Synthesis of some novel 1,3,6-trisubstituted-lhthiazol0[ 3,21]purine-2,4 diones and xanthine schiff bases as potenial anti-asthmatic and antiinflammatory agents

In this study, the design, synthesis and preliminary pharmacological investigation of novel J,3-diethyl-8-disubstituted xantines 12-18, I, 3, 6-trisubstituted-J H-thiazolo[J,2-fl purine-2,4- diones 19-25 and xanthine Schiff bases 28-33 was described. J,3-Diethyl-8-substituted xantines 12-18 were prepared by the reaction of I, 3-diethyl-8-thioxo-3, 7. 8, 9-tetrahydropurine-2, 6-dione 4 with the appropriate phenacyl bromides 5-/l. Compound 4 was in turn prepared by the reaction of 5,6-diamino-l,3-diethyluracil 3 with carbon disulfide. The derivatives 19-25 were obtained by cyclodehydration of compounds 12-18 in po/yphosphoric acid [PPA]. Schiff bases 28-33 were synthesized by the reaction of acetohydrazide 27 with appropriate aldehyde in refluxed ethanol. The effect of the new derivatives as potential anti-asthmatic was evaluated using acetycholine induced brocnhospasm in Guinea pigs, most of tested compounds showed significant anti-bronchoconstriction activity in comparison with aminophylline as a standard drug. Anti-inflammatory activity of the target compounds was investigated using indomethacin as a reference drug and some compounds exhibited potent anti-inflammatory activity

Antibiotic dispensing without prescription in Jordanian community pharmacies: a pharmacist's perspective

The sale of antibiotics without medical prescriptions has been recognized as a major source of drug misuse and medication risk in Jordan. This practice constitutes one of the major causes of the on going problem of antibiotic resistance. This study provides a pharmacist perspective on the problem through presenting the most common antibiotics dispensed, the related indications, and pharmacists proposed solutions to this problem in the city of Amman, Jordan. This was achieved by means of a structured questionnaire prepared by the investigators and completed by the pharmacists themselves. It was suggested that the problem at hand can be overcome through the enforcement of laws to control such practice. Also, increasing awareness among patients and pharmacists, and empowering pharmacists to play more active role in patients care are important steps that will contribute in minimizing this practice

Design and synthesis of some new 1,2,4-triazole derivatives as potential antibacterial agents

Triazoles with different substituent groups are found to possess diverse applications in the field of medicinal chemistry. A new series of novel 1, 3, 5-trisubstituted[1, 2, 4]triazole derivatives, their Schiff bases and their amide derivatives were synthesized. Schiff bases [6-10] were prepared by the reaction of the triazoles amine 5 with equimolar amounts of the appropriate substituted benzaldehydes. The amide derivatives [25-39] were obtained by condensation of triazole amines [21-24] with the appropriate acid chloride. Chemical structures were confirmed by IR, [1]H-NMR, [13]C-NMR, FAB-MS, EI-HRMS spectra and elemental analyses. All the newly synthesized compounds were tested for in vitro activity against certain strains of bacteria such as Staph. aureus, Staph. saprophyticus, Escherichia coli and Bacillus cereus. Most of the tested new compounds exhibited promissing antibacterial activity. Some of them showed antibacterial activity more significant than the reference drugs. Compounds 6-10, 33, 36 and 39 were the most potent derivatives

Synthesis, anti-bronchoconstrictive, and antibacterial activities of some new 8-substituted-1,3-dimethylxanthine derivatives

Methylxanthines especially theophylline have been recognized as potent bronchodilators for the relief of acute asthma for over 50 years. Recently, it was found that bacterial infection has a role in asthma pathogenesis. Accordingly, the present work involves the synthesis of different series of 8-substituted [aryl, aralkyl, cycloalkyl, and heteroaryl]-l,3-dimethylxanthines. The chemical structures of these compounds were elucidated by IR, [1]H NMR, [13]C NMR, elemental analyses, and high resolution EI-MS or FAB-MS for some compounds. The bronchodilator activity was evaluated using acetylcholine induced bronchospasm in guinea pigs, and most of the compounds showed significant anti-bronchoconstrictive activity in comparison with aminophylline as a standard. Also, the antibacterial activity of all the target compounds was investigated in-vitro against Gram-positive and Gram-negative bacteria using ampicillin as a reference drug. Results showed that some of the tested compounds have potent antibacterial activity. A pharmacophore model was computed to get useful insight on the essential structural features of bronchodilator activity

Synthesis of some novel 1, 3, 5-trisubstituted [1,2,4] triazole derivatives as potential antibacterial agents

In the present work, some new l,3,5-trisiubstituted [l,2,4]-triazole derivatives and their Schiff's bases were synthesized. The chemical structure of the target compounds was confirmed by IR, [1]H-NMR, [13]C-NMR, FAB-MS, EI-HRMS spectra and elemental analyses. The title compounds were tested for their in vitro antibacterial activity against Gram-positive and Gram-negative ones using ampicillin and nalidixic acid as reference drugs. Some of them showed antibacterial activity more significant than the reference drugs

Antitumor activity of some new 1,3,8-trisubstituted purine-2,6-diones and 1,3,6-trisubstitutedthiazolo[2,3-f] purine-2,4-diones

New l,3,8-trisubsttiuted purine-2,6-diones and 1,3,6-trisubstituted thiazolo[2,3-f] purine-2,4-diones were designed and synthesized as potential antitumor agents. The cytotoxic effects of the tested compounds were assessed against two human malignant-cell lines: T-cell leukemia derived SKW-3 and breast cancer -derived MDA-MB-231 using the methyl thiazolyl tetrazolium [MTT-dye] reduction assay, after 72 h exposure. The data -were fitted to sigmoidal concentration response curves and the corresponding 1C 50 values were calculated using commercially available software [GraphPad Prizm]. Compound AH-206 was the most potent cytotoxic agent among the newly synthesized compounds, with 1C 50 value of 17.3 micro M. Prominent activity was also encountered with compounds AH-201, AH-205, AH-208, AH-214 and AH-217, all having 1C[50] values below 100 micro M

Synthesis and quantitative structure activity relationship [QSAR] study of new 3-allyl-5-substituted-3,4,5,6-tetrahydro-2H-l,3,5-thiadiazine-2-thiones of a potential antimicrobial activity

Fifteen new 3-allyl-5-substituted-3,4,5,6-tetrahydro-2H-l,3,5-thia diazine-2-thiones were synthesized by the reaction of allylamine with carbon disulfide and potassium hydroxide, followed by formaldehyde and appropriate primary amine such as alkyl, aralkylamines, glycine, L-alanine or ethyl glycine ester. The title compounds were tested, in vitro, for antimicrobial activity against gram-positive bacteria [Bacillus cereus, Staphylococcus aureus, Micrococcus leuteus], Gram-negative bacteria [Escherichia coli, Serratia marcescens, Pseudomonas aeruginosa], and some fungi [Aspergillus flavus, Aspergillus niger, Candida albicans, Geotrichum candidum, Scopulariopsis brevicaulis and Tricho-phyton rubrum], using agar disc method. Quantitative structure activity relationship study was performed using the log form of MIC against Scopulariopsis brevicaulis fungi and some physico-chemical descriptors [MR, L, and Fr] of substituents at N-5 position. The log MIC were found to be negatively linearly correlated with MR and L and positively linearly correlated with Fr