26416-25-1Relevant academic research and scientific papers
Novel pyrrolidine or piperidine derivatives having activity for T-type calcium channel
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Paragraph 0299-0302; 0309-0312, (2020/04/23)
A pyrrolidine or piperidine compound having activity for T - type calcium channel, wherein the pyrrolidine or piperidine compound of Formula 1 according to the present invention has an excellent antagonistic activity to, T-type calcium channel, and can be used as a preventive or therapeutic agent, for pain diseases, or cancer related to cancer, or cancer such as, epilepsy and,hepatic pain, angina. (by machine translation)
Synthesis and biological evaluation of pyrrolidine-based T-type calcium channel inhibitors for the treatment of neuropathic pain
Yang, Hak Kyun,Son, Woo Seung,Lim, Keon Seung,Kim, Gun Hee,Lim, Eun Jeong,Gadhe, Changdev G.,Lee, Jae Yeol,Jeong, Kyu-Sung,Lim, Sang Min,Pae, Ae Nim
, p. 1460 - 1471 (2018/09/26)
The treatment of neuropathic pain is one of the urgent unmet medical needs and T-type calcium channels are promising therapeutic targets for neuropathic pain. Several potent T-type channel inhibitors showed promising in vivo efficacy in neuropathic pain a
Benzo-fused lactams that promote the release of growth hormone
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, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
General Base Catalysis, Structure-Reactivity interactions, and Merging of Mechanisms for Elimination Reactions of (2-Arylethyl)quinuclidinium Ions
Gandler, Joseph R.,Jencks, William P.
, p. 1937 - 1951 (2007/10/02)
Structure-reactivity parameters and interaction coefficients are reported for elimination reactions of N-(2-arylethyl)quinuclidinium ions and for 2-arylethyl halides and tosylates in 60percent Me2SO/wares at 40 deg C, based on direct measurements of Bronsted β values for general base catalysis by oxyanion buffers, Hammet ρ values, and β1g for substituted quinuclidines.The Bronsted slopes increase from β - 0.67 for N-(2-(p-nitrophenyl)ethyl)quinuclidinium ions, which react by an E1cBirr mechanism, to β ca. 0.9 for the reactions of other N-(2-arylethyl)quinuclidinium ions by a concerted E2 elimination.There is no detectable interaction between the base catalyst and the leaving group for E1cB elimination, so that the interaction coefficient pxy = dβ1g/dpKBH = dβ/dpK1g is ca.0 for the N-(2-(p-nitrophenyl)ethyl)quinuclidinium ions.In contrast, values of β1g become less negative with increasing pKa of the base catalyst for the p-cyano and other N-(2-arylethyl)quinuclidinium ions, giving a constant value of pxy = 0.018 for the E2 elimination reactions of these compounds.The positive pxy coefficient for the N-(2-phenylethyl)quinuclidinium ions is confirmed by the observation of less negative values of β1g as the effective basicity of aqueous tetramethylammonium hydroxyde is increased by the addition of Me2SO.An increase in β with poorer leaving groups in the series of 2-(p-nitrophenyl)ethyl halides also corresponds to a positive pxy coefficient and an E2 mechanism.The interaction between the leaving group and central atoms is shown by the less negative values of β1g with electron-withdrawing substituents on the β-phenyl group, which corresponds to a negative coefficient pyy' = -dβ1g/d?- = -dρ/dpK1g = -0.09.A small decrease in β with electron-withdrawing substituents on the β-phenyl group suggests an interaction between the base catalyst and the central atoms that is described by a negative coefficient pxy' = dβ/d?- = dρ/dpKBH = -0.07.The sign of the pyy' and pxy' coefficient are consistent with an important component of proton transfer in the transition state.These properties of the E2 elimination reactions of N-(2-arylethyl)quinuclidinium ions can be described by a reaction coordinate that is rotated 24 deg counterclockwise from the x coordinate (for proton transfer) on a reaction coordinate-energy diagram that is defined by the observed structure-reactivity parameters.In contrast, β increases with increasing ? for elimination reactions of 2-arylethyl bromides with a positive value of pxy' = 0.07.This suggests more diagonal character to the transition state on the reaction coordinate diagram.The change from E1cB to an E2 mechanism is more easily described as a transformation of mechanism than as a change between two coexisting mechanisms.
