TITLE:
Synthesis and PAMPA Permeability Assay of New Sulfonyl Hydrazone Derivatives
AUTHORS:
Luiz Felipe Schmitz de Souza, Tiago Tizziani, Larissa Sens, Dalila Venzke, Inês Maria Costa Brighente, Moacir Geraldo Pizzolatti, Ricardo José Nunes
KEYWORDS:
Sulfonyl Hydrazones, PAMPA Permeability, Organic Synthesis, Medicinal Chemistry
JOURNAL NAME:
Journal of Biosciences and Medicines,
Vol.7 No.9,
September
20,
2019
ABSTRACT: This work describes the synthesis of seven new sulfonyl hydrazones, which were proposed from the general structure of acyl hydrazones and 2,4-dinitrosulfonamides. Sulfonyl hydrazones are a class of compounds known to exhibit a wide range of biological activity. In this sense, the study of the pharmacokinetic properties of the bioactive molecules is of extreme importance; therefore, in this article the permeability of these compounds with in vitro PAMPA assay mimetizing the permeability through the gastrointestinal tract as well as lipophilicity through miLogP was investigated. All compounds presented good permeability results; it was possible to make a structure-activity relationship with the obtained results and a comparison between the results.