N-[4-(Dimethyl­amino)­benzyl­idene]-4H-1,2,4-triazol-4-amine

The title compound, C11H13N5, is a Schiff base synthesized by the reaction of 4-amino-4H-1,2,4-triazole and 4-(dimethyl­amino)­benzaldehyde. The dihedral angle between the benzene and triazole rings is 43.09 (11)°. The crystal structure displays weak C—H⋯N inter­actions

Crystal structure of 4-({(1E,2E)-3-[3-(4-fluorophenyl)- 1-isopropyl-1H-indol-2-yl]allylidene}amino)-5- methyl-1H-1,2,4-triazole-5(4H)-thione

The title compound, C23H22FN5S, exists in a trans conformation with respect to the methene C C and the acyclic N C bonds. The 1,2,4-triazole-5(4H)-thione ring makes dihedral angles of 88.66 (9) and 84.51 (10)�, respectively, with the indole and benzene rings. In the crystal, molecules are linked by pairs of N— H� � �S hydrogen bonds, forming inversion dimers with an R2 2(8) ring motif. The dimers are linked via C—H� � �� interactions, forming chains along [110]. The chains are linked via �—� interactions involving inversion-related triazole rings [centroid–centroid distance = 3.4340 (13) A ° ], forming layers parallel to the ab plane

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

The lipophilicity of 9H-xanthene and 9H-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 Rekker's 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. © 1993

Synthesis of N‐(9H‐Xanthen‐9‐yl)aminoalkanamide and N‐(9H‐Thioxanthen‐9‐yl)aminoalkanamide Derivatives and their in vitro Evaluation as Potential Intercalators and Antitumor Drugs

A series of new N‐(9H‐xanthen‐9‐yl)aminoalkanamide and N‐(9H‐thio‐xanthen‐9‐yl)aminoalkanamide derivatives was synthesized and evaluated as potential intercalators by measuring their DNA binding affinity. They were also tested for cytotoxic activity against L1210. The results suggest that the cytotoxicity of these molecules was not due to an intercalating mechanism. Copyright © 1994 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinhei

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

A series of new 1H-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)-1H-1,2,4-triazole 2b, 1-benzyl-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 2c and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-1,2,4-triazole 4h proved active against reovirus-1, and compounds 1-[(2-hydroxyethoxy)methyl]-5-phenyl-3-(2-pyrazinyl)-1H-1,2,4-triazole 4f and 1-[(2-hydroxyethoxy)methyl]-5-(3-methylphenyl)-3-(2-pyrazinyl)-1H-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. © 1994

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

A series of new N,N′-disubstituted thioureas were prepared and evaluated in vitro for their activity against myxoviruses. Compound N-[4-(3-propoxy-1H-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-1H-1,2,4-triazol-l-yl)phenyl]thiourea 5g and N-(1-adamantanyl)-N′-[4-(3-propoxy-1H-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. © 1994