinobu Kawauchi, Shigeru Miki, Takahiro Seki, Edward P. Garvey, Koichiro Nakahara, Akihiko Sato, Akemi Suyama, Toshio Fujishita, Tomokazu Yoshinaga
Publikováno v:
Antiviral research. 81(2)
Passage of HIV-1 in the presence of integrase inhibitors (INIs) generates resistant viruses that have mutations in the integrase region. Integrase-resistant mutations Q148K and Q148R were identified as primary mutations with the passage of HIV-1 IIIB
Autor:
Lisa St. John-Williams, Toshio Fujishita, Toshiro Yamaguchi, John S Walsh, M.Jane Cox Rosemond
Publikováno v:
Chemico-biological interactions. 147(2)
S-1360, a 1,3-diketone derivative, was the first HIV integrase inhibitor to enter human trials. Clinical data suggested involvement of non-cytochrome P450 clearance pathways, including reduction and glucuronidation. Reduction of S-1360 generates a ke
Autor:
Tamio Fujiwara, Toshio Fujishita, Takeshi Endo, David R. Davies, Yehuda Goldgur, Hirohiko Sugimoto, Hitoshi Murai, Tomokazu Yoshinaga, Gerson H. Cohen, Robert Craigie
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America. 96(23)
HIV integrase, the enzyme that inserts the viral DNA into the host chromosome, has no mammalian counterpart, making it an attractive target for antiviral drug design. As one of the three enzymes produced by HIV, it can be expected that inhibitors of
Autor:
Kunio Hayashi, Masaru Kawakami, Tomoji Kawabata, Toshio Fujishita, Ryuichi Kiyama, Mariko Hara, Masafumi Fujimoto, Shigeyuki Nakajima
Publikováno v:
Chemicalpharmaceutical bulletin. 43(6)
A novel series of 6-alkyl-7-oxo-4,7-dihydropyrazolo[1,5-alpha]pyrimidine-3-carboxyli c acid derivatives was prepared as angiotensin II (AII) receptor antagonists. When evaluated in an in vitro binding assay using COS cells transfected with a cDNA enc
Autor:
Shigeyuki Nakajima, Masaru Kawakami, Masafumi Fujimoto, Tomoji Kawabata, Toshio Fujishita, Koichi Ohtani, Mariko Hara, Ryuichi Kiyama, Koji Itazaki
Publikováno v:
European journal of pharmacology. 289(2)
Angiotensin AT1 receptor antagonists are divided into two types, surmountable, based on the way they inhibit angiotensin II-induced vasoconstriction. To elucidate what causes the difference, we studied how antagonists associate with and dissociate fr
Autor:
Toshio Fujishita, Mariko Hara, Masahiro Fuji, Masuhisa Nakamura, Tomoji Kawabata, Masafumi Fujimoto, Ryuichi Kiyama
Publikováno v:
Chemicalpharmaceutical bulletin. 43(3)
Starting from recently reported nonpeptidic angiotensin II (AII) receptor antagonists, we have designed and prepared a new series of 6-arylimidazo[4,5-c]pyridine derivatives. Variation of phenyl groups at the 4-, 6- or 7-position of imidazo[4,5-c]pyr