Search

The present work describes an efficient and environmentally benign four component synthesis of structurally diverse substituted pyrido-pyrimidines involving the reaction of barbituric acid, 4-hydroxy 6-methyl 2-pyrone, an aromatic aldehyde and ammonium acetate in low transition temperature mixture (LTTM) (glycerol:proline: 1:1). The LTTM serves as green solvent which is an inexpensive, nontoxic and plays a dual function (reusable catalyst and solvent), and is found to be an excellent reaction endorsing medium. The present protocol offers some advantages such as easy work up, shorter reaction time, an excellent yield with higher atom economy, maximum reaction efficiency with an excellent green chemistry metrics. The synthesized compounds have been evaluated for their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay as well as molecular docking studies performed on myeloperoxidase enzyme. Tested scaffolds exhibits an excellent results of virtual screening and antioxidant activity. [ABSTRACT FROM AUTHOR]

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 H37RV strain using Microplate Alamar Blue Assay method. Together, biological activity data and docking data showed that the tested scaffolds exhibited excellent antituberculotic activity. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

A highly competent-diversity oriented synthesis of coumarin core derivatives using a Knoevenagel condensation followed by Michael addition and subsequent cyclization in the presence of (±)-camphor-10-sulfonic acid in a water/ethanol (1:1) solvent system is depicted. Furthermore, easy workup procedures with good yield, rapid reactions with high atom economy, and catalyst recyclability are the fascinating features of the procedure. [ABSTRACT FROM AUTHOR]