مشروع البحث: Design, synthesis and characterization of a novel five-membered heterocyclic derivatives and studying their potential biological activity
| dc.contributor.advisor | Prof. Dr. Hamida Mohamed Abdel-Hamid | |
| dc.contributor.advisor | Prof. Dr. Doaa Ahmed Ghareeb | |
| dc.contributor.advisor | Prof. Dr. Mohammed Salah Ayoup | |
| dc.contributor.advisor | Prof. Dr. Mohamed Nabil Abd Al Moaty | |
| dc.date.accessioned | 2026-01-27T09:10:06Z | |
| dc.date.available | 2026-01-27T09:10:06Z | |
| dc.description | The first part: included 3,5-diaryl-1,2,4-oxadiazole scaffolds 129 and 130 were synthesized and used as ligands to obtain three novel Ag(I) complexes 131-133. The structure of the Ag(I) complexes 131-133 have been confirmed by single crystal X-ray diffraction. Complex 131 has the dinuclear formula [Ag(129)(NO3)]2. 132 and 133 are monomeric complexes having the formula [Ag(130)2(NO3)] and [Ag(130)2]ClO4, respectively. In vitro, trypsin, ALDH2, and iNOS inhibition activities were assessed for the free ligands and their Ag(I) complexes. Interestingly, Ag(I) complexes 131-133 revealed more prominent trypsin inhibitory activity than the ligands 129 and 130. The oxadiazole derivative 130 and its Ag(I) complex 133 showed significant ALDH2 inhibition (45% and 55%, respectively). Complex 133 (IC50 = 35.61 μM) surpassed its 1,2,4-oxadiazole ligand 130 (IC50 = 88 μM) and evidenced the most prominent ALDH2 inhibitory activity. | |
| dc.description.abstract | This thesis includes three chapters: The first chapter is the introduction deals with the role of five-membered heterocyclic compounds especially 1,2,4-oxadiazoles ring in assisting organic synthesis and their biological effects. Nitrogen -containing heterocyclic entities exist in many chemotherapeutic agents. Heterocyclic compounds based on 1,2,4-oxadiazoles ring existed in several drugs. | |
| dc.identifier | 888 | |
| dc.identifier.uri | https://dspace.academy.edu.ly/handle/123456789/1898 | |
| dc.subject | Design, synthesis and characterization of a novel five- | |
| dc.title | Design, synthesis and characterization of a novel five-membered heterocyclic derivatives and studying their potential biological activity | |
| dspace.entity.type | Project | |
| project.endDate | 2025 | |
| project.funder.name | الكيمياء | |
| project.investigator | ربيعة إمحمد العجيلي الاشهب | |
| project.startDate | 2024 | |
| relation.isOrgUnitOfProject | b2e3dee1-ae54-4811-ae6d-5b930f16d76f | |
| relation.isOrgUnitOfProject.latestForDiscovery | b2e3dee1-ae54-4811-ae6d-5b930f16d76f |