Artikel: Design, Synthesis, and Biological Evaluation of 4,4'-Difluorobenzhydrol Carbamates as Selective M
Pharmaceuticals (Basel, Switzerland)
2022 Band 15, Heft 2
Abstract: Due to their important role in mediating a broad range of physiological functions, muscarinic acetylcholine receptors (mAChRs) have been a promising target for therapeutic and diagnostic applications alike; however, the list of truly subtype-selective ... ...
| Abstract | Due to their important role in mediating a broad range of physiological functions, muscarinic acetylcholine receptors (mAChRs) have been a promising target for therapeutic and diagnostic applications alike; however, the list of truly subtype-selective ligands is scarce. Within this work, we have identified a series of twelve 4,4'-difluorobenzhydrol carbamates through a rigorous docking campaign leveraging commercially available amine databases. After synthesis, these compounds have been evaluated for their physico-chemical property profiles, including characteristics such as HPLC-logD, tPSA, logBB, and logPS. For all the synthesized carbamates, these characteristics indicate the potential for BBB permeation. In competitive radioligand binding experiments using Chinese hamster ovary cell membranes expressing the individual human mAChR subtype |
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| Sprache | Englisch |
| Erscheinungsdatum | 2022-02-18 |
| Erscheinungsland | Switzerland |
| Dokumenttyp | Journal Article |
| ZDB-ID | 2193542-7 |
| ISSN | 1424-8247 |
| ISSN | 1424-8247 |
| DOI | 10.3390/ph15020248 |
| Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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