Michael P Dwyer
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Explore the profile of Michael P Dwyer including associated specialties, affiliations and a list of published articles.
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31
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601
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Recent Articles
1.
Morriello G, Dwyer M, Chen Y, Ginetti A, Xu S, Lu J, et al.
Bioorg Med Chem Lett
. 2021 May;
44:128082.
PMID: 33991626
A focused SAR study was conducted on a series of N1-substituted pyrazolopyrimidinone PDE2 inhibitors to reveal compounds with excellent potency and selectivity. The series was derived from previously identified internal...
2.
Stachel S, Berger R, Nomland A, Ginnetti A, Paone D, Wang D, et al.
ACS Med Chem Lett
. 2018 Aug;
9(8):815-820.
PMID: 30128073
Herein we describe the development of a series of pyrazolopyrimidinone phosphodiesterase 2A (PDE2) inhibitors using structure-guided lead identification and design. The series was derived from informed chemotype replacement based on...
3.
Bungard C, Williams P, Schulz J, Wiscount C, Holloway M, Loughran H, et al.
ACS Med Chem Lett
. 2017 Dec;
8(12):1292-1297.
PMID: 29259750
Using the HIV-1 protease binding mode of and as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core...
4.
Tong L, Yu W, Chen L, Selyutin O, Dwyer M, Nair A, et al.
J Med Chem
. 2016 Nov;
60(1):290-306.
PMID: 27808515
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A...
5.
Tong L, Yu W, Coburn C, Chen L, Selyutin O, Zeng Q, et al.
Bioorg Med Chem Lett
. 2016 Sep;
26(21):5354-5360.
PMID: 27680588
We describe the impact of proline modifications, in our tetracyclic-indole based series of nonstructural protein 5A (NS5A) inhibitors, to their replicon profiles. This work identified NS5A inhibitors with an improved...
6.
Tong L, Yu W, Coburn C, Meinke P, Nair A, Dwyer M, et al.
Bioorg Med Chem Lett
. 2016 Sep;
26(20):5132-5137.
PMID: 27634194
Herein, we describe our research efforts to develop unique cores in molecules which function as HCV nonstructural protein 5A (NS5A) inhibitors. In particular, various fused tetracyclic cores were identified which...
7.
Yu W, Zhou G, Coburn C, Zeng Q, Tong L, Dwyer M, et al.
Bioorg Med Chem Lett
. 2016 Aug;
26(19):4851-4856.
PMID: 27568086
As part of an ongoing effort in NS5A inhibition at Merck we now describe our efforts for introducing substitution around the tetracyclic indole core of MK-8742. Fluoro substitution on the...
8.
Dwyer M, Keertikar K, Chen L, Tong L, Selyutin O, Nair A, et al.
Bioorg Med Chem Lett
. 2016 Jul;
26(16):4106-11.
PMID: 27423481
A matched and mixed capping SAR study was conducted on the tetracyclic indole class of HCV NS5A inhibitors to examine the influence of modifications of this region on the overall...
9.
Yu W, Coburn C, Nair A, Wong M, Rosenblum S, Zhou G, et al.
Bioorg Med Chem Lett
. 2016 Jul;
26(15):3414-20.
PMID: 27394665
Herein we describe our research efforts around the aryl and heteroaryl substitutions at the aminal carbon of the tetracyclic indole-based HCV NS5A inhibitor MK-8742. A series of potent NS5A inhibitors...
10.
Yu W, Vibulbhan B, Rosenblum S, Martin G, Vellekoop A, Holst C, et al.
Bioorg Med Chem Lett
. 2016 Jun;
26(15):3793-9.
PMID: 27282743
HCV NS5A inhibitors have demonstrated impressive in vitro virologic profiles in HCV replicon assays and robust HCV RNA titer reduction in the clinic making them attractive components for inclusion in...