The synthesis and anti-inflammatory evaluation of 1,2,3-triazole linked isoflavone benzodiazepine hybrids

Mengheres, Gabriel; Olajide, Olumayokun A.; Hemming, K.

doi:10.24820/ark.5550190.p011.396

Cited by 7 publications

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“…Mengheres et al (2020) reported the synthesis and anti-inflammatory activity of eight isoflavone-benzodiazepine hybrids ( 75a – 75h , Figure 26 ) obtained through the Click Chemistry approach from propargylated benzodiazepines and isoflavone azides [ 115 ]. All compounds were found to decrease in vitro the NO production on lipopolysaccharide (LPS)-stimulated BV2 mouse brain microglial cells, with 18.06–64.28% NO production at 20 µM, whereas natural isoflavones daidzein and formononetin showed 34.94% and 72.70% NO production, respectively, at the same concentration.…”

Section: Other Activitiesmentioning

confidence: 99%

“…All compounds were found to decrease in vitro the NO production on lipopolysaccharide (LPS)-stimulated BV2 mouse brain microglial cells, with 18.06–64.28% NO production at 20 µM, whereas natural isoflavones daidzein and formononetin showed 34.94% and 72.70% NO production, respectively, at the same concentration. Among them, compounds 75g (19.99% NO production and 66.35% cell viability) and 75h (19.88% NO production and 60.24% cell viability), having the same benzodiazepine scaffold, showed reasonable cell viability (>60%) and significant inhibition of NO production, being selected as the most promising compounds of this study [ 115 ].…”

Section: Other Activitiesmentioning

confidence: 99%

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Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry

et al. 2021

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As a result of the biological activities of natural flavonoids, several synthetic strategies aiming to obtain analogues with improved potency and/or pharmacokinetic profile have been developed. Since the triazole ring has been associated with several biological activities and metabolic stability, hybridization with a 1,2,3-triazole ring has been increasingly reported over the last years. The feasible synthesis through copper (I) catalyzed azide-alkyne cycloaddition (CuAAC) has allowed the accomplishment of several hybrids. Since 2017, almost 700 flavonoid hybrids conjugated with 1,2,3-triazole, including chalcones, flavones, flavanones and flavonols, among others, with antitumor, antimicrobial, antidiabetic, neuroprotective, anti-inflammatory, antioxidant, and antifouling activity have been reported. This review compiles the biological activities recently described for these hybrids, highlighting the mechanism of action and structure–activity relationship (SAR) studies.

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Section: Other Activitiesmentioning

confidence: 99%

Section: Other Activitiesmentioning

confidence: 99%