Article ; Online: Evaluation of honokiol, magnolol and of a library of new nitrogenated neolignans as pancreatic lipase inhibitors.
2023 Volume 134, Page(s) 106455
Abstract: Obesity is a complex disease defined as an excessive amount of body fat. It is considered a risk factor for several pathologies; therefore, there is an increasing interest in its treatment. Pancreatic lipase (PL) plays a key role in fat digestion, and ... ...
Abstract | Obesity is a complex disease defined as an excessive amount of body fat. It is considered a risk factor for several pathologies; therefore, there is an increasing interest in its treatment. Pancreatic lipase (PL) plays a key role in fat digestion, and its inhibition is a preliminary step in the search for anti-obesity agents. For this reason, many natural compounds and their derivatives are studied as new PL inhibitors. This study reports the synthesis of a library of new compounds inspired by two natural neolignans, honokiol (1) and magnolol (2) and bearing amino or nitro groups linked to a biphenyl core. The synthesis of unsymmetrically substituted biphenyls was achieved through an optimisation of the Suzuki-Miyaura cross-coupling reaction followed by the insertion of allyl chains, thus furnishing the O- and/or N-allyl derivatives, and finally, a sigmatropic rearrangement yielding in some cases, the C-allyl analogues. Magnolol, honokiol and the twenty-one synthesised biphenyls were evaluated for their in vitro inhibitory activity toward PL. Three compounds (15b, 16 and 17b) were more effective inhibitors than the natural neolignans (magnolol IC |
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MeSH term(s) | Lignans/chemistry ; Biphenyl Compounds/pharmacology ; Biphenyl Compounds/chemistry |
Chemical Substances | magnolol (001E35HGVF) ; honokiol (11513CCO0N) ; diphenyl (2L9GJK6MGN) ; Lignans ; Biphenyl Compounds |
Language | English |
Publishing date | 2023-03-06 |
Publishing country | United States |
Document type | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 120080-x |
ISSN | 1090-2120 ; 0045-2068 |
ISSN (online) | 1090-2120 |
ISSN | 0045-2068 |
DOI | 10.1016/j.bioorg.2023.106455 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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