In this paper we present the room temperature synthesis of a novel serie of 1,4-disubstituted-1,2,3-triazoles 4a-l by employing the (3 + 2) cycloaddition reaction of pyrimidinones containing alkyne functions with different model azides in the presence of
Fethi Zribi +5 more
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Analyzing binary heterocyclic pyrimidinones using density functional theory (DFT) calculations and Monte Carlo (MC) simulations, as well as assessing their ADME (Absorption, Distribution, Metabolism, and Excretion) and toxicological properties is the ...
Ahmed M. Wahba +2 more
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Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17b-Hydroxysteroid Dehydrogenase Type 2 (17b-HSD2) Inhibitors [PDF]
In this study, a series of conformationally restricted thieno[3,2-d]pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones was designed and synthesized with the goal of improving the biological activity as 17b-hydroxysteroid dehydrogenase type 2 ...
Rolf W. Hartmann +2 more
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Continuous-flow retro-Diels–Alder reaction: an efficient method for the preparation of pyrimidinone derivatives [PDF]
The syntheses of various pyrimidinones as potentially bioactive products by means of the highly controlled continuous-flow retro-Diels–Alder reaction of condensed pyrimidinone derivatives are presented.
Imane Nekkaa +3 more
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Mesoporous molecular sieve MCM-41 catalyzed one-pot synthesis of 3,4-dihydro-2(1H)-pyrimidinones and –thiones under solvent-free conditions [PDF]
An efficient synthesis of 3,4-dihydro-2(1H)-pyrimidinones and -thiones using MCM-41 as the catalyst from an aldehyde, β-keto ester, and urea or thiourea under solvent-free conditions is described.
Rahim Hekmatshoar +3 more
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CoMFA and CoMSIA Studies on Inhibitors of HIV-1 Integrase - Bicyclic Pyrimidinones [PDF]
To understand the structural requirements of HIV-1 integrase inhibitors and to design new ligands against human HIV-1 integrase with enhanced inhibitory potency, a 3D QSAR (quantitative structure-activity relationship) study with comparative molecular ...
V. Radhika, S. Sree Kanth, M. Vijjulatha
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A green method for the synthesis of isoxazolyl aryl thieno[2,3-d]pyrimidinones using reusable polyethylene glycol as simple solvent catalyst and evaluation of anti-microbial activity [PDF]
Novel series of isoxazolyl aryl thieno[2,3-d]pyrimidinones 4 have been synthesized from (E)-2-amino-5-(3-methyl-4-nitroisoxazol-5-yl)-N-(3-methyl-5-styrylisoxazol-4-yl)-4-arylthiophene-3-carboxamide synthon 3.
Saini, Ramakrishna ; Department of Chemistry, Kakatiya University, Warangal 506 009, India +2 more
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Alteration of insect growth regulators by the action of inhibitors is becoming an attractive strategy to combat disease-transmitting insects. In the present study, we investigated the larvicidal effect of 1,2,3-triazolyl-pyrimidinone derivatives against ...
Katharigatta N. Venugopala +16 more
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BACKGROUND Malaria is responsible for 429,000 deaths per year worldwide, and more than 200 million cases were reported in 2015. Increasing parasite resistance has imposed restrictions to the currently available antimalarial drugs.
Kamilla Rodrigues Rogerio +9 more
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Five-Membered Heterocyclic Ring Via Dichalcones [PDF]
In this study some of dichalcone compounds (4-12) were prepared by the reaction of benzalacetone and its derivatives with a number of different ketones (acetophenone, acetanilide, 2-butanone).
N. Ahmad, O Ali
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