Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors

Bioactive compounds ofCrocus sativusL. and their semi-synthetic derivatives as promising anti-Helicobacter pylori, anti-malarial and anti-leishmanial agents

“…Starting from this point, we assessed the anti-H. pylori, anti-malarial and anti-leishmanial effects of two natural products found in C. sativus L., crocin (1) and safranal (2), and of the semi-synthetic safranal derivatives (3)(4)(5)(6)(7)(8)(9). The thiosemicarbazonic derivatives 4 and 5 and the (thiazol-2-yl)hydrazonic compound 9 exhibited the best anti-H. pylori activities and a possible mechanism of action, corroborated by molecular modeling studies, might be the inhibition of several targets as FabZ and HpPDF.…”

“…One of the reasons for the failure of H. pylori eradication in many countries is the increasing antibiotic resistance 1 . Among the new strategies for the treatment of H. pylori infection, it can be mentioned the inhibition of urease 2,3 , an enzyme that permits the survival of H. pylori in the harsh acidic environment of the stomach and its colonization of the gastric mucosa, by neutralization of the gastric acidity thanks to the ammonia production from host urea. Several natural and synthetic compounds such as sulforaphane, an isothiocyanate extracted from crucifers 4 , allyl isothiocyanates 5 , flavonoids and their corresponding reductive derivatives 6 , quercetin and its analogues 7 and some synthetic thiosemicarbazones 3 are effective urease inhibitors.…”

“…Among the new strategies for the treatment of H. pylori infection, it can be mentioned the inhibition of urease 2,3 , an enzyme that permits the survival of H. pylori in the harsh acidic environment of the stomach and its colonization of the gastric mucosa, by neutralization of the gastric acidity thanks to the ammonia production from host urea. Several natural and synthetic compounds such as sulforaphane, an isothiocyanate extracted from crucifers 4 , allyl isothiocyanates 5 , flavonoids and their corresponding reductive derivatives 6 , quercetin and its analogues 7 and some synthetic thiosemicarbazones 3 are effective urease inhibitors. Instead, caffeic acid phenethyl ester, one of the principal components of propolis, was found to be a competitive inhibitor of H. pylori peptide deformylase (HpPDF), an enzyme that catalyzes the removal of the formyl group from the N-terminus of nascent polypeptide chains, which is essential for H. pylori survival 8 .…”

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

“…All the compounds were screened at different sites (A & B) of the enzyme. The nickel-containing catalytic site A is the most commonly tested site in the literature [26], while site B is less commonly targeted [20,27]. Our compounds bind more strongly to Site B than to site A.…”

Synthesis, Crystal Structures and Urease Inhibition of N’-(2-Bromobenzylidene)-2-(4-nitrophenoxy) acetohydrazide and N’-(4-Nitrobenzylidene) -2-(4-nitrophenoxy)acetohydrazide

“…Aslam and co-workers reported that hydrazone compounds derived from thiosemicarbazide possess urease inhibitory activities. 3 Recently, our research group has reported some urease inhibitors with various types of organic compounds or metal complexes 4 and some metal complexes derived from hydrazone ligands.…”