1160748-13-9Relevant articles and documents
Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential α-glucosidase inhibitors
Asadi, Mehdi,Asemanipoor, Nafise,Biglar, Mahmood,Faramarzi, Mohammad Ali,Hajimiri, Mir Hamed,Hamedifar, Haleh,Larijani, Bagher,Mahdavi, Mohammad,Mohammadi-Khanaposhtani, Maryam,Moradi, Shahram,Vahidi, Mahbobeh
, (2020)
In this study, a series of benzimidazole-1,2,3-triazole hybrids 8a-n as new α-glucosidase inhibitors were designed and synthesized. In vitro α-glucosidase inhibition activity results indicated that all the synthesized compounds (IC50 values ranging from 25.2 ± 0.9 to 176.5 ± 6.7 μM) exhibited more inhibitory activity in comparison to standard drug acarbose (IC50 = 750.0 ± 12.5 μM). Enzyme kinetic study on the most potent compound 8c revealed that this compound was a competitive inhibitor into α-glucosidase. Moreover, the docking study was performed in order to evaluation of interaction modes of the synthesized compounds in the active site of α-glucosidase and to explain structure-activity relationships of the most potent compounds and their corresponding analogs.
New 4,5-diphenylimidazole-acetamide-1,2,3-triazole hybrids as potent α-glucosidase inhibitors: synthesis, in vitro and in silico enzymatic and toxicity evaluations
Sepehri, Nima,Azizian, Homa,Ghadimi, Reza,Abedinifar, Fahimeh,Mojtabavi, Somayeh,Faramarzi, Mohammad Ali,Moghadamnia, Ali Akbar,Zabihi, Ebrahim,Mohebbi, Gholamhossein,Larijani, Bagher,Hamedifar, Haleh,Mohammadi-Khanaposhtani, Maryam,Mahdavi, Mohammad
, p. 679 - 693 (2021/06/14)
Herein, a new series of 4,5-diphenylimidazole-acetamide-1,2,3-triazole hybrids as potent α-glucosidase inhibitors was designed and synthesized. All the synthesized compounds exhibited excellent inhibition potencies (IC50 values = 55.6–149.2 μM)
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes
Guo, Liangqin,Parker, Dann L.,Zang, Yi,Sweis, Ramzi F.,Liu, Weiguo,Sherer, Edward C.,Buist, Nicole,Terebetski, Jenna,Kelly, Terri,Bugianesi, Randal,Priest, Birgit T.,Dingley, Karen H.,Li, Xiaofang,Mitelman, Stan,Salituro, Gino,Trujillo, Maria E.,Pachanski, Michele,Kirkland, Melissa,Powles, Mary Ann,Eiermann, George J.,Feng, Yue,Shang, Jin,Howard, Andrew D.,Ujjainwalla, Feroze,Sinz, Christopher J.,Debenham, John S.,Edmondson, Scott D.,Nargund, Ravi P.,Hagmann, William K.,Li, Derun
supporting information, p. 1107 - 1111 (2016/12/16)
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound 4 suffered from poor metabolic stability and poor solubility. Lead optimization strategies to improve potency, efficacy, metabolic stability, and solubility are described. This optimization led to compound 20e, which showed significant reduction of glucose excursion in wild-type but not in GPR142 deficient mice in an oral glucose tolerance test (oGTT) study. These studies provide strong evidence that reduction of glucose excursion through treatment with 20e is GPR142-mediated, and GPR142 agonists could be used as a potential treatment for type 2 diabetes.
