Organic Chemistry - Advanced Glycation End-products (AGE) Trapping Agents: Design and Synthesis of Nature Inspired Indeno[2,1-c]pyridinones 

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Advanced Glycation End-products (AGE) Trapping Agents: Design and Synthesis of Nature Inspired Indeno[2,1-c]pyridinones

Anaga Nair, Basavaraja D,  Billu Abraham, P Nisha,  Sunil Varughese, Jayamurthy Purushothaman, Sasidhar B. Somappa*

Advanced glycation end products (AGEs) are implicated to be the key players in most of the diabetic complications. 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%).

Bioorganic Chemistry, 2020, 105, 104375

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