Aspasia Papadaki-Valiraki

Synthesis and anti-myxovirus activity of some novel N,N'-disubstituted thioureas

Abstract A series of new N,N ′-disubstituted thioureas were prepared and evaluated in vitro for their activity against myxoviruses. Compound N -[4-(3-propoxy-1 H -1,2,4-triazol-1-yl)phenyl]- N ′-(2-pyrazinyl)thiourea 5d exhibited specific activity against respiratory syncytial virus in HeLa cells. Compounds N -(1-adamantanyl)- N ′-[4-(3-ethoxy-1 H -1,2,4-triazol-l-yl)phenyl]thiourea 5g and N -(1-adamantanyl)- N ′-[4-(3-propoxy-1 H -1,2,4-triazol-1-yl)phenyl]thiourea 5h proved active against influenza A in Madin-Darby canine kidney (MDCK) cells and respiratory syncytial virus in HeLa cells.

Synthesis and antiviral activity of some new 1H-1,2,4-triazole derivatives

Abstract A series of new 1 H -1,2,4-triazole derivatives was synthesised and evaluated in vitro for activity against various DNA and RNA viruses. Compounds 1-benzyl-5-(4-methylphenyl)-3-(2-pyrazinyl)-1 H -1,2,4-triazole 2b , 1-benzyl-5-(3-methylphenyl)-3-(2-pyrazinyl)-1 H -1,2,4-triazole 2c and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1 H -1,2,4-triazole 4h proved active against reovirus-1, and compounds 1-[(2-hydroxyethoxy)methyl]-5-phenyl-3-(2-pyrazinyl)-1 H -1,2,4-triazole 4f and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1 H -1,2,4-triazole 4h against parainfluenza-3 virus, in Vero cells at concentrations that were 5- to 40-fold lower than the cytotoxic concentration required to alter normal cell morphology.

Medicinal Chemistry: Synthesis and Pharmacochemical Investigation of Some Novel 1, 2, 4‐4H‐triazoles with Potential Antiviral Activity

We report the synthesis of some mercaptotriazole derivatives in an effort to discover underlying structural requirements for antiviral activity. A preliminary antiviral study was performed and the contribution of the compounds to free radical processes was investigated. Because lipophilicity influences both biological activity and antioxidant potential we calculated lipophilicity and attempted to correlate this with antioxidant activity.

Use of reversed-phase high-performance liquid chromatography in lipophilicity studies of 9H-xanthene and 9H-thioxanthene derivatives containing an aminoalkanamide or a nitrosoureido group : comparison between capacity factors and calculated octanol-water partition coefficients

Abstract The lipophilicity of 9 H -xanthene and 9 H -thioxanthene derivatives, containing either a basic alkanamide or a nitrosoureido group, was studied by means of reversed-phase high-performance liquid chromatography using an octadecylsilane stationary phase, methanol as organic modifier and n -decylamine as a masking agent. Correlation of the extrapolated capacity factors with log P values calculated according to Rekkers fragmental system showed an excellent parallelism between HPLC and the octanol-water partition system and permitted the generation of a hydrophobic fragmental constant for the nitrosoureido group. Tetrahydrofuran was also tried as an organic modifier but without satisfactory results.

High-performance liquid chromatography in stability studies of an organophosphorus insecticide in free form and after formulation as emulsifiable conce

Abstract DCPE [α-(diethoxyphosphinoximino)dicyclopropylmethane] is an organophosphorus compound with good insecticidal activity. It is a yellow oily liquid, p

Synthesis and antifungal activity of some alkynylthio compounds

Abstract Some 4-( p -alkoxyphenylthio)but-2-yn-yl-amine hydrochlorides and 4-( p -alkoxyphenylthio)prop-1-yn-yl-iodides were prepared and tested for their antifungal activity. All the tested compounds were active in inhibiting the growth of 4 fungal types. The iodine compounds were the more effective.