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Mark Stahlhut

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Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.

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All Publications

2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Nigel J Liverton; Steven W Ludmerer; Terry A Lyle; John A McCauley
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers.
Bioorganic & medicinal chemistry letters 2012;22(23):7207-13.
2012: Michael T Rudd; Mark Stahlhut; Vincenzo Summa; Anne Taylor; Nicole Trainor; Joseph P Vacca; Bang-Lin Wan; Christine Burlein; Kimberly Bush; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Adam Gates; Kevin F Gilbert; Donald J Graham; Steven Harper; M Katharine Holloway; Qian Huang; Steven W Ludmerer; Terry A Lyle; John A McCauley; Stephanie McClain; Carolyn McHale; Charles J McIntyre; Kevin T Nguyen; David B Olsen; Joseph J Romano; Michael Rowley; Nigel J Liverton
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Bioorganic & medicinal chemistry letters 2012;22(23):7201-6.
2012: Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
Antimicrobial agents and chemotherapy 2012;56(8):4161-7.
2010: Nigel J Liverton; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Donald J Graham; Daria J Hazuda; M Katherine Holloway; Steven W Ludmerer; John A McCauley; Charles J McIntyre; David B Olsen; Michael T Rudd; Mark Stahlhut; Joseph P Vacca
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Antimicrobial agents and chemotherapy 2010;54(1):305-11.
2008: Steven W Ludmerer; Donald J Graham; Mihir Patel; Kevin Gilbert; Mark Stahlhut; David B Olsen
A transient cell-based phenotype assay for hepatitis C NS3/4A protease: application to potency determinations of a novel macrocyclic inhibitor against diverse protease sequences isolated from plasma infected with HCV.
Journal of virological methods 2008;151(2):301-7.
2008: Nigel J Liverton; M Katharine Holloway; John A McCauley; Michael T Rudd; John W Butcher; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Kevin F Gilbert; Shi-Shan Mao; Charles J McIntyre; Kevin T Nguyen; Joseph J Romano; Mark Stahlhut; Bang-Lin Wan; David B Olsen; Joseph P Vacca
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease.
Journal of the American Chemical Society 2008;130(14):4607-9.
2007: Subharekha Raghavan; Zhijian Lu; Teresa Beeson; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lori Gabryelski; Emilio A Emini; James R Tata
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.
Bioorganic & medicinal chemistry letters 2007;17(19):5432-6.
2007: Gabor Butora; David B Olsen; Steven S Carroll; Daniel R McMasters; Christoph Schmitt; Joseph F Leone; Mark Stahlhut; Christine Burlein; Malcolm MacCoss
Synthesis and HCV inhibitory properties of 9-deaza- and 7,9-dideaza-7-oxa-2'-C-methyladenosine.
Bioorganic & medicinal chemistry 2007;15(15):5219-29.
2006: Amos B Smith; Adam K Charnley; Hironori Harada; Jason J Beiger; Louis-David Cantin; Craig S Kenesky; Ralph Hirschmann; Sanjeev Munshi; David B Olsen; Mark Stahlhut; William A Schleif; Lawrence C Kuo
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
Bioorganic & medicinal chemistry letters 2006;16(4):859-63.
2006: Donald J Graham; Mark Stahlhut; Osvaldo A Flores; David B Olsen; Daria J Hazuda; Robert L LaFemina; Steven W Ludmerer
A genotype 2b NS5B polymerase with novel substitutions supports replication of a chimeric HCV 1b:2b replicon containing a genotype 1b NS3-5A background.
Antiviral research 2006;69(1):24-30.
2005: Joanne E Tomassini; Krista Getty; Mark Stahlhut; Sung Shim; Balkrishen Bhat; Anne B Eldrup; Thazha P Prakash; Steven S Carroll; Osvaldo A Flores; Malcolm MacCoss; Daniel R McMasters; Giovanni Migliaccio; David B Olsen
Inhibitory effect of 2'-substituted nucleosides on hepatitis C virus replication correlates with metabolic properties in replicon cells.
Antimicrobial agents and chemotherapy 2005;49(5):2050-8.
2005: Thazha P Prakash; Marija Prhavc; Anne B Eldrup; P Dan Cook; Steven S Carroll; David B Olsen; Mark Stahlhut; Joanne E Tomassini; Malcolm MacCoss; Sheila M Galloway; Cathy Hilliard; Balkrishen Bhat
Synthesis and evaluation of S-acyl-2-thioethyl esters of modified nucleoside 5'-monophosphates as inhibitors of hepatitis C virus RNA replication.
Journal of medicinal chemistry 2005;48(4):1199-210.
2004: Sheo B Singh; John G Ondeyka; Nasios Tsipouras; Carolyn Ruby; Vinod Sardana; Marvin Schulman; Manuel Sanchez; Fernando Pelaez; Mark Stahlhut; Sanjeev Munshi; David B Olsen; Russell Lingham
Hinnuliquinone, a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease.
Biochemical and biophysical research communications 2004;324(1):108-13.
2004: David B Olsen; Anne B Eldrup; Linda Bartholomew; Balkrishen Bhat; Michele Bosserman; Alessandra Ceccacci; Lawrence F Colwell; John F Fay; Osvaldo A Flores; Krista Getty; Jay A Grobler; Robert L LaFemina; Eric J Markel; Giovanni Migliaccio; Marija Prhavc; Mark Stahlhut; Joanne E Tomassini; Malcolm MacCoss; Daria J Hazuda; Steven S Carroll
A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties.
Antimicrobial agents and chemotherapy 2004;48(10):3944-53.
2004: Ronald M Kim; Elizabeth A Rouse; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Emilio A Emini; James R Tata
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.
Bioorganic & medicinal chemistry letters 2004;14(18):4651-4.
2003: Giovanni Migliaccio; Joanne E Tomassini; Steven S Carroll; Licia tomei; Sergio Altamura; Balkrishen Bhat; Linda Bartholomew; Michele Bosserman; Alessandra Ceccacci; Lawrence F Colwell; Riccardo Cortese; Raffaele De Francesco; Anne B Eldrup; Krista Getty; Xiaoli S Hou; Robert L LaFemina; Steven W Ludmerer; Malcolm MacCoss; Daniel R McMasters; Mark Stahlhut; David B Olsen; Daria J Hazuda; Osvaldo A Flores
Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro.
The Journal of biological chemistry 2003;278(49):49164-70.
2003: Nancy J Kevin; Joseph L Duffy; Brian A Kirk; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Lixia Jin; Jiunn H Lin; Emilio A Emini; James R Tata
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.
Bioorganic & medicinal chemistry letters 2003;13(22):4027-30.
2003: Joseph L Duffy; Brian A Kirk; Nancy J Kevin; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Lixia Jin; Jiunn H Lin; Emilio A Emini; James R Tata
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.
Bioorganic & medicinal chemistry letters 2003;13(19):3323-6.
2003: Fengqi Zhang; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Lixia Jin; Jiunn H Lin; Emilio A Emini; James R Tata
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters 2003;13(15):2573-6.
2003: Joseph L Duffy; Thomas A Rano; Nancy J Kevin; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Lixia Jin; Jiunn H Lin; Emilio A Emini; James R Tata
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.
Bioorganic & medicinal chemistry letters 2003;13(15):2569-72.
2003: Zhijian Lu; Subharekha Raghavan; Joann Bohn; Mark Charest; Mark Stahlhut; Carrie A Rutkowski; Amy L Simcoe; David B Olsen; William A Schleif; Anthony Carella; Lori Gabryelski; Lixia Jin; Jiunn H Lin; Emilio A Emini; Kevin Chapman; James R Tata
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
Bioorganic & medicinal chemistry letters 2003;13(10):1821-4.
2003: Steven S Carroll; Joanne E Tomassini; Michele Bosserman; Krista Getty; Mark Stahlhut; Anne B Eldrup; Balkrishen Bhat; Dawn Hall; Amy L Simcoe; Robert L LaFemina; Carrie A Rutkowski; Bohdan Wolanski; Zhucheng Yang; Giovanni Migliaccio; Raffaele De Francesco; Lawrence C Kuo; Malcolm MacCoss; David B Olsen
Inhibition of hepatitis C virus RNA replication by 2'-modified nucleoside analogs.
The Journal of biological chemistry 2003;278(14):11979-84.
2002: Subharekha Raghavan; Zheng Yang; Ralph T Mosley; William A Schleif; Lori Gabryelski; David B Olsen; Mark Stahlhut; Lawrence C Kuo; Emilio A Emini; Kevin Chapman; James R Tata
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.
Bioorganic & medicinal chemistry letters 2002;12(20):2855-8.
2002: Joseph L Duffy; Nancy J Kevin; Brian A Kirk; Kevin Chapman; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Lixia Jin; Jiunn H Lin; Emilio A Emini; James R Tata
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.
Bioorganic & medicinal chemistry letters 2002;12(17):2423-6.
2002: Yuan Cheng; Fengqi Zhang; Thomas A Rano; Zhijian Lu; William A Schleif; Lori Gabryelski; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Jiunn H Lin; Lixia Jin; Emilio A Emini; Kevin Chapman; James R Tata
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Bioorganic & medicinal chemistry letters 2002;12(17):2419-22.
2002: Yuan Cheng; Thomas A Rano; Tracy T Huening; Fengqi Zhang; Zhijian Lu; William A Schleif; Lori Gabryelski; David B Olsen; Mark Stahlhut; Lawrence C Kuo; Jiunn H Lin; Xin Xu; Lixia Jin; Timothy V Olah; Debra McLoughlin; Rick C King; Kevin Chapman; James R Tata
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Bioorganic & medicinal chemistry letters 2002;12(4):529-32.
2000: Bruce D Dorsey; Colleen McDonough; S L McDaniel; R B Levin; Christina L Newton; J M Hoffman; Paul L Darke; Joan Zugay-Murphy; Emilio A Emini; William A Schleif; David B Olsen; Mark Stahlhut; Carrie A Rutkowski; Lawrence C Kuo; Jiunn H Lin; I-Wu Chen; Stuart R Michelson; M Katharine Holloway; Joel R Huff; Joseph P Vacca
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Journal of medicinal chemistry 2000;43(18):3386-99.
1999: David B Olsen; Mark Stahlhut; Carrie A Rutkowski; HB Schock; A L vanOlden; Lawrence C Kuo
Non-active site changes elicit broad-based cross-resistance of the HIV-1 protease to inhibitors.
The Journal of biological chemistry 1999;274(34):23699-701.