Pharmacologic Profile of the Dihydropyrimidine Calcium Channel Blockers SQ 32,547 and SQ 32,946

Grover, Gary J.; Dzwonczyk, Steven; McMullen, Diane M.; Normandin, Diane E.; Parham, Charles S.; Sleph, Paul G.; Moreland, Suzanne

doi:10.1097/00005344-199508000-00015

Cited by 243 publications

(27 citation statements)

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“…2 Particular interest has been devoted to potent orally active antihypertensive DHPMs, such as (R)-SQ 32926 (2) and related derivatives. [3][4][5][6] These substances can be considered as close structural analogs of the well-established and therapeutically used calcium channel blockers of the 1,4-dihydropyridine type (DHPs, e.g. nifedipine, 3; (R)-nilvadipine, 4; Chart 1).…”

mentioning

confidence: 99%

Determination of absolute configuration in 4-aryl-3,4-dihydro-2(1H)-pyrimidones by high performance liquid chromatography and CD spectroscopy

et al. 1999

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confidence: 99%

Determination of absolute configuration in 4-aryl-3,4-dihydro-2(1H)-pyrimidones by high performance liquid chromatography and CD spectroscopy

et al. 1999

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“…DHPMs are also used as orally active antihypertensive agents [10,11] , as α1a adrenoceptor selective antagonists [12] and cyclooxygenase-2 inhibitors [13] . The batzelladine alkaloids A and B are used for the treatment of the epidemic, acquired immune deficiency syndrome (AIDS), which inhibited the binding of human immunodeficiency virus envelope protein gp-120 to human CD4 cells to become potential new leads for AIDS therapy [14] .…”

Section: Research Papermentioning

confidence: 99%

Synthesis and Antimicrobial Activity of Fluorine Containing Pyrazole-clubbed Dihydropyrimidinones

Desai¹,

Vaghani²,

Patel³

et al. 2018

pharmaceutical-sciences

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Desai, et al.: Fluorine Containing Pyrazole-clubbed DihydropyrimidinonesIn the present communication synthesis of pyrazole-containing dihydropyrimidinone motifs (4a-o) and their antimicrobial activity and cytotoxicity were reported. The newly synthesized compounds were characterized using infrared, proton nuclear magnetic resonance, carbon-13 nuclear magnetic resonance and mass spectral techniques. Compounds 4b, 4c, 4f, 4g, 4i and 4j were the most active derivatives identified during antimicrobial activity screening. On the basis of antibacterial activities, it was observed that compounds 4b and 4c exhibited activity against methicillin resistant Staphylococcus aureus with minimum inhibitory concentrations of 12.5 and 6.25 µg/ml, respectively. From structure activity relationship studies, it could be concluded that electron withdrawing groups played a crucial role in enhancing antimicrobial and cytotoxic effects of title compounds. In addition, the results of the cytotoxicity studies indicated that compounds 4b, 4c, 4g and 4j possessed lower levels of cytotoxicity.

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“…The reaction products of the reaction are dihydropyrimidinones (DHPMs), which are energetic therapeutic synthons that show a varied range of biological actions such as antiseptic, antiinflammatory, antiviral, anti-tumor [3][4][5]. A huge number of dihydropyrimidinones derivatives have biological value, e.g., antagonists, antihypertensive agents, significant calcium channel blockers, and neuropeptide antagonists [6][7][8][9][10][11]. The research into structural modification of DHPMs 1 has led to the discovery of pharmacologically active compounds, as represented in the DHPMs scaffold ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Solvent-Free Biginelli Reactions Catalyzed by Hierarchical Zeolite Utilizing a Ball Mill Technique: A Green Sustainable Process

et al. 2017

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Abstract:A sustainable, green one-pot process for the synthesis of dihydropyrimidinones (DHPMs) derivatives by a three-component reaction of β-ketoester derivatives, aldehyde and urea or thiourea over the alkali-treated H-ZSM-5 zeolite under ball-milling was developed. Isolation of the product with ethyl acetate shadowed by vanishing of solvent was applied. The hierachical zeolite catalyst (MFI27_6) showed high yield (86%-96%) of DHPMs in a very short time (10-30 min). The recyclability of the catalyst for the subsequent reactions was examined in four subsequent runs. The catalyst was shown to be robust without a detectable reduction in catalytic activity, and high yields of products showed the efficient protocol of the Biginelli reactions.

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Pharmacologic Profile of the Dihydropyrimidine Calcium Channel Blockers SQ 32,547 and SQ 32,946

Cited by 243 publications

References 0 publications

Determination of absolute configuration in 4-aryl-3,4-dihydro-2(1H)-pyrimidones by high performance liquid chromatography and CD spectroscopy

Determination of absolute configuration in 4-aryl-3,4-dihydro-2(1H)-pyrimidones by high performance liquid chromatography and CD spectroscopy

Synthesis and Antimicrobial Activity of Fluorine Containing Pyrazole-clubbed Dihydropyrimidinones

Solvent-Free Biginelli Reactions Catalyzed by Hierarchical Zeolite Utilizing a Ball Mill Technique: A Green Sustainable Process

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