2015
DOI: 10.5155/eurjchem.6.2.163-168.1224
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Abstract: The present study reports a convenient approach for the synthesis of cyanoacetamide based derivatives (7-27) via two-step process involving Knoevenagel reaction, followed by three component reaction to avail desired compounds. All the synthesized compounds were obtained in good to excellent yield and extensively characterized employing 1 H NMR, 13 C NMR, mass spectrometry and physical parameters. Further, these compounds were screened for urease inhibition. All of the synthesized compounds exhibited good to ex… Show more

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Cited by 10 publications
(10 citation statements)
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“…Motivated by broad spectrum of biological and pharmaceutical applications of cyano acetamide derivatives [135] , [136] , [137] , [138] , [139] , [140] , [141] , [142] , [143] , in 2015, Qureshi et al screened several compounds based on this moiety ( Scheme 47 ) to continue determine their urease inhibitory activity [144] and continue previous studies of urease inhibitors [133] , [134] . According to the authors, the high urease inhibitory activity potentially resulted from the extra interaction of the furan and thiophene ring with the urease nickel center.…”
Section: Organic Substances As Urease Inhibitorsmentioning
confidence: 99%
“…Motivated by broad spectrum of biological and pharmaceutical applications of cyano acetamide derivatives [135] , [136] , [137] , [138] , [139] , [140] , [141] , [142] , [143] , in 2015, Qureshi et al screened several compounds based on this moiety ( Scheme 47 ) to continue determine their urease inhibitory activity [144] and continue previous studies of urease inhibitors [133] , [134] . According to the authors, the high urease inhibitory activity potentially resulted from the extra interaction of the furan and thiophene ring with the urease nickel center.…”
Section: Organic Substances As Urease Inhibitorsmentioning
confidence: 99%
“…Due to the flexibility of the enzyme structure and its ability to bind multidisciplinary scaffolds, several natural extracts or synthetic compounds can be designed as inhibitors. In this context, compounds bearing urea or thiourea such as barbiturates and thiobarbiturates [9][10][11], and fragments that mimic urea like iminothiazolines [12], cyanoacetamides [13], and hydrazones [14] have been designed and suggested as inhibitors forJack bean urease enzyme [8][9][10]. Extracts of green tea and cranberries exhibited an inhibition action of urease, and therefore were used to treat gastritis or urinary tract infection [6].…”
Section: Introductionmentioning
confidence: 99%
“…Extracts of green tea and cranberries exhibited an inhibition action of urease, and therefore were used to treat gastritis or urinary tract infection [6]. Some natural flavonoids such as cotton (gossypolone, gossypol, and apogossypol), Pistacia atlantica and Daphne retusa showed the inhibitory potential of Jack beans and Helicobacterpylori (H. pylori) urease [12,13]. On the other hand, a family of aromatic heterocycles compounds previously offered a very interesting effect against urease activity of H. pylori or Jack bean.…”
Section: Introductionmentioning
confidence: 99%
“…Barbiturates and thiobarbiturates have also been extensively studied due to their urea-bearing structure. However, barbituric and thiobarbituric acid analogues are also typically associated with moderate-to-low activity. These molecules were aggregated in cluster 4 (Figure , M.5. ), which showed high median intracluster similarity (0.46) despite the relatively large size ( N = 130), and low percentage of actives (34.6%).…”
Section: Resultsmentioning
confidence: 99%