Robert G Gentles
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Explore the profile of Robert G Gentles including associated specialties, affiliations and a list of published articles.
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18
Citations
130
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Recent Articles
1.
Chupak L, Zheng X, Hu S, Huang Y, Ding M, Lewis M, et al.
Bioorg Med Chem
. 2016 Feb;
24(7):1455-68.
PMID: 26917221
N-Benzylic-substituted glycine sulfonamides that reversibly inhibit diacylglycerol (DAG) lipases are reported. Detailed herein are the structure activity relationships, profiling characteristics and physico-chemical properties for the first reported series of DAG...
2.
Alt A, Pendri A, Bertekap Jr R, Li G, Benitex Y, Nophsker M, et al.
J Pharmacol Exp Ther
. 2015 Nov;
356(2):293-304.
PMID: 26582730
The muscarinic acetylcholine receptor subtype 1 (M1) receptors play an important role in cognition and memory, and are considered to be attractive targets for the development of novel medications to...
3.
Lewis M, Hunihan L, Watson J, Gentles R, Hu S, Huang Y, et al.
J Pharmacol Exp Ther
. 2015 Jun;
354(3):340-9.
PMID: 26109678
The present studies represent the first published report of a dopamine D1 positive allosteric modulator (PAM). D1 receptors have been proposed as a therapeutic target for the treatment of cognitive...
4.
Rigat K, Lu H, Wang Y, Argyrou A, Fanslau C, Beno B, et al.
J Biol Chem
. 2014 Oct;
289(48):33456-68.
PMID: 25301950
HCV infection is an urgent global health problem that has triggered a drive to discover therapies that specifically target the virus. BMS-791325 is a novel direct antiviral agent specifically targeting...
5.
Lemm J, Liu M, Gentles R, Ding M, Voss S, Pelosi L, et al.
Antimicrob Agents Chemother
. 2014 Apr;
58(6):3485-95.
PMID: 24733465
BMS-791325 is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. BMS-791325 inhibits recombinant NS5B proteins from HCV genotypes 1,...
6.
Gentles R, Ding M, Bender J, Bergstrom C, Grant-Young K, Hewawasam P, et al.
J Med Chem
. 2014 Jan;
57(5):1855-79.
PMID: 24397558
Described herein are structure-activity relationship studies that resulted in the optimization of the activity of members of a class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors. Subsequent iterations of analogue...
7.
Brown J, Hunihan L, Prack M, Harden D, Bronson J, Dzierba C, et al.
J Neurochem
. 2013 Nov;
129(2):275-83.
PMID: 24266811
NMDA receptor hypofunction is hypothesized to contribute to cognitive deficits associated with schizophrenia. Since direct activation of NMDA receptors is associated with serious adverse effects, modulation of the NMDA co-agonists,...
8.
Appiah K, Blat Y, Robertson B, Pearce B, Pedicord D, Gentles R, et al.
J Biomol Screen
. 2013 Nov;
19(4):595-605.
PMID: 24241710
Recent genetic evidence suggests that the diacylglycerol lipase (DAGL-α) isoform is the major biosynthetic enzyme for the most abundant endocannabinoid, 2-arachidonoyl-glycerol (2-AG), in the central nervous system. Revelation of its...
9.
Ding M, He F, Hudyma T, Zheng X, Poss M, Kadow J, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(8):2866-71.
PMID: 22424979
Presented here are initial structure-activity relationship (SAR) studies on a series of novel heteroaryl fused tetracyclic indole-based inhibitors of the hepatitis C viral polymerase, NS5B. The introduction of alternative heterocyclic...
10.
Ding M, He F, Poss M, Rigat K, Wang Y, Roberts S, et al.
Org Biomol Chem
. 2011 Jul;
9(19):6654-62.
PMID: 21800000
Three synthetic approaches have been developed that allow efficient access to novel heteroaryl fused indole ring systems, including: 7,8,9,10-tetrahydro-6H-azepino[1,2-a]indoles, 4-oxo-2,3-dihydro-1H-[1,4]diazepino[1,7-a]indoles and 1,2,4,5-tetrahydro-[1,4]oxazepino[4,5-a]indoles. Each strategy is fully exemplified and the relative...