A. Arasappan

发表

Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening.

M. McCoy, M. Senior, D. Wyss, 2004, Journal of medicinal chemistry.

Novel substituted pyrimidines as HCV replication (replicase) inhibitors.

X. Tong, R. Reynolds, B. Feld, 2012, Bioorganic & Medicinal Chemistry Letters.

Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.

X. Tong, M. Maccoss, R. Reynolds, 2012, Bioorganic & medicinal chemistry letters.

5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.

X. Tong, M. Maccoss, R. Reynolds, 2012, Bioorganic & medicinal chemistry letters.

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034.

A. Arasappan, F. G. Njoroge, W. Pan, 2008, Bioorganic & medicinal chemistry letters.

Building a Culture of Medicinal Chemistry Knowledge Sharing.

Andrew M Haidle, I. Raheem, Yeon-Hee Lim, 2022, Journal of medicinal chemistry.

Tetramethylguanidinium azide as a new reagent for the stereoselective synthesis of glycosyl azides

P. Fuchs, A. Arasappan, C. Li, 1993 .

Preclinical Characterization of the Antiviral Activity of SCH 900518 (Narlaprevir), a Novel Mechanism-Based Inhibitor of Hepatitis C Virus NS3 Protease

X. Tong, R. Ralston, B. Feld, 2010, Antimicrobial Agents and Chemotherapy.

Cyclic sulfones as novel P3-caps for hepatitis C virus NS3/4A (HCV NS3/4A) protease inhibitors: synthesis and evaluation of inhibitors with improved potency and pharmacokinetic profiles.

X. Tong, A. McPhail, A. Arasappan, 2010, Journal of medicinal chemistry.

Preparation and Wittig reactions of an α-keto amino acid derivative

A. Arasappan, J. Huffman, M. O'donnell, 1990 .

P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.

V. Madison, A. Arasappan, F. G. Njoroge, 2006, Bioorganic & medicinal chemistry letters.

The double addition reaction of alkoxymethyl nucleophiles to esters to generate novel polyoxygenated species

Vishal A. Verma, A. Arasappan, F. G. Njoroge, 2010 .

Stereoselective Synthesis of β-Substituted β-Amino Sulfones and Sulfonamides via Addition of Sulfonyl Anions to Chiral N-Sulfinyl Imines

A. McPhail, A. Arasappan, T. Chan, 2006 .

The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor.

Zhuyan Guo, Frank Bennett, X. Tong, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species.

R. Doll, Zhuyan Guo, A. Arasappan, 2010, Bioorganic & medicinal chemistry.

Practical and efficient method for amino acid derivatives containing β-quaternary center: application toward synthesis of hepatitis C virus NS3 serine protease inhibitors

A. Arasappan, F. G. Njoroge, T. Meng, 2007 .

Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor:

Weiying Yang, Zhuyan Guo, Andrea Hart, 2006, Journal of medicinal chemistry.

Synthesis and pharmacological evaluation of vinyl sulfone based anticancer agents

P. Fuchs, A. Mahadevan, R. Merriman, 1994 .

N-PENTENYL GLYCOSIDE METHODOLOGY IN THE STEREOSELECTIVE CONSTRUCTION OF THE TETRASACCHARYL CAP PORTION OF LEISHMANIA LIPOPHOSPHOGLYCAN

A. Arasappan, B. Fraser-Reid, 1996 .

n-Pentenyl furanosides: synthesis and glycosidation reactions of some galacto derivatives

A. Arasappan, B. Fraser-Reid, 1995 .

Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.

N. Yao, A. Arasappan, F. G. Njoroge, 2004, Bioorganic & medicinal chemistry letters.

Novel methods to functionalize thiazolo[4,5-c]pyridines

M. Maccoss, A. Arasappan, F. G. Njoroge, 2010 .

Discovery of novel P3 sulfonamide-capped inhibitors of HCV NS3 protease. Inhibitors with improved cellular potencies.

X. Tong, A. Arasappan, K. Cheng, 2009, Bioorganic & medicinal chemistry.

Novel inhibitors of the hepatitis C virus NS3 proteinase.

B. Dasmahapatra, A. Arasappan, F. G. Njoroge, 2005, Bioorganic & medicinal chemistry letters.

Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.

Zhuyan Guo, Frank Bennett, Rong-Sheng Yang, 2007, Journal of medicinal chemistry.

Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor.

Weiying Yang, Frank Bennett, Jesse Wong, 2010, ACS medicinal chemistry letters.

Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.

S. Tamura, S. Kemp, M. Lim-Wilby, 2006, Journal of medicinal chemistry.

Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease.

Weiying Yang, Frank Bennett, X. Tong, 2009, Journal of medicinal chemistry.

2′-Modified Guanosine Analogs for the Treatment of HCV

Q. Dang, A. Stamford, Vishal A. Verma, 2016, Nucleosides, Nucleotides & Nucleic Acids.

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.

S. Tamura, N. Yao, B. Malcolm, 2005, Bioorganic & medicinal chemistry letters.

Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles.

Zhuyan Guo, Frank Bennett, Sumei Ruan, 2009, Journal of medicinal chemistry.

Toward second generation hepatitis C virus NS3 serine protease inhibitors: discovery of novel P4 modified analogues with improved potency and pharmacokinetic profile.

Frank Bennett, X. Tong, A. Arasappan, 2009, Journal of medicinal chemistry.

The use of tetramethylguanidinium azide in non-halogenated solvents avoids potential explosion hazards

T. Shih, P. Fuchs, J. U. Jeong, 1994 .

Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.

X. Tong, M. Maccoss, N. Bansal, 2012, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.

X. Tong, M. Maccoss, N. Bansal, 2012, Bioorganic & medicinal chemistry letters.

Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.

V. Madison, A. Arasappan, F. G. Njoroge, 2005, Bioorganic & medicinal chemistry letters.

Stereoselective Synthesis of β‐Substituted β‐Amino Sulfones and Sulfonamides via Addition of Sulfonyl Anions to Chiral N‐Sulfinyl Imines.

A. McPhail, A. Arasappan, T. Chan, 2006 .

Stereoselective synthesis of beta-substituted beta-amino sulfones and sulfonamides via addition of sulfonyl anions to chiral N-sulfinyl imines.

A. McPhail, A. Arasappan, T. Chan, 2006, Organic letters.

2′-Modified Guanosine Analogs for the Treatment of HCV

Q. Dang, A. Stamford, Vishal A. Verma, 2016, Nucleosides, nucleotides & nucleic acids.

Discovery of the HCV NS3/4A Protease Inhibitor SCH503034. Key Steps in Structure-Based Optimization

P. Weber, M. Senior, Z. Hong, 2007 .