ChemInform Abstract: Search for New Ca++ Antagonists. Lipophilic Oximes and Phosphonates.

Bellucci, C.; Teodori, Elisabetta; Gualtieri, Fulvio; Piacenza, Guy

doi:10.1002/chin.198612287

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“…Chemistry. The reaction pathways used to synthesise the designed compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) are described in Schemes 1-4 and their chemical and physical characteristics are reported in Table 1.…”

Section: Introductionmentioning

confidence: 99%

“…For several years we have been involved in the design and synthesis of L-type calcium channel antagonists related to verapamil, − and we decided to take advantage of the experience accumulated during this researche to design and study N-type calcium channel antagonists. Indeed, during the past decade, it was found that the classic L-type antagonists are not that specific, as a few of them show some action also on other types of calcium channels, namely the N-type.…”

Section: Introductionmentioning

confidence: 99%

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Design, Synthesis, and Preliminary Pharmacological Evaluation of 4-Aminopiperidine Derivatives as N-Type Calcium Channel Blockers Active on Pain and Neuropathic Pain

et al. 2004

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Several compounds with a 4-aminopiperidine scaffold decorated on both nitrogen atoms by alkyl or acyl moieties containing the structural motifs of verapamil and of flunarizine, as well as those that are more frequent in known N-type calcium channel antagonists, have been synthesized. Antinociceptive activity on the mouse hot-plate test was used to select molecules to be submitted to further studies. Active compounds were tested in vitro on a PC12 rat pheochromocytoma clonal cell line, to evaluate their action on N-type calcium channels, and on a rat model of neuropathic pain. Two compounds that show N-type calcium channel antagonism and are endowed with potent action on pain and neuropathic pain (3 and 18) have been selected for further studies.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Preliminary Pharmacological Evaluation of 4-Aminopiperidine Derivatives as N-Type Calcium Channel Blockers Active on Pain and Neuropathic Pain

et al. 2004

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ChemInform Abstract: Search for New Ca++ Antagonists. Lipophilic Oximes and Phosphonates.

Abstract: Das Nitril (I) reagiert mit den Dioxolanylalkylbromiden (II) über (III) zu den Aldehyden (IV).

Cited by 1 publication

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Design, Synthesis, and Preliminary Pharmacological Evaluation of 4-Aminopiperidine Derivatives as N-Type Calcium Channel Blockers Active on Pain and Neuropathic Pain

Design, Synthesis, and Preliminary Pharmacological Evaluation of 4-Aminopiperidine Derivatives as N-Type Calcium Channel Blockers Active on Pain and Neuropathic Pain

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