Robert M Rzasa
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Explore the profile of Robert M Rzasa including associated specialties, affiliations and a list of published articles.
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14
Citations
107
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Recent Articles
1.
Cushing T, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, et al.
J Med Chem
. 2014 Dec;
58(1):480-511.
PMID: 25469863
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification...
2.
Rzasa R, Frohn M, Andrews K, Chmait S, Chen N, Clarine J, et al.
Bioorg Med Chem
. 2014 Dec;
22(23):6570-6585.
PMID: 25456383
We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors. Structure-activity studies improved the solubility (pH 7.4) and maintained high PDE10A activity compared...
3.
Chen J, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, et al.
Bioorg Med Chem Lett
. 2013 Oct;
23(23):6447-54.
PMID: 24139583
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding known adverse...
4.
Rzasa R, Hu E, Rumfelt S, Chen N, Andrews K, Chmait S, et al.
Bioorg Med Chem Lett
. 2012 Nov;
22(24):7371-5.
PMID: 23149228
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial...
5.
Bryan M, Biswas K, Peterkin T, Rzasa R, Arik L, Lehto S, et al.
Bioorg Med Chem Lett
. 2011 Nov;
22(1):619-22.
PMID: 22088753
A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human...
6.
Reichelt A, Falsey J, Rzasa R, Thiel O, Achmatowicz M, Larsen R, et al.
Org Lett
. 2010 Jan;
12(4):792-5.
PMID: 20099864
An efficient and convenient method for the synthesis of [1,2,4]triazolo[4,3-a]pyridines was exemplified by the synthesis of 20 analogues bearing a variety of substituents at the 3-position. The methodology involves a...
7.
Kaller M, Zhong W, Henley C, Magal E, Nguyen T, Powers D, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6591-4.
PMID: 19864130
Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved...
8.
Herberich B, Cao G, Chakrabarti P, Falsey J, Pettus L, Rzasa R, et al.
J Med Chem
. 2008 Sep;
51(20):6271-9.
PMID: 18817365
Investigations into the structure-activity relationships (SAR) of a series of phthalazine-based inhibitors of p38 are described. These efforts originated from quinazoline 1 and through rational design led to the development...
9.
Pettus L, Xu S, Cao G, Chakrabarti P, Rzasa R, Sham K, et al.
J Med Chem
. 2008 Sep;
51(20):6280-92.
PMID: 18817364
The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic...
10.
Low W, Dang Y, Schneider-Poetsch T, Shi Z, Choi N, Rzasa R, et al.
Methods Enzymol
. 2007 Oct;
431:303-24.
PMID: 17923240
Natural products continue to demonstrate their utility both as therapeutics and as molecular probes for the discovery and mechanistic deconvolution of various cellular processes. However, this utility is dampened by...