[Research on a substance with antiviral activity. XXI. Preparation and antiherpes activity of 2-acylamino-3,5-dichloropyridine].
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Biomedical subjects
Publications and source records attributed to A Ferranti.
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A few hydrazones holding benzofuran and 1H-indene moieties were synthesized and screened for in vitro antimicrobial activity. The most active N'-(5-nitro-2-furoyl)-N2-(3-chloro-1H-indenyl-2-methylene)hydrazine (II c) showed higher activity than nitrofurantoin against some microorganisms, especially Pseudomonas aeruginosa.
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Some 1-(5'-nitrofurfuryl)-5-halouracils were synthetized and tested in vitro for antimicrobial activity. N.M.R. spectra of the compounds proved 1-substitution on uracil.
Derivatives of different chemical structures, namely hydrazones of aromatic compounds and bis-homoanalogues of pyrimidine and purine nucleosides, have been investigated for inhibiting activity on Herpes simplex virus infection of human HEp-2 cell cultures. Some thiosemicarbazones, nucleoside analogues and guanylhydrazones proved active [compounds (I), (II b), (II c), (III), (IV a), (IV b), (V a), (V b); Fig. 1]. An increase in the number of guanylhydrazone chains linked to a fluorene structure [from 1 to 3: compounds (II a), (II b) and (II c)] increased the "activity index" (i.e., toxic versus active concentrations: Table II). Further in vitro investigations have been carried out on bis-guanylhydrazone of 1-phenyl-2-chloro-3,7-diformylindole (I) and it was found that its activity is of the order of 1 microgram per ml (Fig. 3). The compound completely blocks low multiplicity infections while it only blocks cytopathogenicity, not viral replication, in high multiplicity infections.
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