Bioactivity of dihydropyrimidinone derivatives as inhibitors of cyclooxygenase-2 (COX-2): an <i>in silico</i> approach

Haq, Kautsar Ul; Sa'adah, Nur Lailatus; Siswanto, Imam; Suwito, Hery

doi:10.1039/d3ra05942a

Cited by 2 publications

(1 citation statement)

References 51 publications

(58 reference statements)

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“…The major reason for the profound activity of DHMPs is due to the presence of pyrimidine nucleus which is an essential fragment of nucleic acid. DHMP scaffolds exhibit a wide array of activities, encompassing “anti‐inflammatory, anti‐HIV, antitubercular, antifungal, anticancer, antibacterial, 19 antihyperglycemic, antihypertensive, anticonvulsant, antimalarial, RT inhibitor, antioxidant, antispasmodic, calcium channel blocker (CCB), antiproliferative, urease inhibition, cyclooxygenase (COX‐2) inhibition, 20 and β‐glucuronidase inhibition properties.” The review is focused on DHMPs and incorporates literature of the last two decades.…”

Section: Introductionmentioning

confidence: 99%

Medicinal perspective of a promising scaffold – dihydropyrimidinones: A review

Sarvaiya,

Vaja,

Paghdar

et al. 2024

Journal of Heterocyclic Chem

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Dihydropyrimidinones (DHMPs) are the most important pharmacophore in Medicinal Chemistry. The synthetic approach for deriving DHMPs involves the Biginelli reaction or a combination of it with other multi‐component reactions (MCRs). The scaffold has received considerable attention due to its diverse therapeutic activity. This review delves into the exploration of the biological characteristics of DHMPs, which play a pivotal role in various therapeutic areas including “anti‐inflammatory, anti‐HIV, anticancer, antitubercular, antifungal, antibacterial, antihyperglycemic, antihypertensive, anticonvulsant, antimalarial, antioxidant,” reverse transcriptase (RT) inhibitor, antispasmodic, calcium channel blockers, antiproliferative, urease inhibitor, cyclooxygenase (COX‐2), and β‐glucuronidase inhibitor activities. The insights provided in this review have the potential to aid researchers in the formulation of novel drugs, facilitating creation of more resilient, efficient, and safer therapeutic agents with reduced toxicity and minimized adverse effects.

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Section: Introductionmentioning

confidence: 99%

Medicinal perspective of a promising scaffold – dihydropyrimidinones: A review

Sarvaiya,

Vaja,

Paghdar

et al. 2024

Journal of Heterocyclic Chem

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Novel Cholesterol-Based Dihydropyrimidinone Derivatives with Potential Biological Activities: An In-silico Investigation

Bendi,

Kaur,

Chinmay

et al. 2024

J. Comput. Biophys. Chem.

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Steroids play essential physiological roles in the living systems, including their role as sex hormones, glucocorticoids, and mineralocorticoids. Usually, they engage in interactions with steroid receptors. Target cell nuclei, cytosol and plasma membranes all have steroid hormone receptors. Cytoplasmic or nuclear, intracellular receptors start the signal transduction process for steroid hormones and cause gene expression alterations over the course of several hours to days. Certain steroid hormones bind to cell surface receptors, including ion channels, G protein-coupled receptors and several nuclear receptors. Dihydropyrimidinones are also significant moieties with important physiological roles. The hybrid molecules can offer several potential biological activities. In this work, we have checked the in silico interaction of some novel cholesterol–dihydropyrimidinones interactions with the sex hormones, mineralocorticoid and glucocorticoid receptors to screen their potential use in the regulation of the sexual cycle or the carbohydrate metabolism or the mineral imbalance.

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Bioactivity of dihydropyrimidinone derivatives as inhibitors of cyclooxygenase-2 (COX-2): an in silico approach

Abstract: Hundreds of dihydropyrimidinone derivatives were virtually screened to find novel COX-2-selective inhibitor candidates.

Cited by 2 publications

References 51 publications

Medicinal perspective of a promising scaffold – dihydropyrimidinones: A review

Medicinal perspective of a promising scaffold – dihydropyrimidinones: A review

Novel Cholesterol-Based Dihydropyrimidinone Derivatives with Potential Biological Activities: An In-silico Investigation

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