Mohamed H. elshershaby

Scopus Publications

Rational design and synthesis of novel phenyltriazole derivatives targeting MRSA cell wall biosynthesis
Mohamed M. Elsebaei, Hany G. Ezzat, Ahmed M. Helal, Mohamed H. El-Shershaby, Mohammed S. Abdulrahman, Moaz Alsedawy., Ahmed K. B. Aljohani, Mohammed Almaghrabi, Marwa Alsulaimany, Basmah Almohaywi,et al.
Royal Society of Chemistry (RSC)
Antimicrobial resistance in methicillin-resistant Staphylococcus aureus (MRSA) is a major global health challenge.

The antimicrobial potential and pharmacokinetic profiles of novel quinoline-based scaffolds: synthesis andin silicomechanistic studies as dual DNA gyrase and DHFR inhibitors
Mohamed H. El-Shershaby, Kamal M. El-Gamal, Ashraf H. Bayoumi, Khaled El-Adl, Mohamed Alswah, Hany E. A. Ahmed, Ahmed A. Al-Karmalamy, and Hamada S. Abulkhair
Royal Society of Chemistry (RSC)
The resistance of pathogenic microbes to currently available antimicrobial agents has been considered a global alarming concern.

From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity
Mohamed H. El-Shershaby, Adel Ghiaty, Ashraf H. Bayoumi, Ahmed A. Al-Karmalawy, Ebtehal M. Husseiny, Mona S. El-Zoghbi, and Hamada S. Abulkhair
Elsevier BV

1,2,4-Triazolo[4,3-c]quinazolines: a bioisosterism-guided approach towards the development of novel PCAF inhibitors with potential anticancer activity
Mohamed H. El-Shershaby, Adel Ghiaty, Ashraf H. Bayoumi, Hany E. A. Ahmed, Mona S. El-Zoghbi, Khaled El-Adl, and Hamada S. Abulkhair
Royal Society of Chemistry (RSC)
Targeting PCAF with small inhibitor molecules has emerged as a potential therapeutic strategy for the treatment of cancer.

Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives
Mohamed H. El‐Shershaby, Kamal M. El‐Gamal, Ashraf H. Bayoumi, Khaled El‐Adl, Hany E. A. Ahmed, and Hamada S. Abulkhair
Wiley
Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed against a panel of pathogenic microbes including Gram‐positive bacteria (Streptococcus pneumoniae and Bacillus subtilis), Gram‐negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungal strains (Aspergillus fumigatus, Syncephalastrum racemosum, Geotrichum candidum, and Candida albicans). Compounds that revealed the best activity were subjected to further biological studies to determine their minimum inhibitory concentrations (MICs) against the selected pathogens as well as their in vitro activity against the E. coli DNA gyrase, to realize whether their antimicrobial action is mediated via inhibition of this enzyme. Four of the new derivatives (14, 17, 20, and 23) demonstrated a relatively potent antimicrobial activity with MIC values in the range of 0.66–5.29 μg/ml. Among them, compound 14 exhibited a particularly potent broad‐spectrum antimicrobial activity against most of the tested strains of bacteria and fungi, with MIC values in the range of 0.66–3.98 μg/ml. A subsequent in vitro investigation against the bacterial DNA gyrase target enzyme revealed a significant potent inhibitory activity of quinoline derivative 14, which can be observed from its IC50 value (3.39 μM). Also, a molecular docking study of the most active compounds was carried out to explore the binding affinity of the new ligands toward the active site of DNA gyrase enzyme as a proposed target of their activity. Furthermore, the ADMET profiles of the most highly effective derivatives were analyzed to evaluate their potentials to be developed as good drug candidates.