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The conversion of thiocarbonohydrazides to 5-substituted amino-1,3,4-thiadiazolyl-1H-pyrazoles in one-step was achieved via the reaction with tetracyanoethylene (TCNE). In this conversion, TCNE is used as a mediator and/or a building block. The product was conclusively confirmed by spectroscopic data and single crystal X-ray structural analysis.

9 Title compounds of type (III) and 9 of type (V) are prepared; 9 of them are screened for their in vitro antibacterial activities.

The title compounds (III) are efficiently obtained in the reaction of 3-aroyl-1-arylthioureas (I) with butynedioate (II) and screened for their antitumor and antioxidant activities.

A series of novel 3,5-diarylpyrazoline derivatives (III) are synthesized and screened for their anticancer activity in a tubulin polymerization inhibitory assay.

The compounds (III) exhibit remarkable antidepressant activity compared with imipramine and compared with phenobarbital they show a good protection against clonic seizures induced by ip injection of pentylenetetrazol in mice (no yields given).

A variety of novel triazepines, triazines and triazoles fused with a triazole ring are synthesized using the binucleophilic centered title hydrazinotriazolethiol (I) as starting material.

Some of the title thiazepine derivatives show effective antitumor, e.g. (IIIb), and/or antioxidative activities, e.g. (IIIb) and (IIId).

Reaction of diacyl thiocarbohydrazides with dimethyl but-2-ynedioate in refluxing ethanol led to 4-oxa-thiazolidine-5-ylidene-acetates in good yields. Reaction of the newly prepared N-(2-(propan-2-ylidene)hydrazine-carbonothioyl)arylhydrazides with dimethyl but-2-ynedioate gave the corresponding (Z)-methyl-2-arylhydrazide-4-oxo-3-(propan-2-ylideneamino)thiazolidine-5-ylidene)-acetates. The mechanism is dis-cussed. Antitumor and antioxidant activities have been also investigated.

Substituted carboxylic acid hydrazides 1a-d reacted with ethenetetracarbonitril 2 in dimethyl formamide with the formation of diacylhydrazines 4a-d and 5-amino-1-substituted pyrazole-3,3,4-tricarbonitriles 5a-d. On the other hand, 1a-d reacted with diethyl (E)-2,3-dicyanobutenedioate 3 to give oxadiazole derivatives 10a-d and pyrazolone derivatives 11a-d, respectively. The prepared compounds 4a-d, 5a-d and 11a-d were evaluated each for antidepressant activity using tail suspension behavioral despair test and anticonvulsant activity against PTZ induced seizures in mice. Compounds 4a and 4b induced markedly antidepressant activity compared to imipramine, and their activities as antidepressant nearly equal twice the activity of imipramine at 10 mg kg(-1) dose level. On the other hand, compounds 11b, 11a and 11d exhibited remarkable protective effect against clonic seizures induced by i.p. injection of PTZ at a dose level of 20 mg kg(-1). The results of anticonvulsant activity are nearly close to phenobarbital sodium at a dose level of 30 mg kg(-1) and more potent than phenytoin sodium at a dose level of 30 mg kg(-1).

New strategy to develop antiviral agents against HIV and herpes virus from the derivatization of peptide nucleic acid monomers has been described.

2',5'-isoDNA mimic chiral peptide nucleic acid (isoPNA) monomers derived from D- and L-aspartic acids were synthesized. These novel monomers were incorporated in aminoethylglycine peptide nucleic acid (aegPNA) thymine dodecamers, and the hybridization properties to RNA and DNA were demonstrated by UV thermal denaturation.