Thirty five different 4-aryl-1-substituted 2,6-dimethyl-3, 5-bis-N-[(substituted) carbamoyl] 1,4-dihydropyridines have been prepared from a three component condensation reaction of N-(2-chlorophenyl)-acetoacetamide; an aromatic aldehyde and a primary amine under four different experimental conditions. Except for conventional, all the experimental conditions are simple, eco-friendly, economical,...

Cancer is a leading cause of death worldwide. Despite the availability of several chemotherapeutic drugs, there is still a great need for more efficient agents for a better management of cancer. In this contribution, a series of 11 1,4-dihydropyridines (1,4-DHPs) (4a, 4b and 7a-i) were synthesized and evaluated for their cytotoxic effect against MCF-7, LS180 and MOLT-4 cancer cell lines using M...

Depolarization of NG108-15 (neuroblastoma-glioma) cells causes an increase in 45Ca2+ influx. This effect is blocked by low concentrations of dihydropyridines such as nitrendipine and by other blockers of voltage-sensitive calcium channels such as D-600, diltiazem, and Cd2+. Two other dihydropyridines, BAY K8644 and CGP 28392, have the opposite effect. Low concentrations of these compounds enhan...

1,4-Dihydropyridines (1,4-DHPs) are recognized as one of the most versatile pharmacophores present as central core in many pharmaceuticals. Low yield and harsh reaction conditions prompted the researchers for the development of new environmental- friendly methods for the synthesis of 1,4-DHPs. This review explored the development of various green chemistry approaches using new catalysts develop...

The 2-mono and 2,6-disubstituted methyl-1,4-dihydropyridines were synthesized by reaction of morpholine, thiophenol, 8-hydroxyquinoline, 2-naphthol and 2-mercopto-1-methyl imidazole with the 2-mono bromo and 2,6-dibromo-1,4-dihidropyridines.

Quantum chemical (MNDo)caleulations have beenused toelucidate the molecular properties and structure - activity relationships of dihydropyridine (DHP) type calcium antagonists. There is a good corielation between the net atomic charges on various atoms of the 4 - phenyl ring of dihydropyridines and pharmacological activity. .Also, activity decreases with increasing free rotation of the phen...

Parathyroid cells express Ca2+ -conducting currents that are activated by raising the extracellular Ca2+ concentration ([Ca2+]o). We investigated the sensitivity of these currents to dihydropyridines, the expression of voltage-dependent Ca(2+) channel (VDCC) subunits, and the effects of dihydropyridines on the intracellular free [Ca2+] ([Ca2+]i) and secretion in these cells. Dihydropyridine cha...

We have investigated the mechanisms of blockade of calcium channel current by the dihydropyridines, e.g. nisoldipine, nitrendipine, and nicardipine. Membrane current was recorded in isolated calf Purkinje fibers using a two-microelectrode voltage-clamp technique, and voltage protocols were designed to identify voltage- and use-dependent block by these compounds systematically. Our results show ...