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Synthesis of some novel quinazolin-4(3H)-one hybrid molecules as potent urease inhibitors. | LitMetric

Synthesis of some novel quinazolin-4(3H)-one hybrid molecules as potent urease inhibitors.

Arch Pharm (Weinheim)

Faculty of Arts and Sciences, Department of Chemistry, Recep Tayyip Erdogan University, Rize, Turkey.

Published: December 2018

A new series of quinazolinone hybrid molecules containing coumarin, furan, 1,2,4-triazole and 1,2,4-thiadiazole rings was designed, synthesized, and screened for their urease inhibition activities. All newly synthesized compounds showed outstanding urease inhibitory potentials with IC values ranging between 1.26 ± 0.07 and 7.35 ± 0.31 μg/mL. Among the series, coumarin derivatives (10a-d) exhibited the best inhibitory effect against urease in the range of IC  = 1.26 ± 0.07 to 1.82 ± 0.10 μg/mL, when compared to standard urease inhibitors such as acetohydroxamic acid and thiourea (IC  = 21.05 ± 0.96 and 15.08 ± 0.71 μg/mL, respectively). Molecular docking studies were also performed to analyze the binding mode of compound 10b, and supported the experimental results.

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Source
http://dx.doi.org/10.1002/ardp.201800182DOI Listing

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