Mark W Stahlhut
Overview
Explore the profile of Mark W Stahlhut including associated specialties, affiliations and a list of published articles.
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Articles
14
Citations
560
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Recent Articles
1.
Rudd M, Butcher J, Nguyen K, McIntyre C, Romano J, Gilbert K, et al.
ChemMedChem
. 2015 Mar;
10(4):727-35.
PMID: 25759009
With the goal of identifying inhibitors of hepatitis C virus (HCV) NS3/4a protease that are potent against a wide range of genotypes and clinically relevant mutant viruses, several subseries of...
2.
Harper S, McCauley J, Rudd M, Ferrara M, DiFilippo M, Crescenzi B, et al.
ACS Med Chem Lett
. 2014 Jun;
3(4):332-6.
PMID: 24900473
A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint was designed using a molecular modeling-derived strategy. Building on the profile of previous clinical compounds...
3.
Rudd M, McCauley J, Butcher J, Romano J, McIntyre C, Nguyen K, et al.
ACS Med Chem Lett
. 2014 Jun;
2(3):207-12.
PMID: 24900304
The discovery of MK-1220 is reported along with the development of a series of HCV NS3/4A protease inhibitors containing a P2 to P4 macrocyclic constraint with improved preclinical pharmacokinetics. Optimization...
4.
Summa V, Ludmerer S, McCauley J, Fandozzi C, Burlein C, Claudio G, et al.
Antimicrob Agents Chemother
. 2012 May;
56(8):4161-7.
PMID: 22615282
HCV NS3/4a protease inhibitors are proven therapeutic agents against chronic hepatitis C virus infection, with boceprevir and telaprevir having recently received regulatory approval as add-on therapy to pegylated interferon/ribavirin for...
5.
McCauley J, McIntyre C, Rudd M, Nguyen K, Romano J, Butcher J, et al.
J Med Chem
. 2010 Feb;
53(6):2443-63.
PMID: 20163176
A new class of HCV NS3/4a protease inhibitors which contain a P2 to P4 macrocyclic constraint was designed using a molecular-modeling derived strategy. Exploration of the P2 heterocyclic region, the...
6.
McCauley J, Rudd M, Nguyen K, McIntyre C, Romano J, Bush K, et al.
Angew Chem Int Ed Engl
. 2008 Oct;
47(47):9104-7.
PMID: 18925594
No abstract available.
7.
Smith 3rd A, Charnley A, Harada H, Beiger J, Cantin L, Kenesky C, et al.
Bioorg Med Chem Lett
. 2005 Nov;
16(4):859-63.
PMID: 16298527
A series of monopyrrolinone-based HIV-1 protease inhibitors possessing rationally designed P2' side chains have been synthesized and evaluated for activity against wild-type HIV-1 protease. The most potent inhibitor displays subnanomolar...
8.
Tomassini J, Getty K, Stahlhut M, Shim S, Bhat B, Eldrup A, et al.
Antimicrob Agents Chemother
. 2005 Apr;
49(5):2050-8.
PMID: 15855531
Nucleosides have been widely used in the treatment of viral diseases, but relatively few have been identified as inhibitors of hepatitis C virus (HCV). The modified ribonucleosides, 2'-C-methyl-adenosine and 2'-O-methyl-cytidine,...
9.
Prakash T, Prhavc M, Eldrup A, Cook P, Carroll S, Olsen D, et al.
J Med Chem
. 2005 Feb;
48(4):1199-210.
PMID: 15715486
Several triphosphates of modified nucleosides (1-6) were identified as inhibitors (IC(50) = 0.08-3.8 microM) of hepatitis C virus RNA-dependent RNA polymerase (RdRp). Although the initial SAR developed by determining the...
10.
Singh S, Ondeyka J, Tsipouras N, Ruby C, Sardana V, Schulman M, et al.
Biochem Biophys Res Commun
. 2004 Oct;
324(1):108-13.
PMID: 15464989
HIV-1 protease is one of several key enzymes required for the replication and maturation of HIV-1 virus. An almost two-decade research effort by academic and pharmaceutical institutions resulted in the...