Leena Sruthi Sudheendran, Akhir Abdul, Saxena Deepanshi, Maitra Rahul, Chopra Sidharth, Deepthi Ani
Department of Chemistry, University of Kerala Kariavattom Trivandrum-695581 India
Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute Sector 10, Janakipuram Extension, Sitapur Road Lucknow-226031 Uttar Pradesh India
RSC Med Chem. 2023 May 3;14(6):1165-1171. doi: 10.1039/d3md00017f. eCollection 2023 Jun 22.
The synthesis of sixteen tryptanthrin appended dispiropyrrolidine oxindoles, employing [3 + 2] cycloaddition of tryptanthrin-derived azomethine ylides with isatilidenes, and their detailed antibacterial evaluation is described. The antibacterial activities of the compounds were evaluated against ESKAPE pathogens and clinically relevant drug-resistant MRSA/VRSA strains, from which the bromo-substituted dispiropyrrolidine oxindole 5b (MIC = 0.125 μg mL) was found to be a potent molecule against ATCC 29213 with a good selectivity index.
描述了通过色胺酮衍生的甲亚胺叶立德与异亚吲哚酮的[3 + 2]环加成反应合成十六种色胺酮连接的双螺吡咯烷氧化吲哚及其详细的抗菌评估。评估了这些化合物对ESKAPE病原体和临床相关耐药性MRSA/VRSA菌株的抗菌活性，从中发现溴代双螺吡咯烷氧化吲哚5b（MIC = 0.125 μg mL）是一种对ATCC 29213有效的分子，具有良好的选择性指数。
