Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656 was written by Waring, Michael J.;Clarke, David S.;Fenwick, Mark D.;Godfrey, Linda;Groombridge, Sam D.;Johnstone, Craig;McKerrecher, Darren;Pike, Kurt G.;Rayner, John W.;Robb, Graeme R.;Wilson, Ingrid. And the article was included in MedChemComm in 2012.Safety of 1-Ethyl-1H-pyrazol-3-amine This article mentions the following:
Glucokinase plays a central role in glucose homeostasis and small mol. activators of the glucokinase enzyme have been the subject of significant pharmaceutical research in the quest for agents capable of delivering improved glycemic control. Here we describe our medicinal chem. campaign to improve on our previously described development candidate in this area, AZD1092, focussed on removal of Ames liability and improved permeability characteristics. This work culminated in the superior compound AZD1656 which has progressed to phase 2 clin. trials. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-3-amine (cas: 55361-49-4Safety of 1-Ethyl-1H-pyrazol-3-amine).
1-Ethyl-1H-pyrazol-3-amine (cas: 55361-49-4) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazoles and pyrimidines have diverse biological and pharmacological activities. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Pyrazofurin is important antimicrobial drug and 2-methylpyrimidine-4-ylamine derivatives I and II were found to be effective inhibitors of Escherichia coli PDHc-E1 with antibacterial and antifungal activity.Safety of 1-Ethyl-1H-pyrazol-3-amine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics