Medicinal and Process Chemistry Division, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
Division of Toxicology and Experimental Medicine, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
Bioorg Med Chem Lett. 2019 Jan 1;29(1):66-72. doi: 10.1016/j.bmcl.2018.11.005. Epub 2018 Nov 8.
A series of novel Benzofuran-tetrazole derivatives were successfully synthesised by integrating multicomponent Ugi-azide reaction with the molecular hybridization approach. Interestingly, a number of synthesized derivatives (5c, 5d, 5i, 5l, 5q and 5s) exhibited significant reduction of aggregation of "human" amyloid beta peptide, expressing on transgenic Caenorhabditis elegans (C. elegans) strain CL4176. Further, in silico docking results have evidenced the exquisite interaction of active compounds with the help of TcAChE-E2020 complex. These findings underscore the potential of these hybrids as lead molecules against Alzheimers's disease.
通过将多组分 Ugi-叠氮反应与分子杂交方法相结合，成功合成了一系列新型苯并呋喃-四唑衍生物。有趣的是，许多合成的衍生物（5c、5d、5i、5l、5q 和 5s）显著减少了在转基因秀丽隐杆线虫（C. elegans）CL4176 菌株上表达的“人”淀粉样β肽的聚集。此外，通过与 TcAChE-E2020 复合物的相互作用，计算机对接结果证明了活性化合物的精确相互作用。这些发现强调了这些杂种作为针对阿尔茨海默病的潜在先导分子的潜力。
