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Pyrazolo[1,5- a]pyrimidine-based inhibitors of HCV polymerase
Synthesis and optimization of novel pyrazolo[1,5- a]pyrimidine HCV polymerase inhibitors are described. The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5- a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds...
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| Published in: | Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (22), p.6331-6336 |
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| Main Authors: | , , , , , , , , , , , |
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| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c416t-f97f5710e2db2692c030e4ce437ec6746a180140b9be6fb8f6010142b0ed27093 |
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| cites | cdi_FETCH-LOGICAL-c416t-f97f5710e2db2692c030e4ce437ec6746a180140b9be6fb8f6010142b0ed27093 |
| container_end_page | 6336 |
| container_issue | 22 |
| container_start_page | 6331 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 19 |
| creator | Popovici-Muller, Janeta Shipps, Gerald W. Rosner, Kristin E. Deng, Yongqi Wang, Tong Curran, Patrick J. Brown, Meredith A. Siddiqui, M. Arshad Cooper, Alan B. Duca, José Cable, Michael Girijavallabhan, Viyyoor |
| description | Synthesis and optimization of novel pyrazolo[1,5-
a]pyrimidine HCV polymerase inhibitors are described.
The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-
a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low nanomolar potencies in a biochemical RdRp assay. SAR trends clearly reveal a stringent preference for a cyclohexyl group as one of the hydrophobes, and improved activities for carboxylic acid derivatives. |
| doi_str_mv | 10.1016/j.bmcl.2009.09.087 |
| format | article |
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a]pyrimidine HCV polymerase inhibitors are described.
The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-
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a]pyrimidine HCV polymerase inhibitors are described.
The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-
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Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Biological and medical sciences</subject><subject>DNA-Directed RNA Polymerases - antagonists & inhibitors</subject><subject>Drug Evaluation, Preclinical</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>HCV polymerase inhibitors</subject><subject>Hepacivirus</subject><subject>Hepatitis C - enzymology</subject><subject>Hepatitis C - virology</subject><subject>Hepatitis C virus</subject><subject>Inhibitory Concentration 50</subject><subject>Medical sciences</subject><subject>Molecular Weight</subject><subject>Pharmacology. 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a]pyrimidine HCV polymerase inhibitors are described.
The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-
a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low nanomolar potencies in a biochemical RdRp assay. SAR trends clearly reveal a stringent preference for a cyclohexyl group as one of the hydrophobes, and improved activities for carboxylic acid derivatives.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19819138</pmid><doi>10.1016/j.bmcl.2009.09.087</doi><tpages>6</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6331-6336 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | ScienceDirect Freedom Collection 2022-2024 |
| subjects | Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences DNA-Directed RNA Polymerases - antagonists & inhibitors Drug Evaluation, Preclinical Enzyme Inhibitors - pharmacology HCV polymerase inhibitors Hepacivirus Hepatitis C - enzymology Hepatitis C - virology Hepatitis C virus Inhibitory Concentration 50 Medical sciences Molecular Weight Pharmacology. Drug treatments Pyrazoles - pharmacology Pyrimidines - pharmacology RNA Replicase - antagonists & inhibitors RNA, Viral - drug effects Small Molecule Libraries |
| title | Pyrazolo[1,5- a]pyrimidine-based inhibitors of HCV polymerase |
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