Please use this identifier to cite or link to this item: http://localhost:8080/xmlui/handle/123456789/3971
Title: Advanced Glycation End-products (AGE) Trapping Agents: Design and Synthesis of Nature Inspired Indeno[2,1-c]Pyridinones
Authors: Anaga, N
Basavaraja, D
Abraham, B
Nisha, P
Varughese, S
Jayamurthy, P
Sasidhar, B S
Keywords: glycation end-products
metabolic disorders
AGE inhibitors
indeno[2,1-c]pyridinones
methylglyoxal trapping
Issue Date: Dec-2020
Publisher: Elsevier
Citation: Bioorganic Chemistry;105:104375
Abstract: Advanced glycation end products (AGEs) are implicated to be the key players in most of the diabetic complications. The AGE’s interfere with the proteins heterogeneously, thereby rendering denaturation and the consequent loss of function and accumulation. Thus, a novel natural product inspired indeno[2,1-c]pyridinone (4a-4ad) molecular templates with AGE’s trapping potential was designed through scaffold hopping approach and synthesized via facile two-step synthetic route. Amongst the tested indeno[2,1-c]pyridinone hybrids, 4i, 4x and 4aa exhibited excellent efficiency in trapping the AGE’s. The percentage of antiglycation is measured by the analytical model system, i.e. via MG trapping capacity; here the compounds 4i, 4x and 4aa with 50.03%, 69.58%, and 93.37% respectively has displayed promising efficiency. In particular, 4aa demonstrated better activity than the positive control aminoguanidine (79.82%). The in-vitro toxicity of compounds was tested on L6 rat skeletal muscle cell lines revealed that none of the compounds showed any significant toxicity at concentrations up to 1000 μM.
URI: https://doi.org/10.1016/j.bioorg.2020.104375
http://hdl.handle.net/123456789/3971
Appears in Collections:2020

Files in This Item:
File Description SizeFormat 
Advanced glycation end-products (AGE) trapping agents_AnagaN_Bioorganic Chemistry.pdf
  Restricted Access
1.8 MBAdobe PDFView/Open Request a copy


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.