40255-47-8Relevant academic research and scientific papers
Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
Lee, Jie Eun,Koh, Hun Yeong,Seo, Seon Hee,Baek, Yi Yeon,Rhim, Hyewhon,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
scheme or table, p. 4219 - 4222 (2010/09/04)
T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs
Synthesis and biological evaluation of novel T-type Ca2+ channel blockers
Jung, Hee Kyung,Doddareddy, Munikumar Reddy,Cha, Joo Hwan,Rhim, Hyewhon,Cho, Yong Seo,Koh, Hun Yeong,Jung, Bong Young,Pae, Ae Nim
, p. 3965 - 3970 (2007/10/03)
A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca 2+ channel. The compound 21 with trifluoromethyl substituents at C3-position of phenyl group (R1) and C2- position of phenyl group (R2) showed the highest inhibitory activity with IC50 value of 1.02μM, which is comparable to that of mibefradil.
POTENTIAL NEUROLEPTICS OF THE ORTHOPRAMIDE SERIES; SYNTHESIS OF N-(3-(TERT.AMINO)PROPYL)-5-SULFAMOYL-2-METHOXYBENZAMIDES
Valenta, Vladimir,Vlkova, Marie,Holubek, Jiri,Svatek, Emil,Metysova, Jirina,Protiva, Miroslav
, p. 797 - 808 (2007/10/02)
Heating ethyl 5-sulfamoyl-2-methoxybenzoate with a series of twelve 3-(tert.amino)propylamines (IIIa-IIIl) afforded the title compounds IIa-IIl which were transformed to salts and subjected to pharmacological screening as potential neuroleptics of the sulpiride series.Only compounds IId (hydrogen oxalate, VUFB-15 453) and IIg (methanesulfonate, VUFB-15 397) showed indications of the desired psychotropic activity.
