Bollettino chimico farmaceutico Journal Impact Factor & Information

Publisher: Societá editoriale farmaceutica

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Other titles Bollettino chimico farmaceutico
ISSN 0006-6648
OCLC 4055131
Material type Periodical
Document type Journal / Magazine / Newspaper

Publications in this journal

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    ABSTRACT: 3,4-Dihydro-1H-benzo[e][1,4]diazepine-2,5-dione 1 has been prepared from the reaction of glycine with isatoic anhydride. Bromination of 1 with molecular bromine in acetic acid affords the 7-bromo derivative 2. Partial and full reduction of 2 with LiAlH4 gives the 7-bromo-1,2,3,4-tetrahydrobenzo[e][1,4]diazepin-5-one 3 and 7-bromo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine 4, respectively. The reaction of 3 with alkyl and acyl halides produces the corresponding derivatives 5. Preliminary pharmacological screening of some of the newly synthesized compounds reveal that they exhibit CNS-depressant and anticonvulsant activity.
    Bollettino chimico farmaceutico 08/2010; 141(1):8-14. DOI:10.1002/chin.200233180
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    ABSTRACT: The effects of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and Polyvinylpyrrolidone (PVP-K30) on the solubility of 2-Hydroxyl-N-(3-methyl-5-ethylisoxazolyl-4-yl)-1,4-naphthoquinone-4-imine (I) were investigated, this compound, a synthetic derivative of isoxazolylnaphthoquinones, has proved to exhibit important biological activity against the causative agent of Chagas' disease and against Staphylococcus aureus. In addition, the effect of co-administration of a water-soluble polymer (PVP-K30) and ionization of I on the HP-beta-CD solubilizing effect was also examined. HP-beta-CD and PVP-K30 possess a significant solubilizing effect by themselves. PVP-K30 increases the solubilizing effect of HP-beta-CD by enhancing the apparent stability constant (Kc) of the I: HP-beta-CD complex. The addition of 0.5% (w/v) PVP-K30 to the complexation medium results in a 83% increase in the stability constant of the complex. The HP-beta-CD solubilization of I can also be improved by ionization of the drug molecule through pH adjustments. Although the Kc of the I complex is larger in the neutral form, a higher overall solubility is attained when I is in its ionized form. A 38-fold solubility enhancement is possible by using a combined approach of pH adjustment and complexation with HP-beta-CD.
    Bollettino chimico farmaceutico 11/2005; 141(1):63-6.
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    ABSTRACT: Chitosan hydrogel beads containing diclofanac sodium were prepared using ionotropic gelation technique in which tripolyphosphate solution was used as a counterion. Chitosan molecular weight, tripolyphosphate concentration and crosslinking time were found to have an effect on the percentage of the drug loading. The loading efficiency of diclofenac sodium was very high (more than 90%). A longer-period of contact with the counterion ions decreased the efficiency of drug loading. The beads produced all had good spherical geometry. The beads showed a narrow size distribution in which 95% of the beads prepared were in the range of 2-3 mm. Comparison of release rate-time plots of dissolution data of marketed product with the newly developed dosage form indicated the ability of the later to sustain more diclofenac sodium release. The beads were evaluated for their bioavailability in six beagle dogs relative to the commercial enteric-coated Voltaren tablets. The in vivo availability study, reveled that the prepared beads filled in hard gelatin capsules had a 126.22% bioavailability relative to that of the commercial Voltaren tablets. The beads showed comparable pharmacokinetic parameters to that of the commercial tablets. The results suggested the possibility of producing a promising sustained drug delivery system for diclofenac sodium.
    Bollettino chimico farmaceutico 01/2005; 143(10):359-64.

  • Bollettino chimico farmaceutico 01/2005;
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    ABSTRACT: A non-bitter chloroquine suspension formulation for pediatric use was prepared in the form of an ion-pair of chloroquine with pamoic acid. Various parameters involved in the formulation of a stable and palatable suspension have been optimized. The suspension was characterized for particle size analysis, viscosity, physical and chemical stability and taste. Release of chloroquine from the ion-pair conducted as dissolution rate studies in simulated gastric media showed near to 100% release instantaneously. In-vivo bioavailability study conducted in albino rats indicated comparable bioavailability of chloroquine from the suspension with that of chloroquine phosphate syrup taken as standard. Stability study conducted over a period of 3 months showed the intactness of the ion-pair and the tasteless behavior of the suspension throughout the period of storage.
    Bollettino chimico farmaceutico 01/2005; 143(10):377-82.

  • Bollettino chimico farmaceutico 01/2005; 144:1-17.
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    ABSTRACT: A variety of 2-substituted-4, 6-diaryl-3-pyridinecarboxylates 4 were obtained through aromatic nucleophilic substitution. reaction of secondary amines with 2-bromo-3-pyridinecarboxylate derivatives 3. The latters were obtained through bromination of 3-aryl-4-benzoyl-2-cyanobutyrates 2 in glacial acetic acid. However; reaction of primary aromatic amines with 2-bromopyridines 3 afforded 2-arylamino-3-pyridinecarboxylates 5 beside the unexpected 2-amino analogues 6. On the other hand, 3-hydroxy-1H-pyrazolo[3,4-b]pyridines 7 were isolated via reaction of 3 with hydrazine hydrate. Good to complete muscle relaxation of rabbit's jejunium, rat's uterus and rabbits aorta was observed during screening representative examples (3a, 4c, Sd, 5f and 6b) of the newly synthesized 3-pyridinecarboxylates indicating the vasodilatation and antihypertension activity for the tested compounds.
    Bollettino chimico farmaceutico 01/2005; 143(10):365-75.
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    ABSTRACT: The paper presents the synthesis of sulfonyl tetrahydropyrimido[4,5-d]pyrimidine derivatives as well as the antimicrobial activity of the obtained compounds. The investigations showed that the obtained sulfonyl derivatives of pyrimido[4,5-d]pyrimidines and especially the compounds with free amino group reveal interesting antibacterial and antifungal activity.
    Bollettino chimico farmaceutico 12/2004; 143(9):321-8.
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    ABSTRACT: In an attempt to design and synthesize more potent quinoline-based chemotherapeutic agents structural modifications of 5, 7-Dibromo-2-methyl-8-benzoyloxyqinoline was carried out. The replacement of the bromine atoms with the requisite alkylamino compound gave four amino-derivatives viz: bis(dipropylamino)-dipyrrolidino-, dipiperidino- and dipiperazino derivatives. The antimicrobial activities of these compounds were investigated against selected Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), Gram-negative bacteria (Escherichin coli, Pseudomonas aeruginosa and Klebsiella spp) and yeast (Candida albicans). All the compounds showed broad or significant antimicrobial activity, which varied from two to ninety times that of the parent compound. The dipyrrolidino derivative was the most effective against Gram-positive bacteria and yeast while the dipiperidino derivative was the most effective against Gram-negative bacteria. No correlation has been established between the minimum inhibitory, (MIC) concentrations of the derivatives and the structural modifications.
    Bollettino chimico farmaceutico 12/2004; 143(9):341-3.
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    ABSTRACT: Photooxygenation reaction of ã -terpinene (1) in the presence of tetraphenyl porphine (TPP) or Rose Bengal (RB) gave 2, 5-dihydroperoxy-1-isopropylene-4-methylene-cyclohexane (2), 3,6-dihydroperorxy-3-isopropyl-6-methyl-2,4-cyclohexadiene (3) and 1,2&4,5-diepoxy-1-isopropyl-4-methylcyclohexane (4). The epoxide 4 was also synthesised through the epoxidation reaction of ã-terpinene (1) with m-chloroperbenzoic acid (mcpba).
    Bollettino chimico farmaceutico 12/2004; 143(9):337-9.
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    ABSTRACT: Various 1,4-substituted derivatives of piperazine (I-XII) were synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (ScMet)--induced seizures and for neurotoxicity (TOX) in the rotorod test in mice and rats. The most promising compounds seem to be 1-[(2,4,6-trimethyl)-phenoxyethyl]-4-(2-hydroxyethyl)-piperazine dihydrochloride (II) and 1,4-bis-[(4-chloro-3-methyl)-phenoxyethyl]-piperazine dihydrochloride (X) which displayed anti-MES activity with their protective index (PI) higher than that for valproate II (rats), X(mice)).
    Bollettino chimico farmaceutico 12/2004; 143(9):329-35.
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    ABSTRACT: Mesalazine, a drug of choice in the management of ulcerative colitis, was chemically modified as 5-(E)-substituted benzylideneaminosalicylic acid by condensing 5-aminosalicylic acid with selected aryl aldehydes with an intention to improve its pharmacological profile. The tests were performed to study their anti-inflammatory effect on carrageenan-induced ulcerative colitis in albino rats. The histopathological findings, serum transaminase level and lipid peroxide content in the intestine and liver were taken as indices of pharmacological activity. The azomethine derivative formed from salicylaldehyde (5-ASASB3) was found to have maximum activity and it reversed the disease symptoms in experimental animals The azomethine derivative markedly reduces the ulcerative colitis when compared with parent molecule, mesalazine.
    Bollettino chimico farmaceutico 11/2004; 143(8):309-13.
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    ABSTRACT: Four novel series of 1,4-naphthoquinone derivatives namely 2,3-disubstiuted 4-[(benzothiazol-2-yl)hydrazono]-1,4-dihydronaphthalen-1-one 4a-c, N1-(2,3-disubstituted-4-oxo-1,4-dihydronaphthalen-1-ylidene)-N2-(benzotriazol-1-yl)acetic acid hydrazide 5a-c, 2,3-disubstituted 4-[(5-aryl-2,3-dihyrothiazol-2-ylidene)hydrazono]-1,4-dihydronaphthalen-1-one 7a-c, and 3-methyl-2-substituted carbamoyl or thiocarbamoyl-hydrazinocarbonylmethylthio-1,4-dihydronaphthalene-1,4-dione 9a-c were synthesized. Three of the new compounds were chosen by NCI to be evaluated as anticancer agents and they showed promising activity. All the prepared compounds were tested as antimicrobial agents.
    Bollettino chimico farmaceutico 11/2004; 143(8):299-307.
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    ABSTRACT: Cyclization of cinnamoyl isothiocyanate with nucleophilic reagents either spontaneously or with added a reagents is reported.
    Bollettino chimico farmaceutico 11/2004; 143(8):291-7.
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    ABSTRACT: The objective of the current study was to determine whether homocysteine elevations precede the development of pre-eclampsia, and to examine the relationship between the occurrence of pre-eclampsia and the degree of hyperhomocysteinemia, so as to find a new prognostic parameter for women with liable to develop pre-eclampsia. The study comprised 103 pregnant females chosen of those attending the Antenatal Care Unit at Benha University Hospital and accepted to donate blood samples at the 16th week of gestation. Women, who delivered at Benha University Hospital, were retrospectively allocated into two groups: Control group (Group C): comprised 64 (71.1%) parturient, who completed their full term pregnancy without the development of pre-eclampsia. Pre-eclampsia group (Group PEc): comprised 26 (28.9%) parturient who developed pre-eclampsia throughout their course of pregnancy but had completed their full term pregnancy. Through the present study, estimated fasting plasma tHcys levels were higher than the 90th percentile of the control group (> or = 5.1 ng/dl) in 6 (9.4%) women in group C and in 9 (34.6%) in group PEc. There was a significant (P<0.05) increase of fasting plasma tHcys levels in nullipara pre-eclamptic parturient as compared to multiparous control parturient. Also, a negative significant correlation was reported between parity and the fasting plasma tHcys level in pre-eclamptic parturient. The present results showed a significant increase of fasting plasma tHcys level in obese women with a positive significant correlation between fasting plasma tHcys level and BMI in PEc group. Thus, it can be concluded that hyperhomocysteinemia is an indirect risk factor for placental vasculopathy predating clinical pre-eclampsia, and can be used as a biomarker for identifying women at risk of complications and adverse pregnancy outcomes.
    Bollettino chimico farmaceutico 10/2004; 143(7):281-7.