Joel Robichaud
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Explore the profile of Joel Robichaud including associated specialties, affiliations and a list of published articles.
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Citations
256
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Recent Articles
1.
Ramtohul Y, Powell D, Leclerc J, Leger S, Oballa R, Black C, et al.
Bioorg Med Chem Lett
. 2011 Aug;
21(19):5692-6.
PMID: 21871798
Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for...
2.
Robichaud J, Fournier J, Gagne S, Gauthier J, Hamel M, Han Y, et al.
Bioorg Med Chem Lett
. 2011 Jun;
21(14):4366-8.
PMID: 21689930
Our series of competitive antagonists against the G-protein coupled receptor P2Y(14) were found to be highly shifted in the presence of serum (>99% protein bound). A binding assay using 2%...
3.
Gauthier J, Belley M, Deschenes D, Fournier J, Gagne S, Gareau Y, et al.
Bioorg Med Chem Lett
. 2011 Apr;
21(10):2836-9.
PMID: 21507640
A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY(14) with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharmacokinetics. Acylglucuronidation was...
4.
Bond E, Beausoleil A, Howell J, Wong A, Robichaud J
J Org Chem
. 2011 Mar;
76(8):2488-93.
PMID: 21391622
While several efficient processes exist to effect the stereoselective creation of carbon-carbon bonds in the α- and β-position of carbonyls, functionalization of the γ-position is much more challenging. We disclose...
5.
Isabel E, Powell D, Black W, Chan C, Crane S, Gordon R, et al.
Bioorg Med Chem Lett
. 2010 Nov;
21(1):479-83.
PMID: 21074991
Potent and orally bioavailable SCD inhibitors built on an azetidinyl pyridazine scaffold were identified. In a one-month gDIO mouse model of obesity, we demonstrated that there was no therapeutic index...
6.
Isabel E, Bateman K, Chauret N, Cromlish W, Desmarais S, Duong L, et al.
Bioorg Med Chem Lett
. 2010 Jan;
20(3):887-92.
PMID: 20061146
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and...
7.
Boyd M, Crane S, Robichaud J, Scheigetz J, Black W, Chauret N, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(3):675-9.
PMID: 19117756
Amino ketone warheads were explored as alternatives to the nitrile group of a potent and selective cathepsin K inhibitor. The resulting compounds were potent and selective inhibitors of cathepsin K...
8.
Robichaud J, Black W, Therien M, Paquet J, Oballa R, Bayly C, et al.
J Med Chem
. 2008 Sep;
51(20):6410-20.
PMID: 18811135
Herein, we report on the identification of nonbasic, potent, and highly selective, nitrile-containing cathepsin K (Cat K) inhibitors that are built on our previously identified cyclohexanecarboxamide core structure. Subsequent to...
9.
Hetu P, Ouellet M, Falgueyret J, Ramachandran C, Robichaud J, Zamboni R, et al.
Arch Biochem Biophys
. 2008 May;
477(1):155-62.
PMID: 18498757
We have characterized the structures of cyclooxygenase-2 (COX-2) and microsomal prostaglandin E(2) synthase-1 (mPGES-1) in intact cells using bifunctional and photo-activatable crosslinking agents. A dimeric complex was detected for COX-2...
10.
Gauthier J, Chauret N, Cromlish W, Desmarais S, Duong L, Falgueyret J, et al.
Bioorg Med Chem Lett
. 2008 Jan;
18(3):923-8.
PMID: 18226527
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2...