Alkylsulfanyl analogs as potent &#945;<sub>2</sub>Î´ ligands.

Shimada, Kousei; Ohata, Yasuo; Kobayashi, Jun; Onishi, Yoshiyuki; Kawamura, Asuka; Domon, Yuki; Arakawa, Naohisa; Inoue, Tatsuya; Kitano, Yutaka; Matsuda, Fumihiko; Abe, Yuki; Deguchi, Tsuneo

Alkylsulfanyl analogs as potent α₂Î´ ligands.

Shimada, Kousei; Ohata, Yasuo; Kobayashi, Jun; Onishi, Yoshiyuki; Kawamura, Asuka; Domon, Yuki; Arakawa, Naohisa; Inoue, Tatsuya; Kitano, Yutaka; Matsuda, Fumihiko; Abe, Yuki; Deguchi, Tsuneo.

Afiliação

Shimada K; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. Electronic address: shimada.kousei.ah@daiichisankyo.co.jp.
Ohata Y; Daiichi Sankyo RD Novare Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan.
Kobayashi J; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Onishi Y; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Kawamura A; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Domon Y; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Arakawa N; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Inoue T; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Kitano Y; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Matsuda F; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Abe Y; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Deguchi T; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.

Bioorg Med Chem Lett ; 28(11): 2000-2002, 2018 06 15.

Article em En | MEDLINE | ID: mdl-29752183

ABSTRACT

ABSTRACT

We identified novel (3R, 5S)-3-aminomethyl-5-methanesulfanyl hexanoic acid (5a DS75091588) and (3R, 5S)-3-aminomethyl-5-ethanesulfanyl hexanoic acid (6a DS18430756) as sulfur-containing Î³-amino acid derivatives that were useful for the treatment of neuropathic pain. These two compounds exhibited a potent analgesic effect in animal models of both type I diabetes and type II diabetes, and good pharmacokinetics.

Assuntos

Canais de Cálcio/metabolismo; Diabetes Mellitus Experimental/tratamento farmacológico; Diabetes Mellitus Tipo 1/tratamento farmacológico; Diabetes Mellitus Tipo 2/tratamento farmacológico; Neuralgia/tratamento farmacológico; Compostos de Sulfidrila/farmacologia; Animais; Caproatos/química; Caproatos/farmacologia; Diabetes Mellitus Experimental/metabolismo; Diabetes Mellitus Tipo 1/metabolismo; Diabetes Mellitus Tipo 2/metabolismo; Modelos Animais de Doenças; Ligantes; Camundongos; Estrutura Molecular; Neuralgia/metabolismo; Compostos de Sulfidrila/química

Palavras-chave

Alkylsulfanyl; Analgesic; Diabetes; α(2)Î´; Î³-Amino acid

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Sulfidrila / Canais de Cálcio / Diabetes Mellitus Experimental / Diabetes Mellitus Tipo 1 / Diabetes Mellitus Tipo 2 / Neuralgia Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article

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