Matthew M Zrada
Overview
Explore the profile of Matthew M Zrada including associated specialties, affiliations and a list of published articles.
Author names and details appear as published. Due to indexing inconsistencies, multiple individuals may share a name, and a single author may have variations. MedLuna displays this data as publicly available, without modification or verification
Snapshot
Snapshot
Articles
9
Citations
120
Followers
0
Related Specialties
Related Specialties
Top 10 Co-Authors
Top 10 Co-Authors
Published In
Published In
Affiliations
Affiliations
Soon will be listed here.
Recent Articles
1.
The anesthetized guinea pig: an effective early cardiovascular derisking and lead optimization model
Morissette P, Nishida M, Trepakova E, Imredy J, Lagrutta A, Chaves A, et al.
J Pharmacol Toxicol Methods
. 2013 May;
68(1):137-49.
PMID: 23649000
Introduction: In recent years, the anesthetized guinea pig has been used increasingly to evaluate the cardiovascular effects of drug-candidate molecules during lead optimization prior to conducting longer, more resource intensive...
2.
Bell I, Stump C, Gallicchio S, Staas D, Blair Zartman C, Moore E, et al.
Bioorg Med Chem Lett
. 2012 May;
22(12):3941-5.
PMID: 22607672
Rational modification of the clinically tested CGRP receptor antagonist MK-3207 (3) afforded an analogue with increased unbound fraction in rat plasma and enhanced aqueous solubility, 2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(6S)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridin]-3-yl]acetamide (MK-8825) (6). Compound 6...
3.
Yang Z, Barrow J, Shipe W, Schlegel K, Shu Y, Yang F, et al.
J Med Chem
. 2008 Sep;
51(20):6471-7.
PMID: 18817368
The discovery of a novel series of potent and selective T-type calcium channel antagonists is reported. Initial optimization of high-throughput screening leads afforded a 1,4-substituted piperidine amide 6 with good...
4.
Shipe W, Barrow J, Yang Z, Lindsley C, Yang F, Schlegel K, et al.
J Med Chem
. 2008 Jun;
51(13):3692-5.
PMID: 18540666
The novel T-type antagonist ( S)- 5 has been prepared and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine...
5.
Fisher T, Kim B, Staas D, Lyle T, Young S, Vacca J, et al.
Bioorg Med Chem Lett
. 2007 Oct;
17(23):6511-5.
PMID: 17931865
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 12 is active...
6.
Cox C, Breslin M, Whitman D, Coleman P, Garbaccio R, Fraley M, et al.
Bioorg Med Chem Lett
. 2007 Mar;
17(10):2697-702.
PMID: 17395460
Installation of a C2-aminopropyl side chain to the 2,4-diaryl-2,5-dihydropyrrole series of kinesin spindle protein (KSP) inhibitors results in potent, water soluble compounds, but the aminopropyl group induces susceptibility to cellular...
7.
Egbertson M, Moritz H, Melamed J, Han W, Perlow D, Kuo M, et al.
Bioorg Med Chem Lett
. 2006 Dec;
17(5):1392-8.
PMID: 17194584
A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.
8.
Stauffer K, Williams P, Selnick H, Nantermet P, Newton C, Homnick C, et al.
J Med Chem
. 2005 Apr;
48(7):2282-93.
PMID: 15801822
Optimization of a previously reported thrombin inhibitor, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-trans-4-aminocyclohexylmethylamide (1), by replacing the aminocyclohexyl P1 group provided a new lead structure, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-2-aminomethyl-5-chlorobenzylamide (2), with improved potency (K(i) = 0.49 nM for...
9.
Su D, Markowitz M, Murphy K, Wan B, Zrada M, Harrell C, et al.
Bioorg Med Chem Lett
. 2004 Nov;
14(24):6045-8.
PMID: 15546726
We have developed an efficient and selective radioligand, the [35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in transgenic rats over-expressing the human bradykinin B1 receptor.