A chalcone was prepared by the reaction of terephthalaldehyde with 3-acetyl-2,5-dimethylthiophene. Treatment of this chalcone with thiosemicarbazide/phenyl hydrazine/guanidine hydrochloride/thiourea afforded the corresponding pyrazoline, pyrazole, and pyrimidine in good yields. All the new compounds have been characterized by IR, 1H-NMR, 13C-NMR, GC-MS and elemental analyses. The anti-bacterial...

In the title hexa-hydro-pyrimidine derivative, C(28)H(42)N(2)O(4)·0.19H(2)O, the 1,3-diazinane ring has a chair conformation with a diequatorial substitution. The asymmetric unit contains one half-organic mol-ecule and a solvent water mol-ecule with occupany 0.095. The mol-ecule lies on a mirror plane perpendicular to [010] which passes through the C atoms at the 2- and 5-positions of the heter...

2-Arylhydrazono-3-oxobutanenitriles 2 was reacted with hydroxylamine hydrochloride to yield amidooxime 3. This was cyclized into the corresponding oxadiazole 4 on refluxing in acetic anhydride. When refluxed in DMF in presence of piperidine, the corresponding 1,2,3-triazoleamine 5 was formed. The latter was acylated to 6 by addition of acetic anhydride while treatment of 5 with malononitrile ga...

A major limitation in triple-helix formation arises from the weak energy of interaction between the third strand and the double-stranded target. We tried to increase the stacking interaction contribution within the third strand by extending the aromatic domain of thymine. We report here the use of 2,4-quinazolinedione as a substitute for thymine in the canonical TA*T triplet. The synthesis and ...

Pipemidic acid, 8-ethyl-5,8-dihydro-5-oxo-2-(1-piperazinyl)-pyrido [2,3-d]pyrimidine-6-carboxylic acid, is a new derivative of piromidic acid. It is active against gram-negative bacteria including Pseudomonas aeruginosa as well as some gram-positive bacteria. Its potency is generally greater than that of piromidic acid and nalidixic acid. Cross-resistance is not observed between pipemidic acid ...

Recent data suggest that SRC family kinases (SFKs) could represent potential therapeutic targets for rhabdomyosarcoma (RMS), the most common soft-tissue sarcoma in children. Here, we assessed the effect of a recently developed selective SFK inhibitor (a pyrazolo[3,4-d]pyrimidine derivative, called SI221) on RMS cell lines. SI221, which showed to be mainly effective against the SFK member YES, s...

This work describes the synthesis and cytotoxic evaluation of thiophene thienopyrimidine derivatives. The investigated compound was subjected to target prediction that indicated its high affinity kinases Janus kinase 2 (JAK2) specifically. Molecular docking screening performed on three different JAK2 proteins downloaded from Protein Data Bank (PDB: 5AEP, 4C62 3ZMM). In vitro inhibitory activity...

General synthetic routes to 4-methyl-5-arylpyrimidines and 5-arylpyrimidines are described. 4-Benzylpyrimidine, 4-methyl-5-phenylpyrimidine, 4-(4-methoxybenzyl)pyrimidine, and 4-methyl-5-(4-methoxyphenyl)pyrimidine have been positively identified as route-specific by-products in the Leuckardt preparations of amphetamine and 4-methoxyamphetamine. Using headspace solid phase microextraction (SPME...