Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Koichiro Morihira"'
Autor:
Takayuki Imaoka, Shin-ichi Tsukamoto, Tatsuaki Morokata, Ippei Sato, Makoto Takeuchi, Toshiya Takahashi, Yosuke Iura, Hideki Inoue, Mitsuaki Ohta, Hirokazu Kubota, Aiko Nitta, Koichiro Morihira
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6876-6881
Optimization starting with our lead compound 1 (IC(50)=4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrroli
Autor:
Shin-ichi Tsukamoto, Makoto Takeuchi, Toshiya Takahashi, Yosuke Iura, Mitsuaki Ohta, Koichiro Morihira, Ippei Sato, Takayuki Imaoka, Aiko Nitta, Tatsuaki Morokata, Hirokazu Kubota, Hiroki Tomioka
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4951-4954
The synthesis and structure–activity relationships of ureas as CCR3 antagonists are described. Optimization starting with lead compound 2 (IC50 = 190 nM) derived from initial screening hit compound 1 (IC50 = 600 nM) led to the identification of (S)
Publikováno v:
Tetrahedron Letters. 40:4235-4238
Cope rearrangement of the taxane-like tricyclic compounds having a 1,5-diene moiety readily takes place to give novel spirocyclic compounds. This transformation is found to be reversible and the product distribution is greatly dependent on the solven
Autor:
Hideki Anan, Yoshiya Terai, Hitoshi Sakashita, Koichiro Morihira, Ei-Ichi Nakai, Tadao Shibanuma, Yasuhiro Yonetoku, Yoshinori Okamoto, Makoto Takeuchi, Hiroyuki Kurihara, Yasuo Isomura
Publikováno v:
Chemical and Pharmaceutical Bulletin. 47:11-21
Based on the X-ray structure of the complex of Ac-Tyr-Val-Ala-Asp-H (L-709049) and interleukin-1 beta converting enzyme (ICE), we synthesized compounds which were derived from 2-NapCO-Val-Pro-Asp-CH2OPh (1) to obtain a potent inhibitor in the cell as
Autor:
Ryo Naito, Ken Ikeda, Tadao Shibanuma, Masahiko Hayakawa, Yasuo Isomura, Koichiro Morihira, Makoto Takeuchi
Publikováno v:
Chemical and Pharmaceutical Bulletin. 46:1274-1285
A series of 1-substituted-4-piperidyl benzhydrylcarbamate derivatives were synthesized and evaluated for binding affinity to M1, M2 and M3 receptors, and for antimuscarinic activities. Receptor binding assays indicated that 1-benzyl-4-piperidyl benzh
Publikováno v:
The Journal of Organic Chemistry. 59:3165-3174
We have developed efficient methods for construction of the C-2 oxygenated aromatic C-ring taxane skeleton based on an eight-membered ring cyclization involving a Lewis acid-mediated intramolecular coupling reaction of the dienol silyl ether at C-10
Autor:
Masaki Seto, Koichiro Morihira, Isao Kuwajima, Yoshiaki Horiguchi, Takashi Furukawa, Setsuo Katagiri
Publikováno v:
Chemistry Letters. 22:133-136
An oxygenated substituent at the 2-position (taxane numbering) plays a critical role to determine the endo/exo cyclization into the 8-membered ring system involved in the taxane skeleton, and the aromatic taxinine derivative was prepared from the cor
Autor:
Hidehiro Arai, Koichiro Morihira, Yusuke Nakamura, Yasuhiro Kataoka, Yoshiaki Horiguchi, Isao Kuwajima
Publikováno v:
ChemInform. 24
Lewis acid-mediated intramolecular cyclization of the dienol silyl ether or enol silyl ether and the acetal for medium-sized ring formation is described. Seven-, eight-, and nine-membered ring cyclization proceed in fairly good yields.
Autor:
Isao Kuwajima, Koichiro Morihira, Hiroyuki Kusama, Toshiyuki Nishimori, Yoshiaki Horiguchi, Takashi Tsuruo
Publikováno v:
ChemInform. 30
Artificial taxoids were synthesized and subjected to evaluation of their ability of multi-drug resistance reversing and antitumor activities. While the taxoid 4 could not increase cellular accumulation of vincristine in multi-drug resistant tumor cel
Autor:
Hidehiro Arai, Yasuhiro Kataoka, Isao Kuwajima, Yusuke Nakamura, Yoshiaki Horiguchi, Koichiro Morihira
Publikováno v:
Tetrahedron Letters. 33:6979-6982
Lewis acid-mediated intramolecular cyclization of the dienol silyl ether or enol silyl ether and the acetal for medium-sized ring formation is described. Seven-, eight-, and nine-membered ring cyclization proceed in fairly good yields.