3-Aryl-1-phenyl-1H-pyrazole derivatives as new multitarget directed ligands for the treatment of Alzheimer's disease, with acetylcholinesterase and monoamine oxidase inhibitory properties
| dc.contributor.author | Kumar, Ashwani | |
| dc.contributor.author | Jain, Sandeep | |
| dc.contributor.author | Parle, Milind | |
| dc.contributor.author | Jain, Neelam | |
| dc.contributor.author | Kumar, Parvin | |
| dc.date.accessioned | 2014-03-12T14:01:39Z | |
| dc.date.available | 2014-03-12T14:01:39Z | |
| dc.date.issued | 2013-12-13 | |
| dc.description.abstract | A series of 3-aryl-1-phenyl-1H-pyrazole derivatives was synthesized in good yield and assayed in vitro as inhibitors of the mice acetylcholinesterase (AChE) and two goat liver monoamine oxidase (MAO) isoforms, MAO-A and MAO-B. Most of the compounds demonstrated a good AChE and selective MAO-B inhibitory activities in the nanomolar or low micromolar range. N-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) benzenamine (3e, pIC50 = 4.2) and N-((4-fluorophenyl)-1-phenyl-1H-pyrazole-4-yl) methylene) methanamine (3f, pIC50 = 3.47) were the most potent AChE and highly selective MAO-B inhibitors respectively. Structure activity relationships showed that chloro derivatives were more effective AChE inhibitors as compared to fluoro derivatives while reverse trend was observed in MAO-B inhibitory activity. With the aid of modeling studies, potential binding orientations as well as interactions of the compounds in the AChE and MAO-B active sites were examined. | en |
| dc.identifier.issn | 1611-2156 | |
| dc.identifier.uri | http://hdl.handle.net/2003/32975 | |
| dc.identifier.uri | http://dx.doi.org/10.17877/DE290R-7363 | |
| dc.language.iso | en | |
| dc.relation.ispartofseries | EXCLI Journal ; Vol. 12, 2013 | en |
| dc.subject | Alzheimer’s disease | en |
| dc.subject | 1H-pyrazole | en |
| dc.subject | AChE | en |
| dc.subject | MAO-B | en |
| dc.subject | molecular modeling | en |
| dc.subject.ddc | 610 | |
| dc.title | 3-Aryl-1-phenyl-1H-pyrazole derivatives as new multitarget directed ligands for the treatment of Alzheimer's disease, with acetylcholinesterase and monoamine oxidase inhibitory properties | en |
| dc.type | Text | |
| dc.type.publicationtype | article | |
| dcterms.accessRights | open access | |
| eldorado.dnb.zdberstkatid | 2132560-1 |