Výsledky vyhledávání

Novel potassium channel openers. Part 4: transformation of the 1,4-benzoxazine skeleton into 1,4-benzothiazine, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroquinoxaline, indoline, and 1,5-benzoxazepine

Autor: Yoko Yamagiwa, Isao Yanagisawa, Akira Matsuhisa, Hiroyuki Nohira, Toru Yoden, Tadao Shibanuma, Ryuji Tsuzuki, Yuzo Matsumoto

Publikováno v: Bioorganic & Medicinal Chemistry. 8:393-404

As part of a search for a new potassium channel opener, the 1,4-benzoxazine skeleton derived from the benzopyran skeleton of cromakalim, was transformed into other fused rings such as 1,4-benzothiazine, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2eceea160e064cf5bd4593fd343fc7e1
https://doi.org/10.1016/s0968-0896(99)00292-8

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Studies on Aromatase Inhibitors IV. Synthesis and Biological Evaluation of N,N-Disubstituted-5-aminopyrimidine Derivatives

Autor: Yosiaki Shimada, Masafumi Kudou, Minoru Okada, Yasuo Isomura, Toru Yoden, Eiji Kawaminami

Publikováno v: Chemical and Pharmaceutical Bulletin. 45:1293-1299

In order to study the potency of the 5-aminopyrimidine skeleton as an aromatase inhibitor, we synthesized various N,N-disubstituted-5-aminopyrimidine derivatives and evaluated their aromatase-inhibitory activity (in vitro) and their inhibitory activi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38101a61fc9dcf24842ef55ad9d248fc
https://doi.org/10.1248/cpb.45.1293

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Studies on Aromatase Inhibitors. II. Synthesis and Biological Evaluation of 1-Amino-1H-1,2,4-triazole Derivatives

Autor: Yasuo Isomura, Yoshiaki Shimada, Toru Yoden, Minoru Okada, Eiji Kawaminami, Masafumi Kudoh

Publikováno v: Chemical and Pharmaceutical Bulletin. 45:333-337

1-N,N-Disubstituted amino-1-H-1,2,4-triazole derivatives were prepared and evaluated for aromatase-inhibitory activity (in vitro) and for the inhibitory activity on pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis (in vivo). 1-N-par

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbe09af60fb580a7069b6e86eab9ae56
https://doi.org/10.1248/cpb.45.333

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Studies on Aromatase Inhibitors. I. Synthesis and Biological Evaluation of 4-Amino-4H-1,2,4-triazole Derivatives

Autor: Masafumi Kudoh, Takashi Fujikura, Yasuo Isomura, Minoru Okada, Yoshiaki Shimada, Eiji Kawaminami, Hisataka Shikama, Toru Yoden

Publikováno v: Chemical and Pharmaceutical Bulletin. 44:1871-1879

Various 4-N-substituted amino-4H-1, 2, 4-triazole derivatives were synthesized and evaluated for aromatase-inhibitory activity (in vitro) and for pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis-inhibitory activity (in vivo). The 4-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea56f06ea1b25880de31c78c8302b362
https://doi.org/10.1248/cpb.44.1871

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ChemInform Abstract: Novel Potassium Channel Activators: Synthesis and Structure-Activity Relationship Studies of 3,4-Dihydro-2H-1,4-benzoxazine Derivatives

Autor: Wataru Uchida, Akira Matsuhisa, Shigeo Fujita, Ryuji Tsuzuki, Masaharu Asano, Yuzo Matsumoto, Isao Yanagisawa, Takashi Fujikura, Kazuhisa Takayama, Toru Yoden

Publikováno v: ChemInform. 27

Strong potassium channel-activating effects were found among a series of novel 4-substituted 3, 4-dihydro-2H-1, 4-benzoxazine derivatives. The key step in preparation was the nucleophilic substitution of 3, 4-dihydro-2H-1, 4-benzoxazine (3) with acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9daf3b9cd8219392d09c0a5206386dd8
https://doi.org/10.1002/chin.199630202

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Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists

Autor: Hiroshi Koutoku, Masafumi Kudoh, Isao Kinoyama, Toru Yoden, Takashi Furutani, Minoru Okada, Nobuaki Taniguchi

Publikováno v: Chemicalpharmaceutical bulletin. 52(11)

The search for novel antiandrogens by high-throughput screening (HTS) of the Yamanouchi chemical library led to the discovery of the lead compound (5), which possesses an arylmorpholine moiety. Through the optimization of the lead compound (5), we ha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8d26c86b9302d8ac6cc594feaa32ccf
https://pubmed.ncbi.nlm.nih.gov/15516756

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Studies on aromatase inhibitors. III. Synthesis and biological evaluation of [(4-bromobenzyl)(4-cyanophenyl)amino]azoles and their azine analogs

Autor: Yasuo Isomura, Toru Yoden, Masafumi Kudoh, Yoshiaki Shimada, Eiji Kawaminami, Minoru Okada

Publikováno v: Chemicalpharmaceutical bulletin. 45(3)

A series of [(4-bromobenzyl)(4-cyanophenyl)amino]azoles and their azine analogs, which have the side chain of the selective aromatase inhibitor YM511, were synthesized and evaluated for aromatase-inhibitory activity (in vitro) and for pregnant mare s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1615d6b29f5180546bbe32b5b4139185
https://pubmed.ncbi.nlm.nih.gov/9085555

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