The present study describes an alkaline water–ethanol mediated series of combinatorial synthesis of 2-amino-4-phenyl-5-H-indeno­[1,2d]­pyrimidine-5-one derivatives through sequential multicomponent reaction of 1,3indandione, aromatic aldehydes, and guanidine hydrochloride along with their anticancer evaluation. The effect of sequential addition of the components in the configuration of the desired product has been studied by UV–visible absorption spectroscopy. The synthetic method obeys most of the green chemistry principles in regard to high atom economy and greener, nontoxic, and noncarcinogenic solvent system (water–ethanol). The selected synthesized compounds have been screened against the human breast cancer cell line MCF7, human colon cancer cell line HT29, and normal viro monkey cell line, out of which 2-amino-4-(4-meth­oxy­phenyl)-5H-indeno­[1,2-d]­pyrimidin-5-one showed significant potency toward human breast cancer cell line (MCF7).

in Wiley Online Library (wileyonlinelibrary.com).One pot three component reaction of 4-hydroxy-6-methylpyran-2-one, 3-methoxy benzaldehyde, and malononitrile in water using protic ionic liquid as a catalyst at room temperature afforded pyrano[4,3-b]pyran derivatives. Protic ionic liquid has been proved to be an efficient and mild catalyst for the synthesis of pyrano[4,3-b]pyran scaffolds due to their highly polar nature. The notable aspects of protic ionic liquid are easy availability, improved reaction rates, high product yields, simple workup procedure, recyclability, and reusability. Molecules docking studies have been performed on enzyme enoyl-ACP-reductase from Mycobacterium tuberculosis. The molecular docking simulation indicated plausible π-alkyl and alkyl-alkyl interactions between the amino acids and scaffolds. The synthesized derivatives have been evaluated for their in vitro antituberculotic activity against M. tuberculosis H 37 RV strain using Microplate Alamar Blue Assay method. Together, biological activity data and docking data showed that the tested scaffolds exhibited excellent antituberculotic activity.

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A highly competent synthesis of novel 7‐aryl‐10‐thioxo‐7, 10, 11, 12‐tertahydro‐9H‐benzo [H] pyrimido [4, 5‐b] quinoline‐8‐one derivatives has been reported through a Knoevenagel condensation followed by Michael addition and subsequent cyclization using ethanol:acetic acid (8:2 v/v). The mentioned protocol has advantages like high yields, cleaner reactions, operational simplicity, and environment friendliness. Moreover, these compounds were further screened against the plant pathogenic fungi like Colletotrichum truncatum, Ustilago maydis, Trichosporon, Trichothecium sp., Aspergillus oryze, Aspergillus terreus, and Aspergillus niger by agar well method bioassay. The results were elaborated for minimum inhibitory concentration determination using agar dilution method against fungal strains C. truncatum and U. maydis as well as broth dilution method for bacteria species Gram‐positive Bacillus megaterium and Gram‐negative Proteus vulgaris. Most of the tested compounds showed promising results towards the antimicrobial activity.

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A simple methodology has been developed for the synthesis of diverse members of multifunctionalized 4-hydroxy-2-methyl-6-(phenyl)pyrimidine-5-carbonitrile derivatives via multicomponent reaction of aromatic aldehydes, ethyl cyanoacetate, and acetamidine hydrochloride using a quantitative amount of NaOH in dry DMF at 80°C in a single procedural step. The carbon skeleton of synthesized compounds resembles the bacimethrin, an antibiotic active against several yeast and bacteria. The anti-inflammatory activities of all the synthesized compounds were assessed on Wistar rats using diclofenac sodium as a standard reference. The compound AC1, 2, 5, 9, and AC10 showed promising anti-inflammatory activity (80-83 %) in comparison with diclofenac sodium (85 %) in the carrageenan-induced rat paw edema assay, which is the key finding of this article. Graphical Abstract The synthesized 4-hydroxy-2-methyl-6-(phenyl)pyrimidine-5-carbonitrile derivatives shown promising anti-inflammatory activity (80-83 %) in comparison with diclofenac sodium (85 %) in the carrageenan-induced rat paw edema assay.Electronic supplementary material The online version of this article (