Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Phenylbenzohydrazides Obtained from Isatoic Anhydride Present Anti-Inflammatory Activity in Vivo and in Vitro

Version 1 : Received: 27 October 2022 / Approved: 31 October 2022 / Online: 31 October 2022 (01:02:02 CET)

A peer-reviewed article of this Preprint also exists.

Paiva, J.P.B.; Cordeiro, M.S.; França, P.R.C.; Branco, L.O.P.; Santos, I.S.; Reis, N.F.; Pimentel, P.P.; Giorno, T.B.S.; Lima, E.C.; Fernandes, P.D. Phenylbenzohydrazides Obtained from Isatoic Anhydride Present Anti-Inflammatory Activity In Vivo and In Vitro. Biomolecules 2022, 12, 1901. Paiva, J.P.B.; Cordeiro, M.S.; França, P.R.C.; Branco, L.O.P.; Santos, I.S.; Reis, N.F.; Pimentel, P.P.; Giorno, T.B.S.; Lima, E.C.; Fernandes, P.D. Phenylbenzohydrazides Obtained from Isatoic Anhydride Present Anti-Inflammatory Activity In Vivo and In Vitro. Biomolecules 2022, 12, 1901.

Abstract

Background: Despite the existence of a wide variety of anti-inflammatory drugs, the vast majority are classified as steroidal or non-steroidal. Both classes with many side effects that limit usage. Thus, the search for new molecules with anti-inflammatory potential is still important. Methods: Five phenylbenzohydrazides were synthetized and evaluated in pre-clinical models of acute inflammation in vivo and in vitro. Results: Substances significantly reduced cell migration induced by carrageenan. It was also observed an intense inhibition in protein extravasation and cytokines (IL-6, IL-1β, and TNF-α) production as well as nitric oxide reduction. INL-11 demonstrated to be the most potent since the reduction was significant even when compared with dexamethasone. In vitro INLs also reduced cytokines and NO production and iNOS activity. INL-11 was the most effective in reducing cell migration in vitro. Conclusions: our data suggest that these substances are suitable for further development to new series of compounds that could lead to new hits and future drug prototypes for anti-inflammatory conditions.

Keywords

Phenylbenzohydrazides; isatoic anhydride; inflammation; anti-inflammatory substance; carrageenan-induced inflammation; nitric oxide

Subject

Medicine and Pharmacology, Pharmacology and Toxicology

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