2009
DOI: 10.2174/138955709787001686
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Genesis of Dihydropyrimidinone Calcium Channel Blockers: Recent Progress in Structure-Activity Relationships and Other Effects

Abstract: In the armamentarium of calcium channel blockers appropriately functionalized 3,4-dihydropyrimidin-2(1H)-ones have received considerable attention in recent past owing to their structural similarity with 1,4-dihydropyridine based drugs. In this review, we highlight detailed investigations in the calcium channel blocking and other activities of this category of compounds as well as trace their genesis from 1,4-dihydropyridine based drugs.

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Cited by 75 publications
(5 citation statements)
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“…This acid-catalyzed cyclocondensation of urea, β-ketoesters and aromatic aldehydes to yield dihydropyrimidines has received significant attention, these products having pharmacological activity including calcium channel modulation, mitotic kinesin Eg5 inhibition, and antiviral and antibacterial activity [4950]. The Biginelli reaction has been performed in flow previously as a route to densely functionalized heterocycles using HBr generated in a prior step as the catalyst for the reaction [51].…”
Section: Resultsmentioning
confidence: 99%
“…This acid-catalyzed cyclocondensation of urea, β-ketoesters and aromatic aldehydes to yield dihydropyrimidines has received significant attention, these products having pharmacological activity including calcium channel modulation, mitotic kinesin Eg5 inhibition, and antiviral and antibacterial activity [4950]. The Biginelli reaction has been performed in flow previously as a route to densely functionalized heterocycles using HBr generated in a prior step as the catalyst for the reaction [51].…”
Section: Resultsmentioning
confidence: 99%
“…Pyrimidines, which have similar structural skeletons of pyridines, are identified as the vital component of nucleic acid and play an integral role as biologically significant antitumor, antiviral, and cardiovascular agents. Unlike light-sensitive and aromatic 1,4-dihydropyridines, the N-3 substituted DHPMs are shown to possess promising stability [ 38 ]. Analogous to 1,4 dihydropyridines, DHPMs have been shown to have a boat conformation for the modulation of their activity.…”
Section: Dihydropyrimidines As Calcium Channel Blockersmentioning
confidence: 99%
“…At present, the awareness of the Biginelli reaction relies on the announcement of a series of literature about the biological activities of DHPMs. These contain anti-proliferative (Treptow et al, 2015), antimicrobial (Tanay et al, 2015), anti-inflammatory (Bahekar & Shinde, 2004), antioxidant (de Vasconcelos et al, 2012), and calcium channel inhibition (Singh et al, 2009) activities.…”
Section: Introductionmentioning
confidence: 99%