Academic Journal
Design, synthesis and anti-Parkinson's disease bioactivity evaluation of isoquinoline derivatives as potent IDO1/TDO dual inhibitors.
| Τίτλος: | Design, synthesis and anti-Parkinson's disease bioactivity evaluation of isoquinoline derivatives as potent IDO1/TDO dual inhibitors. |
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| Συγγραφείς: | Yang Z; Department of Pharmacy, West China Hospital, Sichuan University, Chengdu 610041, PR China., Lin Z; Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China., Yang C; Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China., Lu R; Department of Pharmacy/Evidence-Based Pharmacy Center, Key Laboratory of Birth Defects and Related Diseases of Women and Children, Children's Medicine Key Laboratory of Sichuan Province, NMPA Key Laboratory for Technical Research on Drug Products In Vitro and In Vivo Correlation, West China Second University Hospital, Sichuan University, Chengdu 610041, PR China. Electronic address: lurunxin@scu.edu.cn., Wu Y; Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China. Electronic address: wyong@scu.edu.cn. |
| Πηγή: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2026 Jul; Vol. 136, pp. 130596. Date of Electronic Publication: 2026 Feb 22. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| Imprint Name(s): | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| Ιατρικοί όροι (MeSH): | Indoleamine-Pyrrole 2,3,-Dioxygenase*/antagonists & inhibitors , Indoleamine-Pyrrole 2,3,-Dioxygenase*/metabolism , Isoquinolines*/pharmacology , Isoquinolines*/chemistry , Isoquinolines*/chemical synthesis , Isoquinolines*/therapeutic use , Enzyme Inhibitors*/chemical synthesis , Enzyme Inhibitors*/pharmacology , Enzyme Inhibitors*/chemistry , Tryptophan Oxygenase*/antagonists & inhibitors , Tryptophan Oxygenase*/metabolism , Parkinson Disease*/drug therapy , Parkinson Disease*/metabolism , Neuroprotective Agents*/chemical synthesis , Neuroprotective Agents*/pharmacology , Neuroprotective Agents*/chemistry , Drug Design*, Animals ; Humans ; Structure-Activity Relationship ; Rats ; Molecular Structure ; Dose-Response Relationship, Drug ; Mice |
| Περίληψη: | Human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) are potential targets for the development of PD according to current research; nevertheless, reports on dual hIDO1/hTDO inhibitors against PD are still lacking. In this study, a series of isoquinoline derivatives were designed, synthesized, and evaluated as novel IDO1/TDO dual inhibitors. Among them, Y-13 showed potent inhibitory activities against both IDO1 (IC (Copyright © 2026. Published by Elsevier Ltd.) |
| Competing Interests: | Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: Anti-inflammatory effects; Isoquinoline derivatives; Neuroprotective effects; Parkinson's disease; Tryptophan-kynurenine pathway |
| Substance Nomenclature: | 0 (Indoleamine-Pyrrole 2,3,-Dioxygenase) 0 (Isoquinolines) 0 (Enzyme Inhibitors) EC 1.13.11.11 (Tryptophan Oxygenase) 0 (Neuroprotective Agents) 0 (IDO1 protein, human) |
| Entry Date(s): | Date Created: 20260224 Date Completed: 20260708 Latest Revision: 20260708 |
| Update Code: | 20260708 |
| DOI: | 10.1016/j.bmcl.2026.130596 |
| PMID: | 41734858 |
| Βάση Δεδομένων: | MEDLINE |
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