2009
DOI: 10.1016/j.bmc.2009.02.038
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Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators

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Cited by 57 publications
(35 citation statements)
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“…It is possible that, over the next 5-10 years, we will see patients with not only GCK-PNDM but also T2DM being treated by novel pharmacological agents that activate glucokinase by a similar mechanism to the mutations that result in GCK-HH. The identification of several classes of small molecule glucokinase activators (GKAs) that bind to the GCK allosteric activator site has drawn considerable recent interest [Bertram et al, 2008;Efanov et al, 2005;Grimsby et al, 2008;Iino et al, 2009;McKerrecher et al, 2006] and at least one GCK-targeted activator is undergoing Phase I clinical trials as a diabetes therapy [Grimsby et al, 2003;Guertin and Grimsby, 2006;McKerrecher et al, 2006]. A recent review has been published outlining the scientific basis and developmental progress of various GKAs [Matschinsky, 2009].…”
Section: Future Prospectsmentioning
confidence: 98%
“…It is possible that, over the next 5-10 years, we will see patients with not only GCK-PNDM but also T2DM being treated by novel pharmacological agents that activate glucokinase by a similar mechanism to the mutations that result in GCK-HH. The identification of several classes of small molecule glucokinase activators (GKAs) that bind to the GCK allosteric activator site has drawn considerable recent interest [Bertram et al, 2008;Efanov et al, 2005;Grimsby et al, 2008;Iino et al, 2009;McKerrecher et al, 2006] and at least one GCK-targeted activator is undergoing Phase I clinical trials as a diabetes therapy [Grimsby et al, 2003;Guertin and Grimsby, 2006;McKerrecher et al, 2006]. A recent review has been published outlining the scientific basis and developmental progress of various GKAs [Matschinsky, 2009].…”
Section: Future Prospectsmentioning
confidence: 98%
“…The GKA activity (EC 50 in lM) data of 3-alkoxy-5-phenoxy-N-thiazolyl benzamide analogs were taken from the reported work of Iino et al (2009) (Table 1). In attempting QSAR, these EC 50 data were converted to negative logarithmic dose in moles (pEC 50 ) because QSAR is a linear free energy relationship, and from the van't Hoff isotherm, free energy change during a process is proportional to the logarithm of the rate or equilibrium constant of the process.…”
Section: Methodsmentioning
confidence: 99%
“…The study was performed on a series of 3-alkoxy-5-phenoxy-N-thiazolyl benzamides analogs (Iino et al, 2009). The emphasis was focused on the quantification of structure activity relationship with a view to delineate the influence of key GKAs activity, which will aid in the designing of potent and safer drugs.…”
Section: Introductionmentioning
confidence: 99%
“…Thiazole derivatives display a wide range of biological activities such as antimicrobial, anticancer and antidiabetic agents …”
Section: Introductionmentioning
confidence: 99%