Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Novel Regioisomeric Analogues of Naphthyl-N-Acylhydrazone Derivatives and Their Anti-Inflammatory Effects

Version 1 : Received: 13 October 2022 / Approved: 14 October 2022 / Online: 14 October 2022 (14:21:35 CEST)

A peer-reviewed article of this Preprint also exists.

Salomé, D.C.; Freitas, R.H.C.N.; Fraga, C.A.M.; Fernandes, P.D. Novel Regioisomeric Analogues of Naphthyl-N-Acylhydrazone Derivatives and Their Anti-Inflammatory Effects. Int. J. Mol. Sci. 2022, 23, 13562. Salomé, D.C.; Freitas, R.H.C.N.; Fraga, C.A.M.; Fernandes, P.D. Novel Regioisomeric Analogues of Naphthyl-N-Acylhydrazone Derivatives and Their Anti-Inflammatory Effects. Int. J. Mol. Sci. 2022, 23, 13562.

Abstract

Background: When homeostasis is disturbed it can occur a pathological event named inflammation. The main drugs used in the treatment consist of the non-steroidal and steroidal anti-inflammatory drugs. However, the side effects remain an obstacle during the treatments. In this work we aimed to evaluate three new regioisomers analogues of naphthyl-N-acylhydrazone derivatives. Methods: Acute models of inflammation in vivo (formalin-induced licking and carrageenan-induced inflammation) as well as in vitro were used to evaluate the effects of LASSBio-2039, LASSBio-2040, and LASSBio-2041. Results: All three substances (at 1, 10 or 30 µmol/kg) presented significant effect in the in vivo model reducing leukocyte migration, nitric oxide (NO) and interleukin-1β production. It was observed that only LASSBio-2039 significantly reduced cell migration in vitro. None of the LASSBios did affect inducible nitric oxide synthase activity nor presented NO scavenger effect. It was not observed any toxic effect neither in vivo nor in vitro. The new regioisomers analogues of naphthyl-N-acylhydrazone derivatives presented a significant anti-inflammatory activity suggesting LASSBio-2039 with a direct effect in leukocytes migratory capacity. Conclusions: Taken together the data indicate that these substances present promising effect for de development a prototype for new drugs.

Keywords

anti-inflammatory substance; N-acylhydrazone; naphthyl-N-acylhydrazone; LASSBio-1524 analogues

Subject

Biology and Life Sciences, Biochemistry and Molecular Biology

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