Samuel L Graham
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Explore the profile of Samuel L Graham including associated specialties, affiliations and a list of published articles.
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Recent Articles
1.
Staas D, Bell I, Burgey C, Deng J, Gallicchio S, Lim J, et al.
Bioorg Med Chem Lett
. 2024 Sep;
112:129944.
PMID: 39233187
A novel series of 3-amino-piperidin-2-one-based calcitonin gene-related peptide (CGRP) receptor antagonists was invented based upon the discovery of unexpected structure-activity observations. Initial exploration of the structure-activity relationships enabled the generation...
2.
Ginnetti A, Paone D, Stauffer S, Potteiger C, Shaw A, Deng J, et al.
Bioorg Med Chem Lett
. 2018 Mar;
28(8):1392-1396.
PMID: 29548573
A second-generation small molecule P2X3 receptor antagonist has been developed. The lead optimization strategy to address shortcomings of the first-generation preclinical lead compound is described herein. These studies were directed...
3.
Egbertson M, McGaughey G, Pitzenberger S, Stauffer S, Coburn C, Stachel S, et al.
Bioorg Med Chem Lett
. 2015 Jul;
25(21):4812-4819.
PMID: 26195137
The IC50 of a beta-secretase (BACE-1) lead compound was improved ∼200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR,...
4.
Bell I, Gallicchio S, Stump C, Bruno J, Fan H, Gantert L, et al.
ACS Med Chem Lett
. 2014 Jun;
4(9):863-8.
PMID: 24900761
Rational modification of the potent calcitonin gene-related peptide (CGRP) receptor antagonist MK-3207 led to a series of analogues with enhanced CNS penetrance and a convenient chemical handle for introduction of...
5.
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...
6.
Stachel S, Steele T, Petrocchi A, Haugabook S, McGaughey G, Holloway M, et al.
Bioorg Med Chem Lett
. 2011 Dec;
22(1):240-4.
PMID: 22130130
We have developed a novel series of pyrrolidine derived BACE-1 inhibitors. The potency of the weak initial lead structure was enhanced using library-based SAR methods. The series was then further...
7.
Blair Zartman C, Bell I, Gallicchio S, Graham S, Kane S, Mallee J, et al.
Bioorg Med Chem Lett
. 2011 Oct;
21(22):6705-8.
PMID: 21982500
Identification of an HIV integrase inhibitor with micromolar affinity for the CGRP receptor led to the discovery of a series of structurally novel CGRP receptor antagonists. Optimization of this series...
8.
Stump C, Bell I, Bednar R, Fay J, Gallicchio S, Hershey J, et al.
Bioorg Med Chem Lett
. 2010 Mar;
20(8):2572-6.
PMID: 20299218
A novel series of potent CGRP receptor antagonists containing a central quinoline ring constraint was identified. The combination of the quinoline constraint with a tricyclic benzimidazolinone left hand fragment produced...
9.
Zhu H, Young M, Nantermet P, Graham S, Colussi D, Lai M, et al.
Bioorg Med Chem Lett
. 2010 Feb;
20(5):1779-82.
PMID: 20122828
This Letter describes the one pot synthesis of tertiary carbinamine 3 and related analogs of brain penetrant BACE-1 inhibitors via the alkylation of the Schiff base intermediate 2. The methodology...
10.
Salvatore C, Moore E, Calamari A, Cook J, Michener M, OMalley S, et al.
J Pharmacol Exp Ther
. 2010 Jan;
333(1):152-60.
PMID: 20065019
Calcitonin gene-related peptide (CGRP) has long been hypothesized to play a key role in migraine pathophysiology, and the advent of small-molecule antagonists has clearly demonstrated a clinical link between blocking...