Bezencon, Olivier published the artcileDesign and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors, Safety of 2-chloro-3-methylisonicotinaldehyde, the main research area is aryl substituted diazabicyclononenecarboxamide preparation selective renin inhibitor antihypertensive; potent nonpeptidic bioavailable diazabicyclononenecarboxamide renin inhibitor; structure aryl substituted diazabicyclononenecarboxamide inhibition renin; mol crystal structure renin bound nonracemic aryloxyethylphenyl diazabicyclononenecarboxamide.
Aryl-substituted diazabicyclononenecarboxamides such as I are prepared as selective human renin inhibitors for potential use as antihypertensive agents. Aryl substituents and the carboxamide moiety of the diazabicyclononenecarboxamides are essential for selective binding to renin; attachment of a substituent to the methyleneaminomethylene bridge of the diazabicyclononenecarboxamides does not modify the binding affinity but alters the pharmacokinetics of the product. I inhibits renin with an IC50 of 0.20 nM in buffer and 19 nM in plasma; a 10 mg/kg dose of I lowers the blood pressures of transgenic rats over a period of 36 h. The structures of both enantiomers of an aryloxyethylphenyl diazabicyclononenecarboxamide sep. bound to human renin are determined by X-ray crystallog.
Journal of Medicinal Chemistry published new progress about Antihypertensives. 790696-96-7 belongs to class pyridine-derivatives, name is 2-chloro-3-methylisonicotinaldehyde, and the molecular formula is C7H6ClNO, Safety of 2-chloro-3-methylisonicotinaldehyde.