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Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors

หน่วยงาน Central Drug Research Institute (CDRI), India

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ชื่อเรื่อง : Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors
นักวิจัย : Arora, Inderpreet , Kashyap, V K , Singh, A K , Dasgupta, Arunava , Kumar, Brijesh , Shaw, A K
คำค้น : Synthesis and Biological evaluation , Bicyclic Iminosugar Hybrids , Conformational constraint , Selectivity of α-glucosidase
หน่วยงาน : Central Drug Research Institute (CDRI), India
ผู้ร่วมงาน : -
ปีพิมพ์ : 2557
อ้างอิง : Organic & Biomolecular Chemistry, 2014, 12(35):6855-68 , http://hdl.handle.net/123456789/1417
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : CSIR-CDRI Communication No. 8730
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Principle guided design of glycan processing enzyme inhibitors involves embedding aromatic group onto charge and shape mimics. Intramolecular azide-alkyne cycloaddition was used as a simple and versatile strategy for the synthesis of novel condensed bicyclic triazoles from carbohydrate derived Perlin aldehydes. These newly synthesised molecules were evaluated for glycosidase inhibition against 11 commercially available enzymes and were found to posess significant affinity (micromolar range) as well as high degree of selectivity for α-glucosidases. Conformational restriction was identified as an important tool to customize the selectivity of enzyme inhibition by five-membered iminosugar

บรรณานุกรม :
Arora, Inderpreet , Kashyap, V K , Singh, A K , Dasgupta, Arunava , Kumar, Brijesh , Shaw, A K . (2557). Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors.
    : Central Drug Research Institute (CDRI), India.
Arora, Inderpreet , Kashyap, V K , Singh, A K , Dasgupta, Arunava , Kumar, Brijesh , Shaw, A K . 2557. "Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors".
    : Central Drug Research Institute (CDRI), India.
Arora, Inderpreet , Kashyap, V K , Singh, A K , Dasgupta, Arunava , Kumar, Brijesh , Shaw, A K . "Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors."
    : Central Drug Research Institute (CDRI), India, 2557. Print.
Arora, Inderpreet , Kashyap, V K , Singh, A K , Dasgupta, Arunava , Kumar, Brijesh , Shaw, A K . Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors. : Central Drug Research Institute (CDRI), India; 2557.