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Jennifer Liras - One of the best experts on this subject based on the ideXlab platform.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
Vijayalakshmi Natarajan - One of the best experts on this subject based on the ideXlab platform.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
Lisa M Reeves - One of the best experts on this subject based on the ideXlab platform.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
Francis J Sweeney - One of the best experts on this subject based on the ideXlab platform.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
John A Barberia - One of the best experts on this subject based on the ideXlab platform.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
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discovery of 3 3 dimethyl 5 hydroxypipecolic hydroxamate based inhibitors of aggrecanase and mmp 13
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Vijayalakshmi Natarajan, Sheri L Snow, Peter G Mitchell, Lori L Loprestimorrow, Lisa M Reeves, Sue A Yocum, Thomas J Carty, John A Barberia, Francis J Sweeney, Jennifer LirasAbstract:Abstract A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE). Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group. Incorporation of geminal alkyl substitution at the 3-position of the piperidine ring improved metabolic stability, presumably by increasing steric hindrance around the metabolically labile hydroxamic acid. This modification also resulted in dramatic improvement of aggrecanase activity with a Slight Reduction in selectivity versus MMP-1. Synthesis, structure activity relationships, and strategies to reduce metabolic clearance are described.
