Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents |
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Authors: | Atul Kumar Siddharth Sharma Vishwa Deepak Tripathi Ram Awatar Maurya Swayam Prakash Srivastava Gitika Bhatia AK Tamrakar Arvind Kumar Srivastava |
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Institution: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow 226 001, India;2. Biochemistry Division, Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow 226 001, India |
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Abstract: | A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipid and TG modulating activity. All these compounds were evaluated in various in vitro models of diabetes to know the possible mechanism of their antihyperglycemic action. Interestingly, compounds 3a–r (diaryl substitution) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds 5a–d (acid substituted) have shown significant glycogen phosphorylase activity. |
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