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Catalyst Free Synthesis of N-(1,3-Dioxoisoindolin-4-Yl)Acetamide Derivatives using Water and their Biological Evaluation | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X

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Abstract

Catalyst Free Synthesis of N-(1,3-Dioxoisoindolin-4-Yl)Acetamide Derivatives using Water and their Biological Evaluation

Author(s): Rajesh Kumar Rapolu, Ravi Kumar Sadineni, Raja Sekhar Bhupathi, VVNKV Prasada Raju, Murthy Chavali, N Srinivasu, Varimadugu Aruna, Chaitanya Mulakayala, Naveen Mulakayala

Green and eco-friendly synthesis of N-(1,3-dioxo-2-phenylisoindolin-4-yl)acetamide derivatives were developed by reacting N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide with different aliphatic aromatic and heterocyclic amines under catalyst free conditions using water as a eco-friendly solvent. These reactions involve simple work-up with high yields. All the compounds were evaluated activity against TNF-α in vitro. Compound 6d showed potent activity against TNF-α with 78% inhibition at 10 μM concentration. Therefore, these compounds found to be valuable leads against TNF-α.


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