The synthesis of several [4,4,3], [4,3,3], and [3,3,3]azapropellanes is reported. Several of the novel amines displayed low-micromolar activities against an amantadine-resistant H1N1 strain, but they did not show activity against an amantadine-sensitive H3N2 strain. None of the tested compounds inhibit the influenza A/M2 proton channel function. Most of the compounds did not show cytotoxicity for MDCK cells.

Azapropellanes with anti-influenza a virus activity / E. Torres, R. Leiva, S. Gazzarrini, M. Rey-Carrizo, M. Frigolé-Vivas, A. Moroni, L. Naesens, S. Vázquez. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 5:7(2014), pp. 831-836. [10.1021/ml500108s]

Azapropellanes with anti-influenza a virus activity

S. Gazzarrini;A. Moroni;
2014

Abstract

The synthesis of several [4,4,3], [4,3,3], and [3,3,3]azapropellanes is reported. Several of the novel amines displayed low-micromolar activities against an amantadine-resistant H1N1 strain, but they did not show activity against an amantadine-sensitive H3N2 strain. None of the tested compounds inhibit the influenza A/M2 proton channel function. Most of the compounds did not show cytotoxicity for MDCK cells.
amantadine; hemagglutinin; influenza; M2 channel; propellane; organic chemistry; drug discovery3003 pharmaceutical science; biochemistry
Settore BIO/04 - Fisiologia Vegetale
2014
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/246261
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