Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 144-fold increase in aqueous solubility compared to ciprofloxacin. Taste evaluation by panel method showed palatable taste in prodrugs compared to the parent drugs. The synthesized compounds were screened for their antimicrobial activity against different bacterial strains which are, Staphylococcus aureus, Pseudomonas aeruginosa, E. coli and Klebsiella pneumonia. The prodrugs have revealed excellent antibacterial activities compared with the parent compounds. Chemical hydrolysis study at pH (1.2 and 7.4) has indicated that these compounds may pass unhydrolyzed through the stomach and produce enough stability to be absorbed from the intestine as indicated by t1/2 values.
Objectives: Two derivatives of cephalexin were synthesized by reaction with isatin-glycine Schiff base and bromoisatin-glycine Schiff base separately. Methods: Cephalexin was linked through the amine group to isatin glycine and bromoisatin glycine Schiff bases by amide bond formation. Results: These derivatives were characterized by FT-IR, H-NMR, elemental CHN analysis and then tested for their antimicrobial activity compared to cephalexin against gram-positive, gram-negative bacteria and Candida albicans fungi. Conclusion: The two compounds showed better activity against Staphylococcus aureus, compound 3b is more active against Escherichia coli, and compound 3a is more active against Klebsiella pneumonia.
In this work, novel compounds of hydrazones derived from (2,4-dinitrophenyl) hydrazine were synthesized. Benzamides derivatives and sulfonamides derivatives were prepared from p-amino benzaldehyde. Then these compounds were condensed with (2,4-dinitrophenyl) hydrazine through Imine bond formation to give hydrazones compounds. The compounds were characterized using FT-IR (IR Affinity-1) spectrometer, and 1HNMR analyses. The majority of the compounds have a moderate antimicrobial activity against “Gram-positive bacteria staphylococcus Aureus, and staphylococcus epidermidis, Gram-negative bacteria Escherichia coli, and Klebsiella pneumoniae, and fungi species Candida albicans” using concentrations of 250 µg\ml.
A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia1 and IIa1).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds and their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).
Compounds (Ia1 and IIa1) were evaluated for&n
... Show MoreThe development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1
... Show MoreThree Schiff bases from Benzaldehyde and Salicylaldehyde have been synthesized (A, 1and 2) and two of them (1and 2) have been tested for anti-inflammatory activity. The p-aminobenzene sulfonamide has been synthesized from acetanilide through the addition of excess chlorosulfonic acid then concentrated ammonia solution; Schiff base of this derivative (2) exhibited good level of activity against egg-white induced edema in rat hind paw, while the other tested derivative exhibited no activity.
Key words: Schiff bases, sulfonamide derivatives, salicylaldehyde
This study aims to isolate the pathogenic yeasts from genital tract and investigate their relationship with the age .The results clarified that the most pathogenic yeast isolated from genital tract was Candida albicans , also the results of C.albicanas isolates susceptibility test, to different antifungal revealed that they were sensitive to Miconazole, Ketoconazole and Clotrimazol and were resistant to Nystatin and Grisofulvin. The study of relationship of vaginal infection with the age showed that the incidence of infection with Candida was high among females age group (19-39 years).
Objective Advantageous properties of silicone elastomer made it one of the favorable materials in maxillofacial prosthesis construction, but these properties may change after months of usage or after pigments addition. This study aimed to define the optimum concentration for a mixture of two types of intrinsic pigments that added to VST-50 maxillofacial silicone material and study their effects on mechanical properties before and after artificial aging. Methods After the pilot study was conducted, 0.1% by weight of rayon flocking and 0. 2% by weight of burnt sienna intrinsic pigment concentration was selected because of improvement in tested mechanical properties of VST-50 maxillofacial silicone. A total of one hundred and eighty samples we
... Show MoreIn this work, The effect of annealing treatment at different temperatures (373, 423 and 473) K and chemical treatment with talwen at different immersion time (40, 60 and 80) min on structural and optical properties of the bulk heterojunction (BHJ) blend copper phthalocyanine tetrasulfonic acid tetrasodium salt/poly dioxyethylenethienylene doped with polystyrenesulphonic acid (CuPcTs/PEDOT:PSS) thin films were investigated. The films were fabricated using spin coating technique. X-ray diffraction (XRD) measurements displayed only one peak at 2θ =4.5o corresponding to (001) direction which has dhkl larger than for standard CuPcTs. The dhkl increase then decrease with increasing annealing temperature and
the time of chemical treatment w
We wanted to find out how selenium (Se) affects broiler chicken performance, meat physicochemical properties, and selenium deposition in the tissues of broilers. Each of the 96 experimental pens had 30 chickens and included a total of 2,880 one-day-old broilers (Cobb 500 strain). A factorial design of four-by-three (SY + SS) and eight replicates (SY + SS) was used for the 12 experimental treatments, with selenium levels ranging from 0.15 to 0.60 ppm and organic (SY) or inorganic (SS) sources of selenium and their relationship (SY + SS). There were no differences in performance (P > 0.05) across Se levels or sources. 106 g/day of ADFI, 63 g/day of ADG, and 1.6844 kg/kg of FCR were found to be the averaging values for these three parameters:
... Show MoreThis paper presents the results of the slope failure analyses from fracture distributions and their relation to tectonic activity; the analytical results have indicated that the phenomena of plane failure, wedge failure and toppling failure can occur at almost of the survey sites within the study area.
The statistical data show that the fracture orientation mainly develop in the E-W, N-S and NW-SE due to the influence of tectonic activity. The occurrence of them together with the rock slope surface orientation has formed plane failure on the slope surface of the 3B highway in the E-W direction and the types of wedge failure and toppling failure on the slope surface of the highw
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