The elaboration of some N-alkylated pyrazole-tetrazole derivatives is reported. The structures of the newly ones are verified using NMR and FTIR spectroscopies, mass spectrometry as well as elemental analysis. Their potencies to inhibit the alpha-amylase enzyme were evaluated using spectrophotometric method and the obtained results showed that some of them were extremely potent with respect to the used positive control. The structure activity relationship showed that the alpha-amylase inhibition activity depends on the alkylation position as well as the nature of the alkyl moiety and the alkylation at the N1 position with a donor group improves the alpha-amylase inhibition activity. Docking study was also performed and the obtained results support the experimental results in the case of the alkylation position effect. These findings suggest that the molecules reported in this study may be used as good drug candidate to treat Type 2 diabetes.
机构:
Women Univ, Dept Zool, Fac Life Sci, Multan 66000, Punjab, PakistanUniv Okara, Dept Chem, Okara 56300, Punjab, Pakistan
Sarfraz, M.
Shah, S. A. Ali
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Univ Teknol MARA UiTM, Atta ur Rahman Inst Nat Prod Discovery, Bandar Puncak Alam 42300, Selangor Darul, Malaysia
Univ Teknol MARA UiTM, Fac Pharm, Bandar Puncak Alam 42300, Selangor Darul, MalaysiaUniv Okara, Dept Chem, Okara 56300, Punjab, Pakistan
机构:
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Wei Li
Jiuhui Li
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Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Jiuhui Li
Hongfeng Shen
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Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Hongfeng Shen
Jiagao Cheng
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Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Shanghai Collaborative Innovation Center for Biomanufacturing TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Jiagao Cheng
Zhong Li
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Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Shanghai Collaborative Innovation Center for Biomanufacturing TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Zhong Li
Xiaoyong Xu
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Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology
Shanghai Collaborative Innovation Center for Biomanufacturing TechnologyShanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology