OBJECTIVE(S) The structure- activity relationship of a series of 36 molecules, showing L-type calcium channel blocking was studied using a QSAR (quantitative structure-activity relationship) method. MATERIALS AND METHODS Structures were optimized by the semi-empirical AM1 quantum-chemical method which was also used to find structure-calcium channel blocking activity trends. Several types of d...

Previous studies have suggested the presence of different types of calcium channels in different regions of stomatogastric neurons. We sought to pharmacologically separate these calcium channel types. We used two different preparations from different regions of stomatogastric neurons to screen a range of selective calcium channel blockers. The two preparations were isolated cell bodies in cultu...

Oxidation of different types of 1,4-dihydropyridines with diphenylpicrylhydrazyl (DPP) and benzoyl peroxide (Bz2O2) as free radical oxidizing agents to pyridine derivatives is reported and a mechanism for this oxidation is also proposed.

An efficient and expeditious catalyst-free procedure was developed for the one- pot synthesis of 1, 4-dihydropyridine derivatives via the three-component reaction of various aldehydes, ethyl acetoacetate, and ammonium acetate in PEG-400. The reaction was carried out at 110°С and the products were obtained in good to high yields.

The four-component Hantzsch reaction provides access to pharmaceutically important dihydropyridines. To expand the utility of this method, we have developed a route under organocatalytic conditions with good yields and excellent ee's. Through catalyst screening, we found that a BINOL-phosphoric acid allowed enantioselective synthesis of six-membered heterocycles with a variety of substitution p...

A metal-free protocol for the synthesis of substituted 1,6-dihydropyridines with quaternary stereogenic centers via a cascade aza-Wittig/6?-electrocyclization process has been developed. The high functional group compatibility and broad scope this method were demonstrated by using wide range easily available vinyliminophosphoranes ketones, yields up to 97%. modification obtained products allowe...