Paul J Gilligan
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Explore the profile of Paul J Gilligan including associated specialties, affiliations and a list of published articles.
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24
Citations
99
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Recent Articles
1.
Yang W, Wang Y, Lai A, Clark C, Corte J, Fang T, et al.
J Med Chem
. 2020 May;
63(13):7226-7242.
PMID: 32456431
Oral factor XIa (FXIa) inhibitors may provide a promising new antithrombotic therapy with an improved benefit to bleeding risk profile over existing antithrombotic agents. Herein, we report application of a...
2.
Fang T, Corte J, Gilligan P, Jeon Y, Osuna H, Rossi K, et al.
Bioorg Med Chem Lett
. 2020 Jan;
30(4):126949.
PMID: 31932224
The discovery of orally bioavailable FXIa inhibitors has been a challenge. Herein, we describe our efforts to address this challenge by optimization of our imidazole-based macrocyclic series. Our optimization strategy...
3.
Smith 2nd L, Orwat M, Hu Z, Han W, Wang C, Rossi K, et al.
Bioorg Med Chem Lett
. 2015 Dec;
26(2):472-478.
PMID: 26704266
The synthesis, structural activity relationships (SAR), and selectivity profile of a potent series of phenylalanine diamide FXIa inhibitors will be discussed. Exploration of P1 prime and P2 prime groups led...
4.
Hu Z, Wong P, Gilligan P, Han W, Pabbisetty K, Bozarth J, et al.
ACS Med Chem Lett
. 2015 May;
6(5):590-5.
PMID: 26005539
Structure-activity relationship optimization of phenylalanine P1' and P2' regions with a phenylimidazole core resulted in a series of potent FXIa inhibitors. Introducing 4-hydroxyquinolin-2-one as the P2' group enhanced FXIa affinity...
5.
Gilligan P
Curr Top Med Chem
. 2015 Apr;
15(10):927-38.
PMID: 25832719
Mutations in the gene for leucine-rich repeat kinase 2 (LRRK2) have been linked to several familial and sporadic late-onset cases of Parkinson's disease. The cumulative data for the effects of...
6.
7.
Dzierba C, Sielecki T, Arvanitis A, Galka A, Johnson T, Takvorian A, et al.
Bioorg Med Chem Lett
. 2012 Jul;
22(15):4986-9.
PMID: 22749422
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
8.
Gilligan P
Expert Opin Ther Pat
. 2010 Feb;
16(7):913-24.
PMID: 20144054
Corticotropin-releasing factor (CRF) coordinates the neural, endocrine and immune responses of the body to stress. Therefore, CRF receptors are important targets for the design of drugs for depression, anxiety and...
9.
Gilligan P, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li Y, et al.
J Med Chem
. 2009 Apr;
52(9):3073-83.
PMID: 19361210
This report describes the syntheses and structure-activity relationships of 8-(4-methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazine corticotropin releasing factor receptor-1 (CRF(1)) receptor antagonists. CRF(1) receptor antagonists may be potential anxiolytic or antidepressant drugs. This research culminated...
10.
Gilligan P, Clarke T, He L, Lelas S, Li Y, Heman K, et al.
J Med Chem
. 2009 Apr;
52(9):3084-92.
PMID: 19361209
This report describes the syntheses and structure-activity relationships of 8-(substituted pyridyl)pyrazolo[1,5-a]-1,3,5-triazine corticotropin releasing factor receptor-1 (CRF(1)) receptor antagonists. These CRF(1) receptor antagonists may be potential anxiolytic or antidepressant drugs. This...