Philip D Stein
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Explore the profile of Philip D Stein including associated specialties, affiliations and a list of published articles.
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186
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Recent Articles
1.
Letourneau J, Stroke I, Hilbert D, Cole A, Sturzenbecker L, Marinelli B, et al.
Bioorg Med Chem Lett
. 2018 Nov;
28(23-24):3601-3605.
PMID: 30392779
Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess...
2.
Stroke I, Letourneau J, Miller T, Xu Y, Pechik I, Savoly D, et al.
Antimicrob Agents Chemother
. 2018 Feb;
62(5).
PMID: 29483125
infection (CDI) is the leading cause of hospital-acquired infectious diarrhea, with significant morbidity, mortality, and associated health care costs. The major risk factor for CDI is antimicrobial therapy, which disrupts...
3.
Letourneau J, Stroke I, Hilbert D, Sturzenbecker L, Marinelli B, Quintero J, et al.
Bioorg Med Chem Lett
. 2018 Jan;
28(4):756-761.
PMID: 29331267
The discovery, synthesis and preliminary structure-activity relationship (SAR) of a novel class of inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB) is described. A high throughput screening (HTS) campaign...
4.
Jimenez-Diaz M, Ebert D, Salinas Y, Pradhan A, Lehane A, Myrand-Lapierre M, et al.
Proc Natl Acad Sci U S A
. 2014 Dec;
111(50):E5455-62.
PMID: 25453091
Drug discovery for malaria has been transformed in the last 5 years by the discovery of many new lead compounds identified by phenotypic screening. The process of developing these compounds...
5.
Zhao G, Kwon C, Bisaha S, Stein P, Rossi K, Cao X, et al.
Bioorg Med Chem Lett
. 2013 May;
23(13):3914-9.
PMID: 23683593
The 5-HT2C receptor has been implicated as a critical regulator of appetite. Small molecule activation of the 5-HT2C receptor has been shown to affect food intake and regulate body weight...
6.
Shi Y, OConnor S, Sitkoff D, Zhang J, Shi M, Bisaha S, et al.
Bioorg Med Chem Lett
. 2011 Nov;
21(24):7516-21.
PMID: 22041058
The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The arylsulfonamide-valerolactam scaffold was derived based on the proposed bioisosterism...
7.
Shi Y, Li C, OConnor S, Zhang J, Shi M, Bisaha S, et al.
Bioorg Med Chem Lett
. 2009 Nov;
19(24):6882-9.
PMID: 19896847
We report the design and synthesis of a novel class of N,N'-disubstituted aroylguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The structure-activity relationships (SAR) investigation led to the...
8.
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors
Shi Y, Zhang J, Shi M, OConnor S, Bisaha S, Li C, et al.
Bioorg Med Chem Lett
. 2009 Jun;
19(15):4034-41.
PMID: 19541481
The N,N'-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a novel class of cyanoguanidine-based lactam derivatives as...
9.
Shi Y, Sitkoff D, Zhang J, Klei H, Kish K, Liu E, et al.
J Med Chem
. 2008 Nov;
51(23):7541-51.
PMID: 18998662
An indole-based P1 moiety was incorporated into a previously established factor Xa inhibitor series. The indole group was designed to hydrogen-bond with the carbonyl of Gly218, while its 3-methyl or...
10.
OConnor S, Atwal K, Li C, Liu E, Seiler S, Shi M, et al.
Bioorg Med Chem Lett
. 2008 Jul;
18(16):4696-9.
PMID: 18644722
A series of acylguanidine derivatives were prepared and investigated as inhibitors of Factor Xa (FXa). These compounds were made by guanidine acylation with carboxylic acids using carbonyl diimidazole (CDI) as...