Department of Applid Chemistry

4-(4-Aminophenyl)-1-thia-4-azaspiro[4.5]decan-3-one 1 was prepared and allowed to react with nitrogen nucleophiles to give the corresponding hydrazones 2–4. Further, compound 1 underwent diazotization and afforded the parallel hydrazono derivative 5; moreover, compound 1 refluxed with active methylene derivatives yielded the corresponding aminospirothiazolo pyridine–carbonitrile derivative 6 and spirothiazolopyridinone–carbonitrile derivative 7. Condensation of spirothiazolidine 1 with 4-chlorobenzaldehyde gave the corresponding spiro arylidiene derivative 8, which was utilized as a component of Micheal addition to react with excess of nitrogen nucleophiles to yield novel ring frameworks 4-(3′-(4-chlorophenyl)–spiro [cyclohexane-1,5′-pyrazolo[3,4-d]thiazol]-6′(1′H)-yl)aniline (9) and 4-(3′-(4-chlorophenyl)-6′H- spiro[cyclohexane-1,5′-thiazolo[5,4-d]isoxazol]-6′-yl)aniline (10). Finally, when spirothiazolo pyridinone–carbonitrile derivative 7 sodium salt generated in situ was reacted...

Reaction of imidazolidineiminothiones with some amino acids methyl ester afforded imidazopyrazine and imidazolidine derivatives. Some of obtained products were synthesized by nano technology; where this method reduces the reaction time significantly. The evaluation of biological activity of some selected compounds was carried out and some of synthesized compounds displayed anticancer activity.

Amino thiophenecarboxylates 1a-d were heated with thiourea to afford 2-thioxothieno[3,2-d]pyrimidin-4(1H)-ones 2a-d. 2-(Methylthio)thieno[3,2-d]pyrimidin-4(1H)-ones 3a-d were synthesized by alkylation of substituted 2-thioxo derivatives 2a-d with methyl iodide. Compounds 3a-d were treated with (2-acetoxyethoxy)methyl bromide to afford 4a-d which were deacetylated to afford 5a-d. The anti-HBV activity of selected compounds was studied.

Peptide nucleic acids (PNAs) are oligonucleotide analogues, in which the entire phosphodiester pentose backbone of DNA or RNA is replaced by a polyamide or peptide backbone (Fig. 1) (1). The complete replacement of the ribose phosphate backbone with an artificial pseudopeptide backbone resulted in the remarkably improved binding to complementary nucleic acid sequences occurring with both high affinity and high selectivity. The most widely known PNAs are based on a N-(2aminoethyl)glycine backbone, which recognize and bind strongly to specific DNA or RNA sequences (2, 3). These characteristics make them potentially useful as antisense and antigene drugs or molecular probes, which have numerous applications in the field of molecular and experimental medicine (4ñ10). The hybridization properties of peptide nucleic acids (PNAs) have attracted widespread interest to this class of compounds (11ñ13). In connection with our work in synthesis of new α-amino acid derivatives (14ñ22) and due to the pharmacological properties of PNAs and amino acid derivatives we were prompted to prepare new N 6-benzyladenine bearing amino acid derivatives to study their antiviral activity. EXPERIMENTAL Chemistry All melting points were uncorrected and were taken in open capillary tubes using silicon oil on Gallenkamp apparatus. Elemental microanalyses were performed on Elementar, Vario EL,

The present work represents the reaction of different hydrazides with carbon disulfide in the presence of potassium hydroxide to afford 1-(1,3,4-oxadiazol-5-ylmethyl-2-thio)-pyrimidinedione derivatives. Conventional heating and microwave irradiation (MW) of the 1,2,4-triazoles with hydrazine hydrate afforded the corresponding 4-amino-1H- 1,2,4-triazole-5(4H)-thiones. Treatment of the latter compounds either with carbon disulfide in the presence of KOH or with methyl iodide followed by reaction with phthalaldehydic acid under microwave conditions using isopropyl alcohol or dimethylformamide as a solvent afforded the thioxo[1,2,4]triazolo[3,4-b]thiadiazoles and 4-amino-5- (methylthio)-4H-1,2,4-triazoles, respectively. Conventional heating and microwave irradiation (MW) of 4-amino-5- (methylthio)-4H-1,2,4-triazoles with different aromatic aldehyde afforded the corresponding schiffE¹s bases. While reaction of 4-aminotriazoles with phthalaldehydic acid afforded different products dependi...

As attempt to cope the microbial drug-resistance, new derivatives of 2-pyridinone and 2-iminochromene with biologically active pyrrole core were designed and synthesized. The 2-pyridone derivatives were synthesized via ring closure of 2-cyano-N'-((1-methyl-1H-pyrrol-2-yl)methylene)acetohydrazide by 1,3-dicarbonyl compound (acetylacetone) or arylidene malononitriles. The 2-iminochromene derivatives were obtained via the cyclocondensation reaction of cyanoacetamide by o-hydroxy aldehyde derivatives to furnish chromene derivatives. The antibacterial and antifungal activities for the synthesized compounds were investigated. All of the 2-pyridinone and 2-iminochromene derivatives showed moderate activity toward both of G -ve and G + ve bacteria (S. aureus).

Coumarin is classified as one of interesting therapeutic starting research points to obtain remarkable compounds with high efficacy. So, during this research, new 2-iminochromene derivatives bearing coumarin moiety were synthesized. At first, cyanoacetohydrazone of 3-acetylcoumarin was prepared and used as the starting material. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazone derivative with 4-hydroxysalicylaldehyde, 5-aryldiazosalicylaldehydes, 2-hydroxynaphthaldehyde and 7-hydroxychromone-6-carboxaldehyde derivative. All of the newly synthesized coumarin derivatives were obtained in excellent yields; so, the new synthesized coumarin derivatives will participate in the enrichment of the chemical libraries.