Synthesis of novel pyrimidine nucleoside analogues owning multiple bases/sugars and their glycosidase inhibitory activity |
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| Authors: | Ravi Kumar Thakur Akansha Mishra KKG Ramakrishna Rohit Mahar Sanjeev K Shukla AK Srivastava Rama P Tripathi |
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| Institution: | 1. Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India;2. Biochemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India;3. Sophisticated Analytical Instrument Facility, CSIR-Central Drug Research Institute, Lucknow 226031, India;4. Academy of Scientific & Innovative Research (AcSIR), New Delhi 110001, India |
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| Abstract: | A series of novel nucleoside analogues having dual bases (pyrimidine and triazole) and sugars have been synthesized by CuAAC reaction of azido sugars with propynylated pyrimidines. These compounds were evaluated for their in vitro α-glucosidase inhibitory activity. In this series, compounds 4b, 4d, 8a, 8b, 8c, 8e, 8g, 8h, and 8i exhibited very good inhibition of α-glucosidase enzyme. Nucleoside analogues 8a, 4b, 8h, and 8c displayed 47.4%, 41.8%, 39.4%, and 34.6% inhibition, respectively, comparable to the standard drug acarbose (53.4%). |
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| Keywords: | Pyrimidine nucleosides Triazoles Azido sugars α-Glucosidase |
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