| ชื่อเรื่อง | : | Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors |
| นักวิจัย | : | Pehere, Ashok D. , Pietsch, Markus , Gütschow, Michael , Neilsen, Paul M. , Pedersen, Daniel Sejer , Nguyen, Steven , Zvarec, Ondrej , Sykes, Matthew J. , Callen, David F. , Abell, Andrew D. |
| คำค้น | : | DRNTU::Engineering::Materials. |
| หน่วยงาน | : | Nanyang Technological University, Singapore |
| ผู้ร่วมงาน | : | - |
| ปีพิมพ์ | : | 2556 |
| อ้างอิง | : | Pehere, A. D., Pietsch, M., Gütschow, M., Neilsen, P. M., Pedersen, D. S., Nguyen, S., et al. (2013). Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors. Chemistry - A European Journal, 19(24), 7975-7981. , 0947-6539 , http://hdl.handle.net/10220/19119 , http://dx.doi.org/10.1002/chem.201204260 |
| ที่มา | : | - |
| ความเชี่ยวชาญ | : | - |
| ความสัมพันธ์ | : | Chemistry - a European journal |
| ขอบเขตของเนื้อหา | : | - |
| บทคัดย่อ/คำอธิบาย | : | Peptide-derived protease inhibitors are an important class of compounds with the potential to treat a wide range of diseases. Herein, we describe the synthesis of a series of triazole-containing macrocyclic protease inhibitors pre-organized into a β-strand conformation and an evaluation of their activity against a panel of proteases. Acyclic azido–alkyne-based aldehydes are also evaluated for comparison. The macrocyclic peptidomimetics showed considerable activity towards calpain II, cathepsin L and S, and the 20S proteasome chymotrypsin-like activity. Some of the first examples of highly potent macrocyclic inhibitors of cathepsin S were identified. These adopt a well-defined β-strand geometry as shown by NMR spectroscopy, X-ray analysis, and molecular docking studies. |
| บรรณานุกรม | : |
Pehere, Ashok D. , Pietsch, Markus , Gütschow, Michael , Neilsen, Paul M. , Pedersen, Daniel Sejer , Nguyen, Steven , Zvarec, Ondrej , Sykes, Matthew J. , Callen, David F. , Abell, Andrew D. . (2556). Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors.
กรุงเทพมหานคร : Nanyang Technological University, Singapore. Pehere, Ashok D. , Pietsch, Markus , Gütschow, Michael , Neilsen, Paul M. , Pedersen, Daniel Sejer , Nguyen, Steven , Zvarec, Ondrej , Sykes, Matthew J. , Callen, David F. , Abell, Andrew D. . 2556. "Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors".
กรุงเทพมหานคร : Nanyang Technological University, Singapore. Pehere, Ashok D. , Pietsch, Markus , Gütschow, Michael , Neilsen, Paul M. , Pedersen, Daniel Sejer , Nguyen, Steven , Zvarec, Ondrej , Sykes, Matthew J. , Callen, David F. , Abell, Andrew D. . "Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors."
กรุงเทพมหานคร : Nanyang Technological University, Singapore, 2556. Print. Pehere, Ashok D. , Pietsch, Markus , Gütschow, Michael , Neilsen, Paul M. , Pedersen, Daniel Sejer , Nguyen, Steven , Zvarec, Ondrej , Sykes, Matthew J. , Callen, David F. , Abell, Andrew D. . Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors. กรุงเทพมหานคร : Nanyang Technological University, Singapore; 2556.
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