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Mostafa M Ghorab,1 Ali S Alqahtani,2,3 Aiten M Soliman,1 Ahmed A Askar4 1Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), Cairo 11765, Egypt; 2Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 3Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; 4Botany and Microbiology Department, Faculty of Science (Boys), Al-Azhar University, Cairo, EgyptCorrespondence: Mostafa M Ghorab; Ali S Alqahtani Tel +20 1067846727Email mmsghorab@yahoo.com; Alalqahtani@ksu.edu.saAim: With the rapid emergence of antibiotic resistance, efforts are being made to obtain new selective antimicrobial agents. Hybridization between quinazolinone and benzenesulfonamide can provide new antimicrobial candidates. Also, the use of nanoparticles can help boost drug efficacy and lower side effects.Materials and Methods: Novel quinazolinone-benzenesulfonamide derivatives 5– 18 were synthesized and screened for their antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria, MRSA and yeast. The most potent compound 16 was conjugated with copper oxide nanoparticles 16-CuONPs by gamma irradiation (4.5 KGy). Characterization was performed using UV–Visible, TEM examination, XRD patterns and DLS. Moreover, compound 16 was used to synthesize two nanoformulations: 16-CNPs by loading 16 in chitosan nanoparticles and the nanocomposites 16-CuONPs-CNPs. Characterization of these nanoformulations was performed using TEM and zeta potential. Besides, the inhibitory profile against Staphylococcus aureus DNA gyrase was assayed. Cytotoxic evaluation of 16, 16-CNPs and 16-CuONPs-CNPs on normal VERO cell line was carried out to determine its relative safety. Molecular docking of 16 was performed inside the active site of S. aureus DNA gyrase.Results: Compound 16 was the most active in this series against all the tested strains and showed inhibition zones and MICs in the ranges of 25– 36 mm and 0.31– 5.0 μg/mL, respectively. The antimicrobial screening of the synthesized nanoformulations revealed that 16-CuONPs-CNPs displayed the most potent activity. The MBCs of 16 and the nanoformulations were measured and proved their bactericidal mode of action. The inhibitory profile against S.aureus DNA gyrase showed IC50 ranging from 10.57to 27.32 μM. Cytotoxic evaluation of 16, 16-CNPs and 16-CuONPs-CNPs against normal VERO cell lines proved its relative safety (IC50= 927, 543 and 637 μg/mL, respectively). Molecular docking of 16 inside the active site of S. aureus DNA gyrase showed that it binds in the same manner as that of the co-crystallized ligand, ciprofloxacin.Conclusion: Compound 16 could be considered as a new antimicrobial lead candidate with enhanced activity upon nanoformulation.Keywords: quinazolinone, benzenesulfonamide, antimicrobial, nanoparticles, nanoformulations, MBC, Staphylococcus aureus DNA gyrase, docking

Introduction: Scholarship applicants often receive different advice on what should be included in their Curriculum Vitae (CV). This study aims to investigate what the essential components of a CV being prepared for scholarships are, how to present them, and what their level of impact is. Materials and Methods: The authors sent an online structured questionnaire to 7512 corresponding authors of recent published papers in Scopus; 124 completed questionnaires were returned. Recommended elements for a CV were chosen according to the Delphi consensus technique with a threshold of 50%. Results: This survey revealed that headings, bullet points and careful error checking were essential parts of the layout. For the content of the CV, besides publications, education and training background, research experience and research interest were also necessary. Moreover, almost all respondents ranked publications as the most important qualification of an academic scholarship candidate. Publications also came first as the most impressive factor, followed by awards and honours. The number of publications, quality of journal, impact factor and total citation should be presented in publication section. The importance of publications in getting academic scholarships is significantly emphasized in this recent study. Conclusions: Having research experience and papers in peer review journals, are highly recommended for students seeking academic scholarships.

Mostafa M Ghorab,1,2 Mansour S Alsaid,1 Maureen Higgins,3 Albena T Dinkova-Kostova,3–5 Abdelaaty A Shahat,1,6 Nehal H Elghazawy,7 Reem K Arafa7,8 1Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia; 2Department of Drug Radiation Research, National Center for Radiation Research & Technology, Atomic Energy Authority, Cairo, Egypt; 3Jacqui Wood Cancer Centre, Division of Cancer Research, Medical Research Institute, University of Dundee, Dundee, UK; 4Department of Medicine, 5Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA; 6Phytochemistry Department, National Research Center, Dokki, Giza, 7Zewail City of Science and Technology, 8Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo,Egypt Abstract: The Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant response elements pathway enables cells to survive oxidative stress conditions through regulating the expression of cytoprotective enzymes such as NAD(P)H:quinone oxidoreductase 1 (NQO1). This work presents the design and synthesis of novel anilinoquinazoline derivatives (2–16a) and evaluation of their NQO1 inducer activity in murine cells. Molecular docking of the new compounds was performed to assess their ability to inhibit Keap1–Nrf2 protein–protein interaction through occupying the Keap1–Nrf2-binding domain, which leads to Nrf2 accumulation and enhanced gene expression of NQO1. Docking results showed that all compounds can potentially interact with Keap1; however, 1,5-dimethyl-2-phenyl-4-(2-phenylquinazolin-4-ylamino)-1,2-dihydropyrazol-3-one (9), the most potent inducer, showed the largest number of interactions with key amino acids in the binding pocket (Arg483, Tyr525, and Phe478) compared to the native ligand or any other compound in this series. Keywords: Kelch domain, molecular modeling, Keap1/Nrf2, cytoprotection, NQO1 induction