Literature DB >> 16309909

Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels.

Takashi Yamamoto1, Seiji Niwa, Seiji Ohno, Tomoyuki Onishi, Hiroyuki Matsueda, Hajime Koganei, Hisayuki Uneyama, Shin-ichi Fujita, Tomoko Takeda, Morikazu Kito, Yukitsugu Ono, Yuki Saitou, Akira Takahara, Seinosuke Iwata, Masataka Shoji.   

Abstract

Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects which are related to its N-type calcium channel inhibitory activity. In order to find specific N-type calcium channel blockers with the least effects on cardiovascular system, we performed structure-activity relationship study on APJ2708, which is a derivative of cilnidipine, and found a promising N-type calcium channel blocker 21b possessing analgesic effect in vivo with a 1600-fold lower activity against L-type calcium channels than that of cilnidipine.

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Year:  2005        PMID: 16309909     DOI: 10.1016/j.bmcl.2005.11.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Molecular modelling and QSAR analysis of some structurally diverse N-type calcium channel blockers.

Authors:  Jignesh Mungalpara; Ashish Pandey; Vaibhav Jain; C Gopi Mohan
Journal:  J Mol Model       Date:  2009-10-04       Impact factor: 1.810

2.  Eco-friendly methodology to prepare N-heterocycles related to dihydropyridines: microwave-assisted synthesis of alkyl 4-arylsubstituted-6-chloro-5-formyl-2-methyl-1,4-dihydropyridine-3-carboxylate and 4-arylsubstituted-4,7-dihydrofuro[3,4-b]pyridine-2,5(1H,3H)-dione.

Authors:  Hortensia Rodríguez; Osnieski Martin; Margarita Suarez; Nazario Martín; Fernando Albericio
Journal:  Molecules       Date:  2011-11-21       Impact factor: 4.411

  2 in total

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