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An environmental friendly synthetic route has been investigated for the synthesis of quinazolin-8 (4H)-one derivatives in the presence of anthranilic acid as a catalyst. The zwitter ion formed in c...

A simple, efficient and convenient approach has been reported for the synthesis of quinazolines by the condensation of 3-amino, 1,2,4-triazole with dimedone and different aromatic aldehydes in the presence of anthranilic acid as a catalyst through a one-pot reaction. The high yield, at low cost, with no need of chromatographic separation, and the environmentally friendly catalyst are the prominent features of this protocol. The zwitterion of anthranilic acid plays an important role in this one-pot reaction.

A convenient and new method has been developed for the synthesis of highly substituted dihydro-2H-dipyrimido[1,2-a,4,5-d]pyrimidine-2,4(3H)-dione derivatives by one-pot three-component reactions of barbituric acid, aromatic aldehydes and 2-aminopyrimidine in ethanol under reflux condition without the support of any catalyst. The benefits of this protocol are catalyst-free, clean reaction procedure and providing excellent yields, and the use of ethanol as a solvent, which has been measured to be comparatively environmentally benign.

Objective of the present work was to evaluate the anti-inflammatory, ulcerogenicity and cyclooxygenase activity of indenopyrimidine derivatives. Anti-inflammatory activity of the tested compounds is investigated by carrageenan-induced rat paw edema assay. Compounds A1, A6, A7 and A12 exhibit the comparable anti-inflammatory activity (79.33-81.33%) to the standard drug diclofenac sodium (85.33%), while A6, A7, A9, A12 and A14 show better ulcer index than the reference standard diclofenac sodium. To rationalize the anti-inflammatory activity, docking experiments are performed to study the ability of these compounds to bind into the active site of COX-2 enzyme.

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. 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.

An ecofriendly route has been investigated for the synthesis of 4-(4-Nitro-phenyl)-2-phenyl-1,4-dihydro-benzo[4,5]imidazo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester derivatives by one-pot three component condensation of ethyl benzoylacetate, aromatic aldehydes and 2-amino benzimidazole using 260 mol% of citric acid as reaction mediator. Citric acid is an inexpensive, non-toxic and greener medium with smoothly activates the rate of reaction. The synthesized compounds were assessed for in-vitro antimycobacterial activity against Mycobacterium tuberculosis H37RV strain using Microplate Alamar Blue Assay (MABA). The results indicate that, among all the synthesized compound series, P-4 and P-9 compounds illustrate effective activity with MIC 25 µg/ml.

An ecofriendly route has been investigated for the synthesis of 4-(4-nitro-phenyl)-2-phenyl-1,4-dihydro-benzo[4,5]imidazo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester derivatives by one-pot, three-component condensation of ethyl benzoylacetate, aromatic aldehydes, and 2-amino benzimidazole using 260 mol% of citric acid as reaction mediator. Citric acid is an inexpensive, nontoxic, and green medium with smoothly activates the rate of reaction. The synthesized compounds were assessed for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37RV strain using the microplate alamar blue assay (MABA). The results indicate that among all the synthesized compound series, P-4 and P-9 compounds illustrate effective activity with a minimum inhibitory concentration of 25 µg/ml.