Synthesis and biological study of novel FELL analogs containing L- or d-tyr instead of l-phe in the N-terminus

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creativework.keywordsAnalgesic activity, Anti-inflammatory activity, Carrageenan-induced paw edema test, FELL analogs, Paw-pressure test
creativework.publisherElsevier B.V.en
dc.contributor.authorBorisova B.
dc.contributor.authorNocheva H.
dc.contributor.authorZlatanova-Tenisheva H.
dc.contributor.authorLaronze-Cochard M.
dc.contributor.authorGérard S.
dc.contributor.authorDanalev D.
dc.date.accessioned2026-01-20T13:58:04Z
dc.date.accessioned2026-01-20T15:55:09Z
dc.date.available2026-01-20T13:58:04Z
dc.date.available2026-01-20T15:55:09Z
dc.date.issued2025-01-01
dc.description.abstractThe high prevalence of pain affecting millions of people worldwide made it a major health problem. At the same time often, inflammation is closely associated to the pain. Thus, creation of molecules with a double effect is a good alternative to the currently existing in the medicinal practice non-steroidal medications. Herein, some modifications in the N- and C-terminus of the tetrapeptide FELL with proven anti-inflammatory properties are performed and the newly synthesized compounds are tested for both analgesic and anti-inflammatory potential. The analgesic and anti-inflammatory activity of the newly synthesized molecules was investigated using Paw-pressure and Carrageenan-Induced Paw Edema tests, respectively, on experimental animals. The results showed a certain “discrepancy” between the analgesic and the anti-inflammatory effects of the newly synthesized substances. Newly synthesized BB9 and BB15, L-Tyr containing C-terminal amide and free acid, respectively, exhibit a more significant analgesic activity compared to those of parent molecules BB1 and BB11, containing L-Phe in the N-terminus. Moreover, taking into account the obtained results for the compounds BB10 and BB16, the preferable substitution is L-Tyr, instead of D-Tyr. It could be concluded that the aromatic OH-function is probably important for the connection with the opioid and cannabinoid receptors. However, the designed structural modifications did not lead to improvement in anti-inflammatory effect compared to those of parent molecules. Moreover, in a context of the positive finding is that all modifications done save the hydrolytic stability of the molecules.
dc.identifier.doi10.1016/j.crbiot.2025.100332
dc.identifier.issn2590-2628
dc.identifier.scopusSCOPUS_ID:105014783238en
dc.identifier.urihttps://rlib.uctm.edu/handle/123456789/1889
dc.language.isoen
dc.source.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=105014783238&origin=inward
dc.titleSynthesis and biological study of novel FELL analogs containing L- or d-tyr instead of l-phe in the N-terminus
dc.typeArticle
oaire.citation.volume10
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