Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives

Mohamed, Bahaa Gamal,Hussein, Mostafa Ahmed,Abdel-Alim, Abdel-Alim Mohamed,Hashem, Mohammed The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.1

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

Embryotoxic and Teratogenic Effects of Tartrazine in Rats

Hashem, Mohamed Mohammed,Abd-Elhakim, Yasmina Mohammed,Abo-EL-Sooud, Khaled,Eleiwa, Mona M.E. Korean Society of ToxicologyKorea Environmental Mu 2019 Toxicological Research Vol.35 No.1

Tartrazine (TAZ) is one of the most commonly used artificial dyes for foods and drugs. We determined the effect of TAZ on fetal development by examining morphological, visceral, and skeletal malformations in rat fetuses following daily oral administration of TAZ to pregnant Wistar rats at the 6th-15th day of gestation. TAZ at 0.45 and 4.5 mg/kg induced 6.0 and 7.1% fetal resorptions, as well as 10.0 and 10.5% fetal mortality, respectively. Fetal body weight and length were significantly lower in the groups treated with TAZ at 0.45 ($3.97{\pm}0.21g$ and $27.3{\pm}0.54mm$, respectively) and 4.5 mg/kg ($3.48{\pm}0.15g$ and $23.22{\pm}1.02mm$, respectively) than in the control group ($4.0{\pm}0.15g$ and $30.01{\pm}0.42mm$, respectively). TAZ at 0.45 and 4.5 mg/kg induced hepatic damage (20 and 33.3%, respectively), dark brown pigmentation due to hemosiderin in the splenic parenchyma (16.7 and 21.7%, respectively), as well as destructed and necrotic renal tubules (16.7 and 26.7%, respectively) in the fetuses. Moreover, TAZ at 0.45 and 4.5 mg/kg caused one or more missing coccygeal vertebrae (20 and 40%, respectively), missing sternebrae (6 and 10%, respectively), missing hind limbs (24 and 4%, respectively), and irregular ribs (16 and 20, respectively) in the fetuses. We concluded that TAZ has embryotoxic and teratogenic potentials in rats.

Embryotoxic and Teratogenic Effects of Tartrazine in Rats

Mohamed Mohammed Hashem,Yasmina Mohammed Abd-Elhakim,Khaled Abo-EL-Sooud,Mona M. E. Eleiwa 한국독성학회 2019 Toxicological Research Vol.35 No.1

Tartrazine (TAZ) is one of the most commonly used artificial dyes for foods and drugs. We determined the effect of TAZ on fetal development by examining morphological, visceral, and skeletal malformations in rat fetuses following daily oral administration of TAZ to pregnant Wistar rats at the 6th-15th day of gestation. TAZ at 0.45 and 4.5 mg/kg induced 6.0 and 7.1% fetal resorptions, as well as 10.0 and 10.5% fetal mortality, respectively. Fetal body weight and length were significantly lower in the groups treated with TAZ at 0.45 (3.97 ± 0.21 g and 27.3 ± 0.54 mm, respectively) and 4.5 mg/kg (3.48 ± 0.15 g and 23.22 ± 1.02 mm, respectively) than in the control group (4.0 ± 0.15 g and 30.01 ± 0.42 mm, respectively). TAZ at 0.45 and 4.5 mg/kg induced hepatic damage (20 and 33.3%, respectively), dark brown pigmentation due to hemosiderin in the splenic parenchyma (16.7 and 21.7%, respectively), as well as destructed and necrotic renal tubules (16.7 and 26.7%, respectively) in the fetuses. Moreover, TAZ at 0.45 and 4.5 mg/kg caused one or more missing coccygeal vertebrae (20 and 40%, respectively), missing sternebrae (6 and 10%, respectively), missing hind limbs (24 and 4%, espectively), and irregular ribs (16 and 20, respectively) in the fetuses. We concluded that TAZ has embryotoxic and teratogenic potentials in rats.

Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives

Bahaa Gamal Mohamed,Mostafa Ahmed Hussein,Abdel-Alim Mohamed Abdel-Alim,Mohammed Hashem 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.1

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3- a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2- alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3- a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

Research Articles : Evaluation of Two Biologically Active Compounds for Control of Wheat Root Rot and its Causal Pathogens

( Mohamed Hashem ) 한국균학회 2002 Mycobiology Vol.30 No.4

Synthesis of super-absorbent poly(AN)-g-starch composite hydrogel and its modelling for aqueous sorption of cadmium ions

Ali Hashem,Chukwunonso Onyeka Aniagor,Mohamed Abdel-Fattah Afifi,Ashraf Abou-Okeil,Sayed Hussein Samaha 한국화학공학회 2021 Korean Journal of Chemical Engineering Vol.38 No.10

To entrench heavy metal chelation functional groups, native corn starch was grafted with acrylonitrile and subsequently hydrolyzed (using sodium hydroxide) to produce chemically crosslinked superabsorbent hydrogels (SAHs) of three-dimensional hydrophilic polymeric networks. SAHs demonstrated fast swelling and superabsorbent properties, with a swelling capacity of 612 g water/g SAHs. Due to the usefulness of equilibrium and kinetic data for elucidating the nature of adsorbate-adsorbent interaction, the adsorption study was extensively modelled using selected nonlinear isotherm and kinetics models. The Toth and intraparticle diffusion models satisfactorily predicted the isotherm and kinetic data, respectively, while the dominance of the metal complexation mechanism was asserted in the study. Meanwhile, the metal ion uptake by SAHs occurred at a fast equilibration time of 20 min. Furthermore, the adsorbent’s instrumental characterization (scanning electron microscopy, SEM; Energy dispersion X-ray, EDX; X-ray diffraction, XRD and Fourier-transform infrared spectroscopy, FTIR) result confirmed that SAHs possesses the desired metal chelation properties. Thus, the potential application of the developed SAHs as biosorbent in the decontamination of the heavy metal-laden stream was explicitly demonstrated in the study.

Novel application of the esterification product of 2,3-dihydroxybutanedioic acid and cellulosic biomass for cobalt ion adsorption

Ali Hashem,Chukwunonso Onyeka Aniagor,Sayed Mohamed Badawy,Ghada Mohamed Taha 한국화학공학회 2021 Korean Journal of Chemical Engineering Vol.38 No.11

A novel biosorbent (‘Manna_COOH’) was synthesized via dual reaction stages of direct carbonylation of hydroxyl groups of richly cellulosic manna root powder and subsequent esterification of the resultant anhydride analogue into an ester of high carboxyl content. Both the biosorbent precursor and the 2,3-dihydroxybutanedioic acid sustain complementary features that ensured their efficient complexation. The biosorbent depicted a carboxyl content of 412.36 m.eq -COOH/100 g sample and was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR). The study further evaluated the cobalt ion adsorption capacity of the synthesized ‘Manna_COOH’ under the effect of some process variable via batch mode. The Freundlich and pseudo-second-order models emerged as the best fit for the equilibrium and kinetic data, respectively. The rich oxygen-based surface functional groups entrenched on the ‘Manna_COOH’ sequel to its functionalization played a major role in making it a promising biosorbent for aqueous Co (II) uptake.

Efficacy of pethidine, ketorolac, and lidocaine gel as analgesics for pain control in shockwave lithotripsy: A single-blinded randomized controlled trial

Abdelwahab Hashem,Fady K. Ghobrial,M. A. Elbaset,Ahmed M. Atwa,Mohamed Fadallah,Mahmoud Laymon,Ahmed El-Assmy,Khaled Z. Sheir,Hassan Abol-Enein 대한비뇨의학회 2019 Investigative and Clinical Urology Vol.60 No.4

Purpose: To compare the safety and efficacy of xylocaine gel and ketorolac as opioid-sparing analgesia compared with pethidine for shock wave lithotripsy (SWL) pain. Materials and Methods: A single-blinded randomized controlled trial (RCT) was performed in 132 patients with renal and upper ureteral stones amenable to treatment with SWL. The first patient group received intravenous (IV) pethidine and placebo gel; the second group received IV ketorolac plus placebo gel; the third group received lidocaine gel locally plus normal saline IV. Stone disintegration was classified as none (no change from basal by kidney, ureter, bladder X-ray or ultrasound [US] imaging), partial (fragmented and >4-mm residual fragments), and complete (≤4-mm residual fragments). Stone disintegration was assessed by kidney-ureter-bladder X-ray and US imaging. Pain was evaluated by use of the Numeric Pain Rating Scale (NPRS). Results: The NPRS scores were highest in the xylocaine group at 10, 20, and 30 minutes (p=0.0001) with no significant difference between the ketorolac and pethidine groups, except at 10 minutes (p=0.03) and a near significant difference at 30 minutes (p=0.054) in favor of ketorolac. Results for stone disintegration (none, partial, and complete, respectively) were as follows: 25 (50.0%), 23 (46.0%), and 2 (4.0%) for pethidine; 19 (35.8%), 23 (43.4%), and 11 (20.8%) for ketorolac; and 26 (89.7%), 3 (10.3%), and 0 (0.0%) for lidocaine (p=0.008). Conclusions: Ketorolac is a safe and more effective alternative to morphine derivatives for SWL analgesia. Lidocaine gel should not be used as mono-analgesia for SWL.

Molecular Genetic Identification of Yeast Strains Isolated from Egyptian Soils for Solubilization of Inorganic Phosphates and Growth Promotion of Corn Plants

( Abd Ei Latif Hesham ),( Hashem M. Mohamed ) 한국미생물 · 생명공학회 2011 Journal of microbiology and biotechnology Vol.21 No.1

Forty yeast strains isolated from soils taken from different locations in Egypt were tested for their P-solubilizing activities on the basis of analyzing the clear zone around colonies growing on a tricalcium phosphate medium after incubation for 5 days at 25oC, denoted as the solubilization index (SI). Nine isolates that exhibited P-solubilization potential with an SI ranging from 1.19 to 2.76 were genetically characterized as five yeasts belonging to the genus Saccharomyces cerevisiae and four non-Saccharomyces, based on a PCR analysis of the ITS1-26S region amplied by SC1/SC2 species-specific primers. The highest Psolubilization efficiency was demonstrated by isolate PSY- 4, which was identified as Saccharomyces cerevisiae by a sequence analysis of the variable D1/D2 domain of the 26S rDNA. The effects of single and mixed inoculations with yeast PSY-4 and Bacillus polymyxa on the P-uptake and growth of corn were tested in a greenhouse experiment using different levels of a phosphorus chemical fertilizer (50, 100, and 200 kg/ha super phosphate 15.5% P2O5). The results showed that inoculating the corn with yeast PSY-4 or B. polymyxa caused significant increases in the shoot and root dry weights and P-uptake in the shoots and roots. The P-fertilization level also had a significant influence on the shoot and root dry weights and P-uptake in the shoots and roots when increasing the P-level from 50 up to 200 kg/ha. Dual inoculation with yeast strain PSY-4 and B. polymyxa at a P-fertilization level of 200 kg/ha gave higher values for the shoot and root dry weights and P-uptake in the shoots and roots, yet these increases were nonsignificant when compared with dual inoculation with yeast strain PSY-4 and B. polymyxa at a P-fertilization level of 100 kg/ha. The best increases were obtained from dual inoculation with yeast strain PSY-4 and B. polymyxa at a P-fertilization level of 100 kg/ha, which induced the following percentage increases in the shoot and root dry weights, and P-uptake in the shoots and roots; 16.22%, 46.92%, 10.09%, and 31.07%, respectively, when compared with the uninoculated control (fertilized with 100 kg/ha).

Controllable Biogenic Synthesis of Intracellular Silver/Silver Chloride Nanoparticles by Meyerozyma guilliermondii KX008616

( Saad A. M. Alamri ),( Mohamed Hashem ),( Nivien A. Nafady ),( Mahmoud A. Sayed ),( Ali M. Alshehri ),( Gamal A. El-shaboury ) 한국미생물생명공학회(구 한국산업미생물학회) 2018 Journal of microbiology and biotechnology Vol.28 No.6

Intracellular synthesis of silver/silver chloride nanoparticles (Ag/AgCl-NPs) using Meyerozyma guilliermondii KX008616 is reported under aerobic and anaerobic conditions for the first time. The biogenic synthesis of Ag-NP types has been proposed as an easy and cost-effective alternative for various biomedical applications. The interaction of nanoparticles with ethanol production was mentioned. The purified biogenic Ag/AgCl-nanoparticles were characterized by different spectroscopic and microscopic approaches. The purified nanoparticles exhibited a surface plasmon resonance band at 419 and 415 nm, confirming the formation of Ag/AgCl-NPs under aerobic and anaerobic conditions, respectively. The planes of the cubic crystalline phase of the Ag/AgCl-NPs were confirmed by X-ray diffraction. Fourier-transform infrared spectra showed the interactions between the yeast cell constituents and silver ions to form the biogenic Ag/AgCl-NPs. The intracellular Ag/AgCl-NPs synthesized under aerobic condition were homogenous and spherical in shape, with an approximate particle size of 2.5-30nm as denoted by the transmission electron microscopy (TEM). The reaction mixture was optimized by varying reaction parameters, including temperature and pH. Analysis of ultrathin sections of yeast cells by TEM indicated that the biogenic nanoparticles were formed as clusters, known as nanoaggregates, in the cytoplasm or in the inner and outer regions of the cell wall. The study recommends using the biomass of yeast that is used in industrial or fermentation purposes to produce Ag/AgCl-NPs as associated by-products to maximize benefit and to reduce the production cost.