Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Ippei Sato"'
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)
Autor:
Takahiro Kuramochi, Issei Tsukamoto, Shuichi Sakamoto, Taku Taguchi, Akio Kakefuda, Ippei Sato
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:717-724
The sodium-calcium exchanger (NCX) transports Na+ and Ca2+ ions, and controls the Ca2+ concentration in myocytes. Calcium overload is induced via activation of reverse NCX, and is responsible for reperfusion injury in heart failure. Hence, NCX is an
Autor:
Ippei Sato, Shuichi Sakamoto, Taku Taguchi, Akio Kakefuda, Hiroyoshi Yamada, Takahiro Kuramochi
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:5039-5056
The sodium–calcium exchanger (NCX) is known as the transporter that controls the concentration of Ca2+ in cardiac myocytes. In the setting of heart failure and myocardial ischemia-reperfusion, NCX underlies an arrhythmogenic transient inward curren
Autor:
Takeshi Terauchi, Taro Terauchi, Naoki Kanoh, Tomoharu Tsukada, Ippei Sato, Takashi Tsunoda, Wataru Shoji, Masaya Nakata
Publikováno v:
Tetrahedron Letters. 44:7741-7745
The Mukaiyama aldol coupling of the second-generation C1C14 (AB) fragment of altohyrtins (spongistatins) with the model α-methyl-β-alkoxyaldehydes revealed that the stereochemistry at the newly formed carbon centers was controlled by the β-alko
Autor:
Kyoko Kimijima, Masataka Morita, Masaya Nakata, Takashi Tsunoda, Gouichirou Hayashi, Ippei Sato, Yasuhiro Nakamura, Naoki Kanoh, Tomoharu Tsukada, Taisaku Tanaka, Taro Terauchi, Wataru Shoji, Takeshi Terauchi
Publikováno v:
Tetrahedron Letters. 44:7747-7751
Coupling of the C1C14 (AB) crotylstannane with the C15C28 (CD) aldehyde followed by stereochemical arrangements gave the C1C28 (ABCD) fragment of altohyrtin C. The C29C44 (EF) fragment was also prepared. The syntheses of these two fragmen
Publikováno v:
Tetrahedron Letters. 41:2649-2653
Autor:
Keiko Suzuki, Ippei Sato, Makoto Takeuchi, Tatsuaki Morokata, Kazuki Ohno, Yosuke Iura, Koichiro Morihira, Hirokazu Kubota, Hiroshi Inami, Toshiya Takahashi, Mitsuaki Ohta, Takayuki Imaoka, Aiko Nitta, Shin-ichi Tsukamoto
Publikováno v:
Bioorganicmedicinal chemistry. 17(16)
Our laboratory has identified several acrylamide derivatives with potent CCR3 inhibitory activity. In the present study, we evaluated the in vitro metabolic stability (CLint; mL/min/kg) of these compounds in human liver microsomes (HLMs), and assesse
Autor:
Tatsuaki Morokata, Hirokazu Kubota, Keiko Suzuki, Takayuki Imaoka, Koichiro Morihira, Yosuke Iura, Mitsuaki Ohta, Toshiya Takahashi, Makoto Takeuchi, Aiko Nitta, Hiroshi Inami, Shin-ichi Tsukamoto, Ippei Sato
Publikováno v:
Bioorganicmedicinal chemistry. 16(18)
In our previous study on discovering novel types of CCR3 antagonists, we found a fluoronaphthalene derivative (1) that exhibited potent CCR3 inhibitory activity with an IC50 value of 20 nM. However, compound 1 also inhibited human cytochrome P450 2D6
Autor:
Noritaka Hamada, Yosuke Iura, Mitsuaki Ohta, Tatsuaki Morokata, Toshiya Takahashi, Koichiro Morihira, Makoto Takeuchi, Keiko Suzuki, Ippei Sato, Takayuki Imaoka, Shin-ichi Tsukamoto, Aiko Nitta, Hiroshi Inami, Hirokazu Kubota
Publikováno v:
Bioorganicmedicinal chemistry. 16(1)
A novel class of potent CCR3 receptor antagonists were designed and synthesized starting from N-{1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide (1),which was found by subjecting our chemical library to high throughput screening (HTS). The CC