J Wityak
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Explore the profile of J Wityak including associated specialties, affiliations and a list of published articles.
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11
Citations
198
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Recent Articles
1.
Sielecki T, Wityak J, Liu J, Mousa S, Thoolen M, Wexler R, et al.
Bioorg Med Chem Lett
. 2000 Apr;
10(5):449-52.
PMID: 10743945
A series of ring constrained analogues of the GPIIb/IIIa receptor antagonist XR299 (1) was investigated as potential inhibitors of glycoprotein IIb/IIIa, a platelet receptor that plays a key role in...
2.
PITTS W, Wityak J, Smallheer J, Tobin A, Jetter J, Buynitsky J, et al.
J Med Chem
. 2000 Jan;
43(1):27-40.
PMID: 10633036
Starting with lead compound 2, we sought to increase the selectivity for alpha(v)beta(3)-mediated cell adhesion by examining the effects of structural changes in both the guanidine mimetic and the substituent...
3.
Olson R, Sielecki T, Wityak J, Pinto D, Batt D, Frietze W, et al.
J Med Chem
. 1999 Apr;
42(7):1178-92.
PMID: 10197962
Modification of the alpha-carbamate substituent of isoxazoline GPIIb/IIIa (alphaIIb beta3) antagonist DMP 754 (7) led to a series of alpha-sulfonamide and alpha-sulfamide diaminopropionate isoxazolinylacetamides which were found to be potent...
4.
Wityak J, Tobin A, Mousa S, Wexler R, Olson R
Bioorg Med Chem Lett
. 1999 Feb;
9(2):123-6.
PMID: 10021912
Isoxazolinylacetamides bearing a phosphoramidate group alpha- to the carboxylate moiety (3) were prepared and evaluated for in vitro antiplatelet efficacy. They were found to bind GPIIb/IIIa with high affinity and...
5.
Duncia J, Santella 3rd J, Higley C, PITTS W, Wityak J, Frietze W, et al.
Bioorg Med Chem Lett
. 1999 Jan;
8(20):2839-44.
PMID: 9873633
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with...
6.
Mousa S, Forsythe M, Bozarth J, Youssef A, Wityak J, Olson R, et al.
J Cardiovasc Pharmacol
. 1998 Nov;
32(5):736-44.
PMID: 9821847
XV454 demonstrated high potency (IC50 = 14-25 nM) in inhibiting human platelet aggregation induced by adenosine diphosphate (ADP, 10 microM), thrombin receptor agonist peptide (TRAP) (10 microM), or collagen (20...
7.
Mousa S, Olson R, Bozarth J, Lorelli W, Forsythe M, Racanelli A, et al.
J Cardiovasc Pharmacol
. 1998 Aug;
32(2):169-76.
PMID: 9700976
This study was undertaken to define the platelet glycoprotein alphaIIb beta3 integrin (GPII/IIIa) affinity, specificity, and oral antiplatelet efficacy of DMP 802, a small-molecule nonpeptide antiplatelet agent. Platelet GPIIb/IIIa integrin...
8.
Mousa S, Forsythe M, Wityak J, Bozarth J, Mu D
J Cardiovasc Pharmacol
. 1998 Mar;
31(3):441-8.
PMID: 9514190
Currently used antiplatelet drugs including aspirin, ticlopidine, and others are effective against certain but not all of the many endogenous platelet activators. Because of their limited efficacy, a significant number...
9.
Xue C, Wityak J, Sielecki T, Pinto D, Batt D, Cain G, et al.
J Med Chem
. 1997 Jun;
40(13):2064-84.
PMID: 9207948
Using isoxazoline XR299 (1a) as a starting point for the design of highly potent, long-duration GPIIb/IIIa antagonists, the effect of placing lipophilic substituents at positions alpha and beta to the...
10.
Wityak J, Sielecki T, Pinto D, Emmett G, Sze J, Liu J, et al.
J Med Chem
. 1997 Jan;
40(1):50-60.
PMID: 9016328
Using the isoxazoline as a common structural feature, three series of glycoprotein IIb/IIIa receptor antagonists were evaluated, culminating in the discovery of XR299 (30). In an in vitro assay of...