The 1st international ZPSC 2021 Design, Synthesis, and Biological Evaluation of Novel Nicotinamide Derivatives as Potential Histone Deacetylase-3 Inhibitors. Mohamed M. S. Hamoud, a* Sravani Pulya, b Nermine A. Osman, a Yamini Bobde, b Abdalla E. A. Hassan, c Hanan A. Abdel-Fattah, a Balaram Ghosh b and Amany M. Ghanim a a Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. b Department of Pharmacy, BITS-Pilani, Hyderabad Campus, Shamirpet, Hyderabad, 500078, India. c Department of Chemistry, Faculty of Science, Zagazig University, Zagazig 44519, Egypt. Abstract A series of nicotinamide derivatives have been designed and synthesized as HDACi. All compounds were tested for their inhibitory activities against pan HDACs (containing predominantly HDAC1 and HDAC2 isozymes) and against the HDAC3 isoform. Among these, compounds 6b and 6n showed comparable pan HDAC inhibitory activity (IC50 = 4.648 μM and IC50 = 5.481 μM, respectively) compared with BG45 (IC50 = 5.506 μM). Compound 6b exhibited the best potency against HDAC3 with IC50 = 0.694 μM. In addition, the anti- proliferative activity of the synthesized compounds 6a–s was evaluated against three different cancer cell lines including B16F10, MCF-7, and A549. Compound 6b displayed the highest antiproliferative potency (IC50 = 4.66 μM in B16F10 cell lines) and compounds 6b, 6c, 6h, 6i, 6l, 6m, and 6n exhibited higher cytotoxicity against all cell lines compared with the reference BG45. The selected potent compounds also displayed significant selectivity against cancer cell lines over normal human embryonic kidney (HEK-293) cell lines. The molecular modelling study displayed possible interactions between the most potent inhibitor 6b and HDAC3 active sites. Furthermore, the predicted in silico studies of all target compounds revealed acceptable physicochemical properties and pharmacokinetic parameters. Published paper: New J. Chem. 44 (2020) 9671–9683. doi:10.1039/D0NJ01274B. * Poster Presenting author - 51 -
The 1st international ZPSC 2021 Microbiology and Immunology Session - 52 -
The 1st international ZPSC 2021 Oral Presentation - 53 -
The 1st international ZPSC 2021 Oxidative stress & Pseudomonas aeruginosa: friends or enemies? Fatma Mohamed, Ghada Shaker, and Momen Askoura * Department of Microbiology and Immunology, Faculty of pharmacy, Zagazig University Abstract The current study intended to illustrate the influence of oxidative stress exposure on the susceptibility of P. aeruginosa to antibiotics and pathogenesis in host. In the present study, a total of 100 P.aeruginosa isolates were recovered from patients with wound infections, urinary tract infections, burn infections, respiratory tract infections, ear and eye infection. Importantly, exposure of P. aeruginosa to oxidative stress by H2O2 significantly affected bacterial susceptibility to tested antibiotics when compared with unstressed bacteria. In addition, the transcript levels of QS genes were significantly higher in unstressed P. aeruginosa compared with H2O2-stressed cells. The effect of oxidative stress on P. aeruginosa pathogenesis was further investigated using mice infection model. The survival rate of mice infected with stressed P. aeruginosa was higher relative to those infected with unstressed bacteria. In addition, body weight of mice infected with unstressed P. aeruginosa was lower than that of mice inoculated with stressed bacteria. Organ samples obtained from mice infected with unstressed bacteria showed a significant increase in bacterial load compared with stressed bacteria. In conclusion, the current study highlights the influence of stress exposure on P. aeruginosa both antibiotic susceptibility and host pathogenesis. More attention should be paid to patients suffering from Pseudomonas infections both during treatment by antibiotics and bacterial control using disinfectants and/or antiseptics. * Oral Presenting author - 54 -
The 1st international ZPSC 2021 Poster Presentation - 55 -
The 1st international ZPSC 2021 Antibiotic susceptibility of Pseudomonas aeruginosa isolated from different clinical sources Fatma A Mohamed*, Ghada H Shaker, Momen M. Askoura Department of Microbiology and Immunology, Faculty of Pharmacy, Zagazig University, Egypt Abstract Pseudomonas aeruginosa (P. aeruginosa) is a Gram negative opportunistic pathogen which is responsible for many infections in humans. It is the causative agent of nosocomial pneumonia, urinary tract infection, surgical site infections and burn infection. Bacterial resistance to antibiotic is an increasing problems worldwide. Emergence of bacterial resistance to antimicrobials pose a challenge in treating pyogenic infection hence periodical monitoring of bacterial profile and their antibiotic susceptibility pattern is important. In current study, P. aeruginosa isolates obtained from different clinical sources were identified according to traditional biochemical tests. Antibiotic susceptibility testing was performed by the disc diffusion method. Importantly, present results show that 53% out of P. aeruginosa isolates exhibited multi drug resistance (MDR) pattern. P. aeruginosa isolates showed higher resistance to ciprofloxacin, gatifloxacin and meropenem and intermediate resistance to cefoperazone, cefepime, pipracillin, tobramycin, pipracillin-tazobactam, ceftazidime and azetreonem while Low bacterial resistance was noted against colistin only. The inappropriate use of antibiotics has led to the development of resistant bacteria which led to ineffective antibiotic therapy. Current study suggests applying of strict policies for antibiotic prescription and dispensing. * Poster Presenting author - 56 -
The 1st international ZPSC 2021 Antibiotic susceptibility of Staphylococcus aureus isolated from different clinical sources Aliaa Abdelghafar *, Nehal Yousef and Momen Askoura Department of Microbiology and Immunology, Faculty of pharmacy, Zagazig University, Egypt Abstract Staphylococcus aureus is a Gram-positive bacterium living as a commensal on skin, mouth and upper respiratory system, making it a risk factor for opportunistic and nosocomial infections. It is the major cause of skin, bone, pneumonia, soft tissue, and urinary tract infections and other invasive infections in both the community and hospital settings. High prevalence of Methicillin Resistant Staphylococcus aureus (MRSA) strains between staphylococcal isolates is very problematic. MRSA strains are common causes of nosocomial infections and are associated with increased morbidity and mortality. The aim of this study is to characterize prevalence of MRSA isolates and determine antibiotic susceptibility patterns of S. aureus clinical isolates toward various antibiotics by disc diffusion method. S. aureus isolates showed high resistance to both β-lactams and tetracycline and intermediate resistance to gentamycin, azithromycin and erythromycin. However, low bacterial resistance was noted against chloramphenicol, ciprofloxacin, clindamycin and sulphamethoxazole- trimethoprim. S. aureus isolates exhibited a higher sensitivity toward linezolid and vancomycin. The current study indicates that linezolid and vancomycin are the most effective antistaphylococcal drugs. * Poster Presenting author - 57 -
The 1st international ZPSC 2021 Pharmaceutical Analytical Chemistry Session - 58 -
The 1st international ZPSC 2021 Oral Presentation - 59 -
The 1st international ZPSC 2021 Development and validation of eco-friendly micellar-HPLC and HPTLC- densitometry methods for the simultaneous determination of paritaprevir, ritonavir and ombitasvir in pharmaceutical dosage forms Roshdy E. Saraya1*, Adel Ehab Ibrahim1, Magda Elhenawee2, Hanaa Saleh2 1 Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Port Said University, Port Said, Egypt. 2 Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. Abstract Ombitasvir, ritonavir and paritaprevir are three recently discovered directly acting antiviral drugs (DAADs) used in combined single dose tablet dosage form for treatment of hepatitis-C viral infections (HCV). The methods of analysis followed by quality control and research laboratories are required to be economic and fast; however, these methods can also produce huge amounts of chemical waste. In this study two fast, economic and green HPLC and HPTLC methods were validated for the simultaneous determination of the three drugs. For HPLC, isocratic elution used a mixture of micellar aqueous mobile phase consisting of (0.15 M sodium lauryl sulfate and 0.01 M sodium dihydrogen phosphate, pH 6.2) and ethanol (56:44 v%). Elution was done on RP-C18 Kinetix_ column (5 mm, 150 mm _ 4.6 mm ID) at flow 1 mL min-1 and 254 nm UV-detector. HPTLC separations were performed on Merck (20 cm 10 cm) aluminum HPTLC plates coated with silica gel 60F254 using a mobile phase, Methylene chloride: methanol: ethyl acetate: ammonia (25%), (5:1:3:1, v/v/v/v) respectively. The calibration curves were linear across ranges of 3-100 µg mL-1 and 0.1- 2 µg/spot for both HPLC and HPTLC methods, respectively. The two methods were applied successfully for the determination of the three drugs under study in their combined tablets dosage forms. * Oral Presenting author - 60 -
The 1st international ZPSC 2021 Poster Presentation - 61 -
The 1st international ZPSC 2021 Spectrophotometric Determination of Etilefrine HCl, Salbutamol Sulphate and Tiemonium Methyl Sulphate Using Surface Plasmon Resonance Band of Gold Nanoparticles Magda Mohamed Ayad, Hisham Ezzat Abdellatef, Mervat Mohamed Hosny, Naglaa Abdel-Sattar Kabil* Department of Analytical Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. Abstract A simple and sensitive method was developed for spectrophotometric determination of etilefrine hydrochloride, salbutamol sulphate and tiemonium methyl sulphate in pure form and in their pharmaceutical formulations. The method was based on reduction of gold solution to gold nanoparticles by the studied drugs in presence of sodium dodecyl sulphate as stabilising agent. Gold nanoparticles (Au NPs) showed a new absorption band at 530 nm that was used for quantitative determination of the cited drugs. Different variables were examined and optimised in the experiment as gold solution concentration, type of buffer, suitable pH, stabilising agent, order of addition, time and temperature of the reaction. Under optimum conditions, the calibration curves were linear with concentration ranges of 3.0-20.0, 5.0-18.0 and 2.0-26.0 μg/mL for etilefrine hydrochloride, salbutamol sulphate and tiemonium methyl sulphate respectively. The method was applied successfully to determine the studied drugs in pure form and in their pharmaceutical dosage forms, exhibiting good reproducibility and accuracy. * Poster Presenting author - 62 -
The 1st international ZPSC 2021 Spectroscopic determination of hydrochlorothiazide and minoxidil in dosage forms and spiked human urine using NBD-Cl Magda M.Ayad1, Fathalla Belal2, Mervat M.Hosny1, Heba Elmansi2 and Omar M.EL-Abassy3* 1Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt 2Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt 3Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo, Egypt Abstract: Sensitive and validated spectroscopic methods were developed for the estimation of each of hydrochlorothiazide (HCT) and minoxidil (MIN) in their pharmaceuticals. The suggested methods relied on the reaction between the two drugs and 4-chloro-7-nitrobenzofurazan (NBD-CL) at borate buffer of pH 8.5. Method (I) involves measuring the reaction products spectrophotometrically at 470 and 475 nm, for HCT and MTN, respectively. The linearity of the method was obtained over the concentration ranges of 5.0-30.0 µg/ml and 1.0-10.0 µg/ml for HCT and MIN respectively. Method (II) is based on spectrofluorimetric measurement of the reaction products at 554 nm upon excitation at 470 nm and 475 nm for HCT and MTN, respectively .The fluorescence-concentration plots showed good linearity over the ranges of 20.0-100.0ng/ml and 10.0-100.0ng/ml for HCT and MIN, respectively. Successful determination of the studied drugs in dosage forms was accomplished with satisfactory percentage recoveries. Method II was further extended to the in-vitro determination of HCT in human urine samples. The stoichiometry of the reaction was assessed and the mechanism of the complexation reaction was studied and explained. The fluorescence quantum yields of the reaction products of HCT and MIN with NBD-Cl, were determined and were found to be 0.25 and 0.20, respectively. * Poster Presenting author - 63 -
The 1st international ZPSC 2021 Designed by: Nada Rady - 64 -
The 1st international ZPSC 2021 - 65 -
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