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8 results on '"Elgaher, Walid A.M."'

2. A hydrogel-based in vitro assay for the fast prediction of antibiotic accumulation in Gram-negative bacteria

Author

Richter, Robert, Kamal, Mohamed.A.M., García-Rivera, Mariel A., Kaspar, Jerome, Junk, Maximilian, Elgaher, Walid A.M., Srikakulam, Sanjay Kumar, Gress, Alexander, Beckmann, Anja, Grißmer, Alexander, Meier, Carola, Vielhaber, Michael, Kalinina, Olga, Hirsch, Anna K.H., Hartmann, Rolf W., Brönstrup, Mark, Schneider-Daum, Nicole, and Lehr, Claus-Michael

Published
2020
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5. NRF2 activators inhibit influenza A virus replication by interfering with nucleo-cytoplasmic export of viral RNPs in an NRF2-independent manner

Author

Waqas, Fakhar H., primary, Shehata, Mahmoud, additional, Elgaher, Walid A.M., additional, Lacour, Antoine, additional, Kurmasheva, Naziia, additional, Begnini, Fabio, additional, Kiib, Anders E., additional, Dahlmann, Julia, additional, Chen, Chutao, additional, Poulsen, Thomas B., additional, Merkert, Sylvia, additional, Martin, Ulrich, additional, Olmer, Ruth, additional, Olagnier, David, additional, Hirsch, Anna K.H., additional, Pleschka, Stephan, additional, and Pessler, Frank, additional

Published
2023
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6. Design, Synthesis, Antimicrobial Activity, and Molecular Docking of Some New Diclofenac Derivatives.

Author

Tolba, Mahmoud S., Hamed, Mahmoud M., Sayed, Mostafa, Kamal El-Dean, Adel M., Abdel-Mohsen, Shawkat A., Ibrahim, Omneya A., Elgaher, Walid A.M., Hirsch, Anna K. H., and Saddik, Abdelreheem Abdelfatah

Subjects
ANTI-infective agents, DICLOFENAC, ACYLATION, CHEMICAL synthesis, MASS spectrometry, MOLECULAR docking, SECONDARY amines, HYDRAZINE derivatives
Abstract

Due to the biological importance of diclofenac derivatives which are included in the composition of the active substance in many medicines used in the treatment of infections. Herein, we present a facile procedure for the synthesis of a new series of diclofenac analogous, in excellent isolated yields starting from the carbohydrazide precursor 1. Acylation and condensation of NH2 group in the starting material with different reagents delivered compounds (2–5). Moreover, the Nucleophilic substitution of chloromethyl derivative 5 with primary and secondary amines gave compounds (6a, 6b, and 7). Furthermore, the hydrazine compound (7) reaction with benzaldehyde and chloroacetylchloride produced derivatives (8, 9). The chemical structures of all newly synthesized compounds have been proved based on elemental and spectral analysis techniques (FTIR, 1HNMR, 13CNMR, and Mass spectroscopy). All synthesized compounds were investigated for their in-vitro antimicrobial activity against different strains of bacteria and fungi in moderate to high activity. A molecular docking approach was utilized to investigate the proposed molecular mechanism of the antibacterial and antifungal activity of the synthesized compounds. [ABSTRACT FROM AUTHOR]

Published
2023
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8. Cystobactamid 507 : Concise Synthesis, Mode of Action, and Optimization toward More Potent Antibiotics

Author

Elgaher, Walid A.M., Hamed, Mostafa M., Baumann, Sascha, Herrmann, Jennifer, Siebenbürger, Lorenz, Krull, Jana, Cirnski, Katarina, Kirschning, Andreas, Müller, Rolf, and Hartmann, Rolf W.

Subjects
Dewey Decimal Classification::500 | Naturwissenschaften::540 | Chemie, Dewey Decimal Classification::600 | Technik::660 | Technische Chemie, antimicrobial agents, gram-negative bacteria, antibiotics, metabolic stability, concise synthesis, anti-bacterial activity, topoisomerase iia, bioactive conformation, ddc:540, ddc:660, antimicrobial resistances, bacteria, total synthesis
Abstract

Lack of new antibiotics and increasing antimicrobial resistance are among the main concerns of healthcare communities nowadays, and these concerns necessitate the search for novel antibacterial agents. Recently, we discovered the cystobactamids—a novel natural class of antibiotics with broad-spectrum antibacterial activity. In this work, we describe 1) a concise total synthesis of cystobactamid 507, 2) the identification of the bioactive conformation using noncovalently bonded rigid analogues, and 3) the first structure–activity relationship (SAR) study for cystobactamid 507 leading to new analogues with high metabolic stability, superior topoisomerase IIA inhibition, antibacterial activity and, importantly, stability toward the resistant factor AlbD. Deeper insight into the mode of action revealed that the cystobactamids employ DNA minor-groove binding as part of the drug–target interaction without showing significant intercalation. By designing a new analogue of cystobactamid 919-2, we finally demonstrated that these findings could be further exploited to obtain more potent hexapeptides against Gram-negative bacteria. © 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.

Published
2020

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