Microwave-assisted synthesis of antimicrobial dihydropyridines and tetrahydropyrimidin-2-ones: Novel compounds against aspergillosis

Chhillar, Anil Kumar; Arya, Pragya; Mukherjee, Chandrani; Kumar, Pankaj; Yadav, Yogesh; Sharma, Abhay; Yadav, Vipul; Gupta, J. R. P.; Dabur, Rajesh; Jha, Hirday N.; Watterson, Arthur C.; Parmar, Virinder S.; Prasad, Ashok K.; Sharma, Gainda L.

doi:10.1016/j.bmc.2005.09.014

Cited by 87 publications

(55 citation statements)

References 39 publications

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“…This new method provided the expected products 35 in excellent yields (90%-98%) after short reaction times (40-80 s) in comparison to the classical Hantzsch methods (Scheme 7) [44][45][46]. 1,4-Dihydropyridine derivatives have a wide range of biological and pharmaceutical activities and are also involved in hydride transfer from the reduced nicotinamide adenine dinucleotide (NADH and NADPH) coenzymes, and analogues thereof, which mediate hydrogen transfer reactions in biological systems [35][36][37].…”

Section: Pyridines Dihydropyridines Piperidinesmentioning

confidence: 99%

“…In addition, others 1,4-dihydropyridines have been discovered as potent calcium channel agonists (such as BAY K 8644 (31)) [41,42]. 1,4-Dihydropyridine derivatives have a wide range of biological and pharmaceutical activities and are also involved in hydride transfer from the reduced nicotinamide adenine dinucleotide (NADH and NADPH) coenzymes, and analogues thereof, which mediate hydrogen transfer reactions in biological systems [35][36][37].…”

Section: Pyridines Dihydropyridines Piperidinesmentioning

confidence: 99%

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Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

et al. 2016

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This review describes the formation of six-membered heterocyclic compounds and their fused analogues under microwave activation using modern organic transformations including cyclocondensation, cycloaddition, multicomponents and other modular reactions. The review is divided according to the main heterocycle types in order of increasing complexity, starting with heterocyclic systems containing one, two and three heteroatoms and their fused analogues. Recent microwave applications are reviewed, with special focus on the chemistry of bioactive compounds. Selected examples from the 2006 to 2015 literature are discussed.

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Section: Pyridines Dihydropyridines Piperidinesmentioning

confidence: 99%

Section: Pyridines Dihydropyridines Piperidinesmentioning

confidence: 99%

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

et al. 2016

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“…This method [4,11] was performed using the erythrocytes from the healthy humans was taken and rinsed them with autoclaved PBS. Erythrocyte suspension (2.0% v/v) was prepared and exposed with IBU and AmpB starting with concentration of 1000 µg/ml at 37°C for 1 hr.…”

Section: Haemolytic Assaymentioning

confidence: 99%

In Vitro Antimycotic Evaluation and Preliminary Combinatorial Studies of Ibuprofen With Standard Antifungal Drugs Against Aspergillus Spp.

Narwal

Balhara

Chaudhary

et al. 2017

Asian J Pharm Clin Res

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Objective: The prevalence of invasive mycoses is increased in the immunocompromised patients with an increase in resistance developed against current antifungal drugs. This has led to the need for discovering novel combinations of the antifungal drugs to combat against resistant pathogenic spp. This study mainly targets to evaluate the antifungal activity of ibuprofen (IBU) alone and in combination with the standard antifungal drugs (polyenes and azoles) against eight isolates of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus niger. Methods:The study was performed using the disc diffusion assay (DDA), microbroth dilution assay and spore germination inhibition assay. Moreover, cytotoxicity was checked by heamolytic assay.Results: Minimum inhibitory concentration (MIC) of IBU against A. fumigatus and A. flavus using DDA is found to be in the range of 250-275 µg/disc while for A. niger isolates, the range was 500-575 µg/disc. Likewise, by broth microdilution assay and spore germination inhibitory assay, MIC determined, were in the range of 500-750 µg/ml against A. fumigatus and A. flavus while for A. niger, it was 1000-1500 μg/ml. Conclusion:IBU demonstrated its antimycotic potential against all the eight isolates of Aspergillus spp. Moreover, preliminary combinatorial evaluation of IBU with the standard antifungal drugs reported by DDA revealed an increase in zone of inhibition as compared to the drugs alone. Further research regarding the confirmation of synergistic interaction between the selected drugs is in progress.

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“…The dihydropyrimidinones (DHPMs) have exhibited interesting and multifaceted pharmacological properties such as antitumor, anti-inflammatory, antiviral, antifungal and antibacterial activity [1][2][3]. In addition, these compounds have emerged as potential calcium channel blockers, antihypertensive, α 1a -adrenergic antagonists and neuropeptide antagonists [4].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and characterization of functionalized dihydropyrimidinones via one-pot isocyanide-based three-component reaction of N-formyl urea and dialkyl ACETYLENEDICARBOXYLATES

Naderi¹,

Mohtat²

2017

Bull. Chem. Soc. Eth.

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Microwave-assisted synthesis of antimicrobial dihydropyridines and tetrahydropyrimidin-2-ones: Novel compounds against aspergillosis

Cited by 87 publications

References 39 publications

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

In Vitro Antimycotic Evaluation and Preliminary Combinatorial Studies of Ibuprofen With Standard Antifungal Drugs Against Aspergillus Spp.

Synthesis and characterization of functionalized dihydropyrimidinones via one-pot isocyanide-based three-component reaction of N-formyl urea and dialkyl ACETYLENEDICARBOXYLATES

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