Design,synthesis, neuroprotective,antibacterial activities and docking studies of novel thieno[2,3-d]pyrimidine-alkyne Mannich base and oxadiazole hybrids |
| |
Authors: | Settypalli Triloknadh Chunduri Venkata Rao Kerru Nagaraju Nallapaneni Hari Krishna Chintha Venkata Ramaiah Wudayagiri Rajendra Daggupati Trinath Yeguvapalli Suneetha |
| |
Institution: | 1. Department of Chemistry, Sri Venkateswara University, Tirupati 517502, Andhra Pradesh, India;2. Department of Zoology, Sri Venkateswara University, Tirupati 517502, Andhra Pradesh, India |
| |
Abstract: | A series of thieno2,3-d]pyrimidine alkyne Mannich base derivatives (7a-e, 8a-e) and thieno2,3-d]pyrimidine 1,3,4-oxadiazole derivatives (9a-e, 10a-e) have been synthesized and evaluated for their neuroprotective and neurotoxicity activities where 9a, 10d displayed good neuroprotection 10.6 and 11.88?µg/mL respectively against the H2O2 induced cell death at the EC50 values and 9b, 9d showed respective toxic effects on PC12 cells at CC50 86.12 and 94.16?µg/mL. Compounds 9a, 9e, 10a and 10b showed strong antibacterial activity against two gram positive (S. aureus, B. subtilis) and two gram-negative strains (E. coli, P. aeruginosa) and showed good binding affinities with C(30) carotenoid dehydrosqualene synthase, Gyrase A and LpxC. This is the first report for the demonstration of thieno2,3-d] pyrimidine derivatives as promising neuroprotective agents against H2O2 induced neurotoxicity on PC12 cells. |
| |
Keywords: | Alkyne Mannich base 1 3 4-Oxadiazole Neuroprotective Neurotoxicity Antibacterial activity Molecular docking |
本文献已被 ScienceDirect 等数据库收录! |
|