Výsledky vyhledávání - "Hidenobu Murafuji"

Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors

Autor: Hidenobu Murafuji, Tsuyoshi Muto, Megumi Goto, Seiichi Imajo, Hajime Sugawara, Yoshiaki Oyama, Yutaka Minamitsuji, Shuji Miyazaki, Kenichi Murai, Hiromichi Fujioka

Publikováno v: Bioorganicmedicinal chemistry letters. 29(2)

A series of imidazolinylindole derivatives were discovered as novel kallikrein 7 (KLK7, stratum corneum chymotryptic enzyme) inhibitors. Structure-activity relationship (SAR) studies led to the identification of potent human KLK7 inhibitors. By furth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b396ccb3a5cbcdd812ae5907cd4d69e
https://pubmed.ncbi.nlm.nih.gov/30522951

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Structure-based drug design to overcome species differences in kallikrein 7 inhibition of 1,3,6-trisubstituted 1,4-diazepan-7-ones

Autor: Hiroki Sakai, Tsuyoshi Muto, Hidenobu Murafuji, Toshiyuki Tomoo, Seiichi Imajo, Hajime Sugawara, Yoshiaki Oyama, Megumi Goto

Publikováno v: Bioorganicmedicinal chemistry. 26(12)

A series of 1,3,6-trisubstituted 1,4-diazepan-7-ones were prepared as kallikrein 7 (KLK7, stratum corneum chymotryptic enzyme) inhibitors. Previously reported compounds 1 – 3 were potent human KLK7 inhibitors; however, they did not exhibit inhibito

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5211457c538fcb04a64130d5dce673b
https://pubmed.ncbi.nlm.nih.gov/29884582

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Structure-based drug design of 1,3,6-trisubstituted 1,4-diazepan-7-ones as selective human kallikrein 7 inhibitors

Autor: Megumi Goto, Hajime Sugawara, Toshiyuki Tomoo, Yoshiaki Oyama, Tsuyoshi Muto, Seiichi Imajo, Hiroki Sakai, Hidenobu Murafuji

Publikováno v: Bioorganicmedicinal chemistry letters. 28(8)

A novel series of 1,3,6-trisubstituted 1,4-diazepan-7-ones were investigated as human kallikrein 7 (KLK7, stratum corneum chymotryptic enzyme) inhibitors. Based on the X-ray co-crystal structure of compound 1 bound to human KLK7, the derivatives of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24349643dea5730ddbcb9979a0150917
https://pubmed.ncbi.nlm.nih.gov/29550094

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Discovery and structure-activity relationship study of 1,3,6-trisubstituted 1,4-diazepane-7-ones as novel human kallikrein 7 inhibitors

Autor: Hiroki Sakai, Megumi Goto, Seiichi Imajo, Hidenobu Murafuji, Hajime Sugawara, Tsuyoshi Muto

Publikováno v: Bioorganicmedicinal chemistry letters. 27(23)

Compound 1, composed of a 1,3,6-trisubstituted 1,4-diazepane-7-one, was discovered as a novel human kallikrein 7 (KLK7, stratum corneum chymotryptic enzyme, SCCE) inhibitor, and its derivatives were synthesized and evaluated. Structure-activity relat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9eebda696849c15e7e899b1e698c881
https://pubmed.ncbi.nlm.nih.gov/29102227

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Phosphodiesterase 7A inhibitor ASB16165 impairs proliferation of keratinocytes in vitro and in vivo

Autor: Masao Murakawa, Kazuhiro Nagahira, Takashi Nakatsuka, Kumiko Kadoshima-Yamaoka, Atsuto Ogata, Ryosuke Yoshioka, Yoshitaka Tanaka, Satomi Kanki, Hidenobu Murafuji, Hidekazu Inoue, Yasuhiro Hayashi, Megumi Goto, Yoshiaki Fukuda

Publikováno v: European Journal of Pharmacology. 633:93-97

Excessive proliferation of epidermal keratinocytes is a typical aspect of chronic skin diseases such as psoriasis. In the present study, the effect of phosphodiesterase 7A (PDE7A) inhibitor ASB16165 on proliferation of keratinocytes was investigated

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::246e320e17a05a0012cfadb309d5ea36
https://doi.org/10.1016/j.ejphar.2010.01.024

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Inhibition of phosphodiesterase 7A ameliorates Concanavalin A-induced hepatitis in mice

Autor: Atsuto Ogata, Takashi Nakatsuka, Hidenobu Murafuji, Kumiko Kadoshima-Yamaoka, Yoshiaki Fukuda, Kenji Chamoto, Kazuhiro Nagahira, Hidekazu Inoue, Yasuhiro Hayashi, Masao Murakawa, Asako Nagahira, Yoshitaka Tanaka, Takashi Nishimura, Kenju Miura, Satomi Kanki, Megumi Goto

Publikováno v: International Immunopharmacology. 9:1347-1351

An intravenous injection of Concanavalin A (Con A) elevated the serum level of alanine aminotransferase (ALT) activity, a marker for liver damage, and an oral administration of PDE7A inhibitor SUN11817 suppressed the increase of ALT activity in a dos

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0794096455cf40766e65dda48885cc3b
https://doi.org/10.1016/j.intimp.2009.08.002

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ASB16165, a phosphodiesterase 7A inhibitor, reduces cutaneous TNF-α level and ameliorates skin edema in phorbol ester 12-O-tetradecanoylphorbol-13-acetate-induced skin inflammation model in mice

Autor: Atsuto Ogata, Hidekazu Inoue, Yasuhiro Hayashi, Yoshiaki Fukuda, Kumiko Kadoshima-Yamaoka, Kazuhiro Nagahira, Satomi Kanki, Hidenobu Murafuji, Masao Murakawa, Ryosuke Yoshioka, Yoshitaka Tanaka, Takashi Nakatsuka, Megumi Goto

Publikováno v: European Journal of Pharmacology. 613:163-166

Possible role of phosphodiesterase 7A (PDE7A) in skin inflammation was examined using ASB16165, a specific inhibitor for PDE7A. Epicutaneous application of phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) to mouse ear resulted in induction of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ca4c0f781b6f023f2a451fb0c06cf37
https://doi.org/10.1016/j.ejphar.2009.04.014

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Phosphodiesterase 7A inhibitor ASB16165 suppresses proliferation and cytokine production of NKT cells

Autor: Hidekazu Inoue, Yasuhiro Hayashi, Yoshitaka Tanaka, Kumiko Kadoshima-Yamaoka, Hidenobu Murafuji, Yoshiaki Fukuda, Masao Murakawa, Takashi Nishimura, Kenji Chamoto, Kenju Miura, Megumi Goto, Takashi Nakatsuka, Kazuhiro Nagahira

Publikováno v: Cellular Immunology. 258:147-151

A possible involvement of phosphodiesterase 7A (PDE7A) in proliferation and function of NKT cells was examined using ASB16165, a selective inhibitor for PDE7A. Stimulation of isolated murine NKT cells with anti-CD3 antibody plus IL-2 induced not only

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22006aad43428471e967f70eab280bf4
https://doi.org/10.1016/j.cellimm.2009.04.005

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Artificial model for cystathionine β-synthase: construction of a catalytic cycle with a pyridoxal model compound having an ionophore function

Autor: Eito Yoshioka, Hidenobu Murafuji, Hiroshi Iwaki, Takeshi Imanishi, Kazuyuki Miyashita

Publikováno v: Tetrahedron. 59:4867-4872

Catalytic transformation of serine- O -carbonate to S -aryl cysteine derivatives was successfully achieved in the presence of Li + by the use of a pyridoxal model compound having an ionophore function, which is the first example mimicking cystathioni

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::82e12654ed927b510475725ac16770f3
https://doi.org/10.1016/s0040-4020(03)00665-3

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Artificial model for cystathionine β-synthase: efficient β-replacement reaction with thiols employing a novel pyridoxal model compound having an imidazole function

Autor: Hiroshi Iwaki, Takeshi Imanishi, Eito Yoshioka, Kazuyuki Miyashita, Hidenobu Murafuji

Publikováno v: Tetrahedron. 59:4873-4879

As a second-generation pyridoxal model compound for cystathionine β-synthase, we designed a novel model compound having an ionophore function and an imidazole function, application of which to the β-replacement reaction with various thiols smoothly

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a3b2d54926703858807f245fe9970c9f
https://doi.org/10.1016/s0040-4020(03)00666-5

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