HALOGENATED ISONIAZID DERIVATIVES .6. EVALUATION OF ANTI-HSV-1 AND ANTI-HIV-1 IN-VITRO ACTIVITIES OF FLUORINATED ANALOGS

The synthesis and evaluation of antiviral in vitro activity are report ed of some 2'-(1-arylethyl)isonicotinohydrazides (5a-d) and N-(1-aryle thyl)isonicotinohydrazonic acids (6a-d), obtained by reducing fluorina ted acetophenone isonicotinoylhydrazones (2a-d) with sodium cyanoboroh ydride. These INH analogues, along with other ones previously prepared , i.e. benzaldehyde isonicotinoylhydrazones 1, l-1-methoxy-1-(4-pyridy l)-2,3-diaza-1,3-butadienes 3 and -methyl-2-(4-pyridyl)-Delta(2)-1,3,4 -oxadiazolines 4, were assayed for anti-HSV-1 activity on the monoblas toid cell line U937. Only some compounds (1b, 1d, 4d and 4e) displayed a moderate antiherpetic activity. In addition, the reduced compounds 5 and 6, submitted to the anti-HIV-1 screening, did not display signif icant effects in reducing virus-induced cythopathogenicity. The cytoto xicity of all compounds has been assayed on Vero cells and some consid erations in correlation with structure are discussed.