174198-29-9Relevant academic research and scientific papers
URAT1 inhibitor for promoting uric acid excretion
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Paragraph 0112; 0113; 0115, (2018/09/21)
The invention belongs to the field of medicinal chemistry, and in particular relates to a URT1 inhibitor for promoting uric acid excretion, which is a compound represented by the structure of the formula (I) or a pharmaceutically acceptable salt thereof. Experiments show that the compound provided by the invention has excellent inhibitory effect to hURAT1 transport uric acid in HEK293 transfectedcells and has a good application prospect in treatment of hyperuricemia or gout. The formula (I) is shown in the description.
Agonist lead identification for the high affinity niacin receptor GPR109a
Gharbaoui, Tawfik,Skinner, Philip J.,Shin, Young-Jun,Averbuj, Claudia,Jung, Jae-Kyu,Johnson, Benjamin R.,Duong, Tracy,Decaire, Marc,Uy, Jane,Cherrier, Martin C.,Webb, Peter J.,Tamura, Susan Y.,Zou, Ning,Rodriguez, Nathalie,Boatman, P. Douglas,Sage, Carleton R.,Lindstrom, Andrew,Xu, Jerry,Schrader, Thomas O.,Smith, Brian M.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Colletti, Steven L.,Tata, James R.,Semple, Graeme
, p. 4914 - 4919 (2008/02/12)
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.
One-pot synthesis of 3(5)-ethoxycarbonylpyrazoles
Martins,Freitag,Flores,Zanatta
, p. 1491 - 1492 (2007/10/02)
A one-pot synthesis of ethoxycarbonylpyrazoles 2a-e, by the cyclocondensation of β-alkoxyvinyl trichloromethyl ketones 1a-e with hydrazine hydrochloride under mild conditions, is reported. A study using compounds 1a-e with different substituents proved that these are versatile building blocks for the synthesis of pyrazole derivatives, having a 3(5)-ethoxycarbonyl substituent, in good yields (70-91%).
