4‐Aryldihydropyridines, a New Class of Highly Active Calcium Antagonists

Abstract

Dedicated to Professor Herbert Griinewald on the occasion of his 60th birthdayThe aryldihydropyridines first prepared by Hanlzsch almost 100 years ago have recently been found to be highly effective calcium antagonists with suitable pharmacological profiles. An illustrative example is dimethyl-1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)pyridine-3,5-dicarboxylate (Nifedipine) which is already employed therapeutically. This substance lowers the frequency of attack of angina pectoris and reduces blood pressure. The discovery of the therapeutic activity of this class of substances initiated renewed investigation of the Hantzsch condensation and the synthesis of numerous 4-aryldihydropyridines and related compounds. Qualitative and quantitative structure/activity relationships of these substances can be deduced from their biological data.

Investigation of Various Green Chemistry Approaches for the Efficient Synthesis of Dialkyl-1, 4-dihydro-4-(substituted phenyl)-2, 6-dimethylpyridine-3, 5-dicarboxylate

“…MCR's have gained significant importance as a tool for the synthesis of a wide variety of useful compounds, including pharmaceuticals [8][9] . Hantzsch 1,4-dihydropyridine (1,4 DHPs) & its derivatives are the class of nitrogen containing heterocycles having 6 membered ring [10][11] . The DHPs heterocyclic ring is a common feature of variety of bioactive compounds of therapeutic activities [12][13] .…”

Carbon-Based Solid Acid Catalyzed Synthesis of Polyhydroquinoline Derivatives via Hantzsch Reaction Under Solvent-Free Conditions

“…In recent years, much attention has been devoted to the synthesis of polyhydroquinoline compounds due to their diverse therapeutic and pharmacological properties, such as vasodilator, antitumor, bronchodilator, antiartherosclerotic, geroprotective and hepatoprotective activity [1][2][3][4][5][6] . Particularly, 4-aryl-1,4-dihydropyridines are well known as calcium channel blockers and have emerged as one of the most important class of drugs for the treatment of cardiovascular diseases 7 .…”

Green Synthesis and Antihypertensive Activity of Some Mannich Bases of 1, 4 Dihydropyridine Compounds

“…1,4-dihydropyridine is a six membered aromatic ring containing N at 1st postion ,which is saturated at1 and 4 th position are 1,4-DHP. The most feasible position for substitution is 4th which exhibit various activities i.e., as the calcium channel antagonists and the heterocyclic ring is the common feature for various pharmacological activities 7 . These chemical classes of compounds were shown to competitively block Ca 2+ movement through the slow channel and thus alter the cardiac action potential, hence called as slow channel blockers or calcium entry blockers or calcium antagonists.…”