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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
Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. X-ray structure of an inhibitor, 15c bound to the protease is presented. Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4...
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Published in: | Bioorganic & medicinal chemistry letters 2004-12, Vol.14 (23), p.5751-5755 |
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container_issue | 23 |
container_start_page | 5751 |
container_title | Bioorganic & medicinal chemistry letters |
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creator | Arasappan, Ashok Njoroge, F. George Parekh, Tejal N. Yang, Xiaozheng Pichardo, John Butkiewicz, Nancy Prongay, Andrew Yao, Nanhua Girijavallabhan, Viyyoor |
description | Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. X-ray structure of an inhibitor,
15c bound to the protease is presented.
Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. Inhibitors derived from this new P2 core exhibited activity in the low μM range. X-ray structure of an inhibitor,
15c bound to the protease is presented. |
doi_str_mv | 10.1016/j.bmcl.2004.09.058 |
format | article |
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Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. Inhibitors derived from this new P2 core exhibited activity in the low μM range. X-ray structure of an inhibitor,
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15c bound to the protease is presented.
Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. Inhibitors derived from this new P2 core exhibited activity in the low μM range. X-ray structure of an inhibitor,
15c bound to the protease is presented.</description><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Biological and medical sciences</subject><subject>Carboxylic Acids - chemical synthesis</subject><subject>Carboxylic Acids - pharmacology</subject><subject>CRYSTAL STRUCTURE</subject><subject>Crystallography, X-Ray - methods</subject><subject>ENZYME INHIBITORS</subject><subject>Hepacivirus - drug effects</subject><subject>Hepacivirus - enzymology</subject><subject>HEPATITIS</subject><subject>Imidazolidines - chemical synthesis</subject><subject>Imidazolidines - pharmacology</subject><subject>MATERIALS SCIENCE</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Conformation</subject><subject>SERINE</subject><subject>Serine Endopeptidases - metabolism</subject><subject>Serine Proteinase Inhibitors - chemical synthesis</subject><subject>Serine Proteinase Inhibitors - pharmacology</subject><subject>SYNTHESIS</subject><subject>Viral Nonstructural Proteins - antagonists & inhibitors</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><recordid>eNp9kd-K1DAUh4so7rj6Al5IEPTKjkmbtM3izTKoKyzrhQp7V9LklMnQJmNOOkz34Xw2U2ZgvfIq_77zJSe_LHvN6JpRVn3crbtRD-uCUr6mck1F8yRbMV7xvORUPM1WVFY0byS_v8heIO4oZZxy_jy7YEJQRkuxyv7c-QMMpMj90dvRGvXgB2usg5znWoXOH-fBaqK0NcRAsAcV7QGQKCQ3sE-LaJFsyMGGCcndjzLn1wQT54Dsg4-gEIh1W9vZ6ANeEZxd3AJa_JCcSWXjnGbOkPs8qJnoMGNUA8EYJh2nAMT36ZiAe5jHf0xE-3E_wPFl9qxXA8Kr83iZ_fry-efmJr_9_vXb5vo215zKmOtSMtNJVXAuTcd7WtZSNLzRstMArFRNb2qumZZGdpVOe5XpGC1ELYQUSpSX2duT12O0LWobQW-1dw50bBmlTS1kgt6foNT57wkwtqNFDcOgHPgJ26pOSdGaJbA4gTp4xAB9uw92VGFOqnaJtt21S7TtEm1LZZuiTUVvzvapG8E8lpyzTMC7M6BQq6EPymmLj1xVFGXNlts_nThIH3awEJZ-wGkwNiztGG__946_ljvFvQ</recordid><startdate>20041206</startdate><enddate>20041206</enddate><creator>Arasappan, Ashok</creator><creator>Njoroge, F. 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Antiparasitic agents</topic><topic>Antiviral agents</topic><topic>Biological and medical sciences</topic><topic>Carboxylic Acids - chemical synthesis</topic><topic>Carboxylic Acids - pharmacology</topic><topic>CRYSTAL STRUCTURE</topic><topic>Crystallography, X-Ray - methods</topic><topic>ENZYME INHIBITORS</topic><topic>Hepacivirus - drug effects</topic><topic>Hepacivirus - enzymology</topic><topic>HEPATITIS</topic><topic>Imidazolidines - chemical synthesis</topic><topic>Imidazolidines - pharmacology</topic><topic>MATERIALS SCIENCE</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Conformation</topic><topic>SERINE</topic><topic>Serine Endopeptidases - metabolism</topic><topic>Serine Proteinase Inhibitors - chemical synthesis</topic><topic>Serine Proteinase Inhibitors - pharmacology</topic><topic>SYNTHESIS</topic><topic>Viral Nonstructural Proteins - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Arasappan, Ashok</creatorcontrib><creatorcontrib>Njoroge, F. George</creatorcontrib><creatorcontrib>Parekh, Tejal N.</creatorcontrib><creatorcontrib>Yang, Xiaozheng</creatorcontrib><creatorcontrib>Pichardo, John</creatorcontrib><creatorcontrib>Butkiewicz, Nancy</creatorcontrib><creatorcontrib>Prongay, Andrew</creatorcontrib><creatorcontrib>Yao, Nanhua</creatorcontrib><creatorcontrib>Girijavallabhan, Viyyoor</creatorcontrib><creatorcontrib>Argonne National Lab. (ANL), Argonne, IL (United States). 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Advanced Photon Source (APS)</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>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</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2004-12-06</date><risdate>2004</risdate><volume>14</volume><issue>23</issue><spage>5751</spage><epage>5755</epage><pages>5751-5755</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. X-ray structure of an inhibitor,
15c bound to the protease is presented.
Synthesis and HCV NS3 serine protease inhibitory activity of some novel 2-oxoimidazolidine-4-carboxylic acid derivatives are reported. Inhibitors derived from this new P2 core exhibited activity in the low μM range. X-ray structure of an inhibitor,
15c bound to the protease is presented.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15501035</pmid><doi>10.1016/j.bmcl.2004.09.058</doi><tpages>5</tpages></addata></record> |
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subjects | Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences Carboxylic Acids - chemical synthesis Carboxylic Acids - pharmacology CRYSTAL STRUCTURE Crystallography, X-Ray - methods ENZYME INHIBITORS Hepacivirus - drug effects Hepacivirus - enzymology HEPATITIS Imidazolidines - chemical synthesis Imidazolidines - pharmacology MATERIALS SCIENCE Medical sciences Pharmacology. Drug treatments Protein Conformation SERINE Serine Endopeptidases - metabolism Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - pharmacology SYNTHESIS Viral Nonstructural Proteins - antagonists & inhibitors |
title | 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 |
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