Thermal/Microwave Assisted Synthesis of Substituted Tetrahydropyrimidines as Potent Calcium Channel Blockers.

Abstract

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Kinetic Cell-Based Morphological Screening: Prediction of Mechanism of Compound Action and Off-Target Effects

“…This observation indicated the calcium modulator-like response maybe an off-target effect or additional mechanism of monastrol, rather than relating to inhibition of Eg5. Searching the literature using the chemical name for the core structure of monastrol, 6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate yielded at least one reference indicating compounds resembling monastrol contain calcium channel antagonistic activity (Kumar et al, 2002). We sought to test the possibility that monastrol treatment may modulate the activity of voltage-gated L-type calcium channels.…”

Chemistry and application of 4‐oxo‐4H‐1‐benzopyran‐3‐carboxaldehyde

“…A 1,4-nucleophilic addition of urea or thiourea to the exocyclic , -unsaturated carbonyl group of the condensate ChrCH= C(COMe)COR followed by cyclization gives the Biginelli product [111]. 3-Formyl-6-methylchromone [112] and 6-formylkhellin [113] have been condensed with ethyl acetoacetate and urea in the presence of piperidine to give the appropriate 6-substituted tetrahydropyrimidine. A dry slurry of 1, ethyl acetoacetate, urea and In(OTf) 3 with sodium sulfate as the solid support has been heated under microwave irradiation to give 121 (R = OEt) [114].…”

One‐Pot Sequential Synthesis of 2‐Amino‐4, 6‐Diaryl Pyrimidines Involving SO3H‐Functionalized Piperazinium‐Based Dicationic Ionic Liquids as Homogeneous Catalysts

“…Pyrimidine derivatives are integral component of nucleic acids in the form of nucleobases such as thymine, uracil and cytosine . They possess wide range of pharmacological activities including antibacterial, antifungal, anti‐inflammatory, analgesic, antiviral, antidiabetic, anticonvulsant, antioxidant, anticancer, calcium channel blockers and central nervous system (CNS) depressant properties . A significant numbers of drug molecules used for treatment of several disorders are mono, di‐, tri‐ and tetra‐ substituted pyrimidine derivatives (Figure ).…”