Joseph Pontillo
Overview
Explore the profile of Joseph Pontillo including associated specialties, affiliations and a list of published articles.
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25
Citations
63
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Recent Articles
1.
Chen C, Wu D, Guo Z, Xie Q, Reinhart G, Madan A, et al.
J Med Chem
. 2008 Nov;
51(23):7478-85.
PMID: 19006286
The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonists is described. A major focus of this optimization was to improve the...
2.
Pontillo J, Wu D, Ching B, Hudson S, Genicot M, Gao Y, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(23):6151-5.
PMID: 18954981
The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s<10 nM), selective against the other...
3.
Wu D, Pontillo J, Ching B, Hudson S, Gao Y, Fleck B, et al.
Bioorg Med Chem Lett
. 2008 Jun;
18(14):4224-7.
PMID: 18550369
The design, synthesis, and SAR of a series of ring-constrained norepinephrine reuptake inhibitors are described. A substantially rigid inhibitor with potent functional activity at the transporter (IC(50)=8 nM) was used...
4.
Chen C, Chen Y, Pontillo J, Guo Z, Huang C, Wu D, et al.
Bioorg Med Chem Lett
. 2008 Apr;
18(11):3301-5.
PMID: 18442910
Incorporation of a carboxylic acid into a series of uracil derivatives as hGnRH-R antagonists resulted in a significant reduction of CYP3A4 inhibitory activity. Highly potent hGnRH antagonists with low CYP3A4...
5.
Tran J, Arellano M, Fleck B, Pontillo J, Marinkovic D, Tucci F, et al.
Med Chem
. 2008 Jan;
4(1):67-74.
PMID: 18220971
A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar K(i)...
6.
Tran J, Tucci F, Jiang W, Marinkovic D, Chen C, Arellano M, et al.
Bioorg Med Chem
. 2007 Jun;
15(15):5166-76.
PMID: 17544282
A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good...
7.
Chen C, Tran J, Jiang W, Tucci F, Arellano M, Wen J, et al.
Bioorg Med Chem Lett
. 2006 Jul;
16(18):4800-3.
PMID: 16824757
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain...
8.
Hudson S, Kiankarimi M, Rowbottom M, Vickers T, Wu D, Pontillo J, et al.
Bioorg Med Chem Lett
. 2006 Jul;
16(18):4922-30.
PMID: 16824755
The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at...
9.
Jiang W, Tucci F, Chen C, Arellano M, Tran J, White N, et al.
Bioorg Med Chem Lett
. 2006 Jun;
16(17):4674-8.
PMID: 16777413
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with...
10.
Dyck B, Zhao L, Tamiya J, Pontillo J, Hudson S, Ching B, et al.
Bioorg Med Chem Lett
. 2006 Jun;
16(16):4237-42.
PMID: 16762549
A series of substituted chromones were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor 1. Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats...