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Some poly functionalized heterocyclic‐compounds containing pyridine‐moieties were readily assembled by combining differently functionalized pyridopyrimidine‐6‐carbonitrile derivatives 1a,b with different electrophilic and nucleophilic reagents via short synthetic routes. The structures of the prepared derivatives were ascertained from their‐spectral‐and elemental analyses. Some of the synthesized compounds were tested as plausible antitumor agents. Most of those tested compounds likes 7, 9, 10, 11a showed cytotoxic potencies against different tumor cell lines. In addition, the assessments for their antioxidant activities have also been done and compound 9 exhibited the highest antioxidant activity while compounds 7 and 10 showed moderate activities. Finally, molecular docking studies were carried out which favorably indicated a high support for the experimental‐results.

The present work describes convenient synthesis of the novel Schiff bases 5a and b by reacting phthalazinones 4a and b with 4-methoxybenzaldehyde Reaction of the Schiff bases with phenylisothiocyanate afforded diazetidine derivatives 7a and b. Also, compounds 4a and b reacted with 2-bromoglucoside tetraacetate giving peracetylated N-glycosides 6a and b, which were deacetylated to afford N-glycosylated phthalazinones 8a and b. On the other hand, when compound 3 was treated with POCl 3 /PCl 5 and/or ethyl chloroacetate, chlorophthalazine and ethyl acetate derivatives 9 and 10 were obtained, respectively. Hydrazinolysis of compounds 9 and 10 produced the hydrazino and hydrazide derivatives 11 and 12, respectively. When compound 11 reacted with 2-furanaldehyde, acetic anhydride, and/or carbon disulphide, it gave compounds 13-15, respectively. Treatment of the hydrazide 12 with aromatic aldehydes, acetic anhydride, ethyl acetoacetate, acetyl acetone, ammonium thiocyanate, and/or phthalic anhydride furnished compounds 17-21. Meanwhile, reacting Schiff base 22 with the chlorophthalazine derivative 9 produced compound 23, which on treatment with furoyl chloride produced compound 24. The structures of the novel compounds were confirmed by IR, 1 H-NMR, 13 C-NMR, MS, and elemental analysis. The newly synthesized compounds were tested against Bacillus subtilis and Staphylococcus aureus as Gram-positive bacteria, Escherichia coli and Pseudomonas aurignosa as Gram-negative bacteria, and Candida albicans and Aspergillus niger as fungi strains. Compounds 5a and b, 23, and 24 showed greater antimicrobial activity than the stranded compounds, suggesting that they could be considered as promising antimicrobial agents.Key words phthalazin-1-one; N-glycosylated phthalazinone; Schiff base; diazetedine; antimicrobial activity Phthalazines as N-heterocycles have received considerable attention in the literature as a consequence of their role as pharmacophore.1,2) Recently, they are derived from a wide range of biologically active natural products, troponoid family.3) A novel series of N-substituted-4-phenyl/benzylphthalazin-1-ones, phthalzine-1,4-dione showed antitumor activity. were prepared from the corresponding phthalazinones. Moreover, many substituted and fused phthalazine and phthalzinone derivatives exhibited antimicrobial activity. 23-26)On the basis of the above findings and in continuation of our research interest in the synthesis of novel biologically active heterocycles, [27][28][29][30][31] and with the aim of preparing new derivatives of phthalazine with potential pharmacological activity, we report here the synthesis of novel Schiff bases containing phthalazine moiety, phthalazinone and fused phthalazine derivatives, followed by evaluation of their antimicrobial activity against different strains of bacteria and fungi, where most of synthesized compounds exhibited a moderate to a strong antimicrobial activities. Some of the tested compounds showed antimicrobial activity higher than the reference compounds. Results and D...

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Subjects and Methods SamplesA total of 500 panoramic radiographs of Egyptian Subjects (262 males and 238 females), aged between 18 and 71 years were analyzed. These panoramic radiographs were undergone at the Oral Radiology Clinic, Faculty of Oral and Dental Medicine, Cairo University (Proline XC, Planmeca Oy -Helsinki, Finland). The exposure parameters were set according to the patient's age and size. The patient's identification number, sex, age and date of radiographic taking were recorded.The inclusion and exclusion criteria were: Subjects should be clinically free from any developmental, endocrine or nutritional disorder and special dental diseases. Panoramic radiographs showing impacted teeth, teeth with root canal treatment, crown restorations, broken teeth, teeth with large areas of enamel overlap between neighboring teeth, missing one of the studied teeth or unclear radiographs were excluded from the study samples. All the three studied teeth, viz., mandibular canines (C), first premolars (PM1) and second premolars (PM2) were clearly visible. Protocols of the study and for radiographs collection of human subjects were approved by Ethical committee of