36983-33-2Relevant academic research and scientific papers
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.
Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Shin, Young-Jun,Gharbaoui, Tawfik,Lindstrom, Andrew,Hong, Vu,Tamura, Susan Y.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
, p. 5620 - 5623 (2008/04/02)
A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niacin receptor, GPR109b. A further series of 4-fluoro-5-alkyl pyrazole-3-carboxylic acids were shown to display similar potency. One example from the series was shown to have improved properties in vivo compared to niacin.
Pyrazole derivative
-
, (2008/06/13)
Novel pyrazole derivatives of the formula (I): STR1 wherein R is an alkyl group and D is an alkoxy group, a hydroxyl group, a halogen atom or an amino group which may be substituted, and salts thereof show strong antagonistic actions to angiotensin II, th
Bisphophonic acid derivatives and pharmaceutical compositions containing the same
-
, (2008/06/13)
Novel bisphosphonic acid derivatives, and a bone resorption-inhibitor and an anti-arthritis containing a bisphosphonic acid derivative represented by the formula (I): STR1 wherein R2 represents a hydrogen atom, an alkyl group, etc., R2 represents a hydrogen atom or a lower alkanoyl group, R3, R4, R5 and R6 may be the same or different, each represents a hydrogen atom or lower alkyl group.
A CONVENIENT SYNTHESIS OF γ-OXO-ACRYLATES
Manfredini, S.,Simoni, D.,Zanirato, V.,Casolari, A.
, p. 3997 - 4000 (2007/10/02)
Ethyl 2,4-dioxoalkanoates react chemoselectively with pyrrolidine acetate at the more electrophilic C-2 carbonyl, producing enaminone esters which on reduction with NaCNBH3 followed by pyrrolidine elimination, were transformed into γ-oxo-acrylates.
Asymmetric Synthesis of a β-Ketol Moiety via 3,5-Disubstitute Isoxazoles: Application to (+)-(S)--Gingerol
Giovanni, Baraldi Pier,Fabio, Moroder,Piero, Pollini Gian,Daniele, Simoni,Achille, Barco,Simonetta, Benetti
, p. 2983 - 2988 (2007/10/02)
A new synthesis of (+/-)--gingerol (13), (+)-(S)--gingerol, and (+)-methyl--gingerol (12c) using 3,5-disubstituted isoxazoles as masked β-ketols, is described.Reductive fission of the labile N-O bond of the isoxazoles (8a) and (8b) gave the enami
