Victor R Guarino
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Explore the profile of Victor R Guarino including associated specialties, affiliations and a list of published articles.
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11
Citations
36
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Recent Articles
1.
Zhang X, Jiang W, Richter J, Bates J, Reznik S, Stachura S, et al.
J Med Chem
. 2024 Feb;
67(5):3571-3589.
PMID: 38385264
PAR4 is a promising antithrombotic target with potential for separation of efficacy from bleeding risk relative to current antiplatelet therapies. In an effort to discover a novel PAR4 antagonist chemotype,...
2.
Priestley E, Banville J, Deon D, Dube L, Gagnon M, Guy J, et al.
J Med Chem
. 2022 Jun;
65(13):8843-8854.
PMID: 35729784
Protease-activated receptor 4 (PAR4) is a G-protein coupled receptor that is expressed on human platelets and activated by the coagulation enzyme thrombin. PAR4 plays a key role in blood coagulation,...
3.
Xiao H, Li N, Duan J, Jiang B, Lu Z, Ngu K, et al.
J Med Chem
. 2020 Dec;
63(23):15050-15071.
PMID: 33261314
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both the...
4.
Hu Z, Wang C, Glunz P, Li J, Cheadle N, Chen A, et al.
Bioorg Med Chem Lett
. 2020 Aug;
30(21):127495.
PMID: 32798651
Structure-activity relationship optimization on a series of phenylpyrazole amides led to the identification of a dual ROCK1 and ROCK2 inhibitor (25) which demonstrated good potency, kinome selectivity and favorable pharmacokinetic...
5.
Guarino V, Olson R, Everlof J, Wang N, Mcdonald I, Haskell R, et al.
Bioorg Med Chem Lett
. 2019 Dec;
30(3):126856.
PMID: 31870650
The objective of this Letter is to report the first (to our knowledge) in vivo proof of concept for a sulfenamide prodrug to orally deliver a poorly soluble drug containing...
6.
Miller M, Banville J, Friends T, Gagnon M, Hangeland J, Lavallee J, et al.
J Med Chem
. 2019 Jun;
62(16):7400-7416.
PMID: 31246024
In an effort to identify novel antithrombotics, we have investigated protease-activated receptor 4 (PAR4) antagonism by developing and evaluating a tool compound, , in a monkey thrombosis model. Beginning with...
7.
Nti-Addae K, Guarino V, Dalwadi G, Stella V
J Pharm Sci
. 2012 Mar;
101(9):3134-41.
PMID: 22374830
The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across...
8.
Guarino V, Nti-Addae K, Stella V
Bioorg Med Chem Lett
. 2011 Apr;
21(9):2780-3.
PMID: 21513867
The objective of this Letter is both to report the permeability results of a linezolid-based sulfenamide prodrug in an MDCK cell model (enterocyte surrogate system) and to discuss the strategic...
9.
Guarino V, Nti-Addae K, Stella V
Bioorg Med Chem Lett
. 2010 Dec;
21(1):172-5.
PMID: 21126873
The objective of this Letter is both to report the permeability results of a linezolid-based sulfenamide prodrug in an MDCK cell model (enterocyte surrogate system) and to discuss the strategic...
10.
Hemenway J, Nti-Addae K, Guarino V, Stella V
Bioorg Med Chem Lett
. 2007 Oct;
17(23):6629-32.
PMID: 17928225
Improved synthetic methods are reported for the preparation of sulfenamide derivatives of carbamazepine (CBZ) for evaluation as prodrugs. These sulfenamide prodrugs were designed to rapidly release CBZ in vivo by...