Dihydropyrimidinones Scaffold as a Promising Nucleus for Synthetic Profile and Various Therapeutic Targets: A Review
Authors:
- 1 May 2021
- journal article
- review article
- Published by Bentham Science Publishers Ltd. in Current Organic Synthesis
- Vol. 18 (3) , 270-293
Abstract
Background: This review elaborates the updated synthetic and pharmacological approaches of a known group of dihydropyrimidinones/thiones from the multi-component reaction like Biginelli reaction, which was named Pietro Biginelli in 1891. This review consists of the reaction of an aromatic aldehyde, urea and ethyl acetoacetate leading to dihydropyrimidinone/thione. Currently, the scientific movement to develop economically viable green methods using compounds that are reusable, non-volatile, easily obtained, etc. Objective: This review covers the recent synthesis and pharmacological advancement of dihydropyrimidinones/ thiones moiety, along with covering the structure-activity relationship of the most potent compounds, which may prove to become better, more efficacious and safer agents. Thus, this review may help the researchers in drug designing and development of new Dihydropyrimidinones entities. Conclusion: This review focuses on the wide application of dihydropyrimidinone/thione review reports the design, synthesis and pharmacological activities of nitrogen-sulphur containing dihydropyrimidinone moiety by using multi-component reaction. Dihydropyrimidinones (DHPM) pharmacophore is an important heterocyclic ring in medicinal chemistry. It is derived from multi-component reactions, “Biginelli reaction” and plays a critical role as anticancer, antioxidant, antimicrobial, anti-inflammatory, anti-HIV-1, antimalarial, anti-inflammatory, antihypertensive and anti-tubercular agents. Exhaustive research has led to its vast biological profile, with a wide range of therapeutic application.Keywords
This publication has 119 references indexed in Scilit:
- Three-component synthesis of pyrano[2,3-d]-pyrimidine dione derivatives facilitated by sulfonic acid nanoporous silica (SBA-Pr-SO3H) and their docking and urease inhibitory activityDARU Journal of Pharmaceutical Sciences, 2013
- Monastrol mimic Biginelli dihydropyrimidinone derivatives: synthesis, cytotoxicity screening against HepG2 and HeLa cell lines and molecular modeling studyOrganic and Medicinal Chemistry Letters, 2012
- Directionality of individual kinesin‐5 Cin8 motors is modulated by loop 8, ionic strength and microtubule geometryThe EMBO Journal, 2011
- Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activityEuropean Journal of Medicinal Chemistry, 2011
- Icilin-evoked behavioral stimulation is attenuated by alpha2-adrenoceptor activationBrain Research, 2011
- Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparumBioorganic & Medicinal Chemistry, 2009
- Enantioselective Synthesis of SNAP-7941: Chiral Dihydropyrimidone Inhibitor of MCH1-RThe Journal of Organic Chemistry, 2008
- Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferationBioorganic & Medicinal Chemistry, 2008
- Anti-obesity effects of small molecule melanin-concentrating hormone receptor1 (MCHR1) antagonistsLife Sciences, 2007
- Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based ScreenScience, 1999