The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels |
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| Authors: | Yamamoto Takashi Niwa Seiji Ohno Seiji Tokumasu Munetaka Masuzawa Yoko Nakanishi Chika Nakajo Akira Onishi Tomoyuki Koganei Hajime Fujita Shin-Ichi Takeda Tomoko Kito Morikazu Ono Yukitsugu Saitou Yuki Takahara Akira Iwata Seinosuke Shoji Masataka |
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| Institution: | aPharmaceutical Research Laboratory, Ajinomoto company Inc., 1-1, Suzuki-cho, Kawasaki-ku, Kawasaki-shi, Japan |
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| Abstract: | In order to find an injectable and selective N-type calcium channel blocker, we have performed the structure–activity relationship (SAR) study on the 2-, 5-, and 6-position of 1,4-dihydropyridine-3-carboxylate derivative APJ2708 (2), which is a derivative of Cilnidipine and has L/N-type calcium channel dual inhibitory activities. As a consequence of the optimization, 6-dimethylacetal derivative 7 was found to have an effective inhibitory activity against N-type calcium channels with more than 170-fold lower activity for L-type channel compared to that of APJ2708. |
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| Keywords: | N-type calcium channel blocker Structure– activity relationships 1 4-dihydropyridine derivative |
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