105901-12-0Relevant academic research and scientific papers
PYRROLE AND PYRAZOLE DERIVATIVES AS POTENTIATORS OF GLUTAMATE RECEPTORS
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Page/Page column 93-94, (2008/06/13)
The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.
Nonpeptide angiotensin II receptor antagonists. I. Synthesis and biological activity of pyridine derivatives
Ueyama,Yanagisawa,Kawai,Sonegawa,Baba,Mochizuki,Kosakai,Tomiyama
, p. 1841 - 1849 (2007/10/02)
Substituted pyridines were synthesized as potential angiotensin II (AII) receptor antagonists. Substitution at the position 2 in the pyridine resulted in potent activity, and the optimal alkyl length was four carbons. The potency further increased with the introduction of a hydroxymethyl group at the position 4. One of the compounds, 2-butyl-6-chloro-4-hydroxymethyl-5-methyl-3-[[2'-(1H-tetrazol-5-yl)bip henyl-4-yl]methyl]pyridine 9 h (KT3-579)is a competitive AII antagonist with a pA2 value of 9.31, and is about 10 times more potent than Du Pont 753. It was found to be an AT1 specific antagonist with an IC50 of 3.09 nM.
