“…[33] Compound 62,w ithouta ny substituent at the N1 position, has excellent inhibitory activity,w hich can be explained by the free NH group in its structure. [35] In 2015, 21 quinazoline derivatives, including compounds 65 and 66,w ere synthesized and proven to be more effective AGIs than acarbose. However,d ocking studies indicateo ther substituents on the benzene ring such as methoxy and chloro groups produce steric hindrance, which prevents binding of these compounds to the enzyme.…”
Section: Other Compoundsmentioning
confidence: 99%
“…However,d ocking studies indicateo ther substituents on the benzene ring such as methoxy and chloro groups produce steric hindrance, which prevents binding of these compounds to the enzyme. [35] In 2015, 21 quinazoline derivatives, including compounds 65 and 66,w ere synthesized and proven to be more effective AGIs than acarbose. [36] Interestingly,ad ocking study shows that their binding mode is quite different from that of acarbose.…”
Over the past few years, the number of people diagnosed with type 2 diabetes has increased owing to an unhealthy diet, a limited amount of exercise, and obesity. The search for novel and efficient antidiabetes agents has become an urgent task for scientists. Among the antidiabetes drugs, α-glucosidase inhibitor drugs have been proven to have many advantages over other drugs, and therefore, a large number of new compounds as α-glucosidase inhibitors has recently been reported. In this review, we summarize these newly found α-glucosidase inhibitors and their structure-activity relationships in antidiabetic studies and provide better structures for α-glucosidase inhibitors or even preclinical candidates. Beyond that, some enlightening strategies for the synthesis of relevant compounds are highlighted.
“…[33] Compound 62,w ithouta ny substituent at the N1 position, has excellent inhibitory activity,w hich can be explained by the free NH group in its structure. [35] In 2015, 21 quinazoline derivatives, including compounds 65 and 66,w ere synthesized and proven to be more effective AGIs than acarbose. However,d ocking studies indicateo ther substituents on the benzene ring such as methoxy and chloro groups produce steric hindrance, which prevents binding of these compounds to the enzyme.…”
Section: Other Compoundsmentioning
confidence: 99%
“…However,d ocking studies indicateo ther substituents on the benzene ring such as methoxy and chloro groups produce steric hindrance, which prevents binding of these compounds to the enzyme. [35] In 2015, 21 quinazoline derivatives, including compounds 65 and 66,w ere synthesized and proven to be more effective AGIs than acarbose. [36] Interestingly,ad ocking study shows that their binding mode is quite different from that of acarbose.…”
Over the past few years, the number of people diagnosed with type 2 diabetes has increased owing to an unhealthy diet, a limited amount of exercise, and obesity. The search for novel and efficient antidiabetes agents has become an urgent task for scientists. Among the antidiabetes drugs, α-glucosidase inhibitor drugs have been proven to have many advantages over other drugs, and therefore, a large number of new compounds as α-glucosidase inhibitors has recently been reported. In this review, we summarize these newly found α-glucosidase inhibitors and their structure-activity relationships in antidiabetic studies and provide better structures for α-glucosidase inhibitors or even preclinical candidates. Beyond that, some enlightening strategies for the synthesis of relevant compounds are highlighted.
“…Some of them show anticancer potency [9,15] or neuroprotective properties [8]. Benzimidazole derivatives are also known as β-glucuronidase [16,17], α-glucosidase [18,19], urease [20], and α-amylase enzymes inhibitors [21]. Molecular modeling studies for 5-aryl-4-(1,3,4-thiadiazol-2-yl)benzene-1,3-diols obtained by us indicated a network of essential bonds between the -OH groups of the benzenediol ring and the residues of amino acid AChE in the active site which results in a significant inhibitory effect against AChE [22,23].…”
In the present study, new 4-(1H-benzimidazol-2-yl)-benzene-1,3-diols, modified in both rings, have been synthesized and their efficacies as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors have been determined.The modified Ellman's spectrophotometric method was applied for the biological evaluation. The compounds showed strong (IC 50 80-90 nM) AChE and moderate (IC 50 5-0.2 µM) BuChE inhibition in vitro. Some compounds were effective toward AChE/BuChE, exhibiting high selectivity ratios versus BuChE, while the other compounds were active against both enzymes. The structure-activity relationships were discussed. The compounds inhibited also in vitro self-induced Aβ(1-42) aggregation and exhibited antioxidant properties. The docking simulations showed that the benzimidazoles under consideration interact mainly with the catalytic site of AChE and mimic the binding mode of tacrine.
“…Our research group has identified many lead scaffolds having antiglycation and α -glucosidase inhibitory activities (Fig. 1 ), as a possible treatment for diabetic management 26 – 31 . Figure 1 Identified representative lead candidates.…”
Current research is based on the identification of novel inhibitors of α-amylase enzyme. For that purpose, new hybrid molecules of hydrazinyl thiazole substituted chromones 5–27 were synthesized by multi-step reaction and fully characterized by various spectroscopic techniques such as EI-MS, HREI-MS, 1H-NMR and 13C-NMR. Stereochemistry of the iminic bond was confirmed by NOESY analysis of a representative molecule. All compounds 5–27 along with their intervening intermediates 1–4, were screened for in vitro α-amylase inhibitory, DPPH and ABTS radical scavenging activities. All compounds showed good inhibition potential in the range of IC50 = 2.186–3.405 µM as compared to standard acarbose having IC50 value of 1.9 ± 0.07 µM. It is worth mentioning that compounds were also demonstrated good DPPH (IC50 = 0.09–2.233 µM) and ABTS (IC50 = 0.584–3.738 µM) radical scavenging activities as compared to standard ascorbic acid having IC50 = 0.33 ± 0.18 µM for DPPH and IC50 = 0.53 ± 0.3 µM for ABTS radical scavenging activities. In addition to that cytotoxicity of the compounds were checked on NIH-3T3 mouse fibroblast cell line and found to be non-toxic. In silico studies were performed to rationalize the binding mode of compounds (ligands) with the active site of α-amylase enzyme.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
