2014
DOI: 10.1016/j.bmcl.2014.07.025
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Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

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Cited by 62 publications
(17 citation statements)
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“…Inhibition of the glucagon receptor using small-molecule ligands may be a promising method to improve glucose and clinical data using small-molecule antagonists is emerging. 28 …”
Section: Glucagon Receptor Antagonistsmentioning
confidence: 99%
“…Inhibition of the glucagon receptor using small-molecule ligands may be a promising method to improve glucose and clinical data using small-molecule antagonists is emerging. 28 …”
Section: Glucagon Receptor Antagonistsmentioning
confidence: 99%
“…In addition to the effects of eliminating glucagon signalling by knocking out the glucagon receptor mentioned above, animal studies have shown that experimental diabetes is markedly improved by immunoneutralization of glucagon by specific glucagon antibodies [63], by the use of antisense oligonucleotides targeting hepatic glucagon expression [64] or by monoclonal glucagon receptor antibodies [30]. Numerous peptide [65][66][67] and non-peptide glucagon receptor antagonists have been developed, including substituted ureas [68], benzamidine derivatives [69], alkylidene hydrazides [70][71][72], -alanine derivatives [73] and furan-2-carbohyrazides [74], and have been shown to reduce blood glucose in dogs and monkeys, as well as in non-diabetic and diabetic rodents and, for one compound, in humans [75]. Kelly et al [76] recently reported that short-term oral administration of the small-molecule glucagon receptor antagonist LY2409021 results in substantial reduction of fasting and postprandial glucose, with minimal hypoglycaemia, but reversible dose-dependent increases in aminotransferases, indicating that longer clinical trials are requested to better evaluate benefits and risks.…”
Section: Search For Selective Glucagon Antagonistsmentioning
confidence: 99%
“…6 Furan-amidine series acts as inhibitors of the enzyme quinone oxidoreductase-2, 7 some furonaphthoquinones shows anti-cancer activity, 8 cyclopenta[b]furans acts as inhibitors of CCR-2 as it is a Gprotein coupled receptor of the chemokinine family 9 and some furan-2-carbohydrazides acts as glucagon receptor antagonists. 10 Some derivatives comprising thiophene and sulfur containing groups attatched with different groups showed as variety of biological activities. [11][12][13] Some natural products with benzofuran scaffold display a variety of biological activities like anti-inflammatory, antibacterial, antitumor, antitubercular activities.…”
Section: Introductionmentioning
confidence: 99%