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Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
Megahed SH, Rasheed S, Herrmann J, El-Hossary EM, El-Shabrawy YI, Abadi AH, Engel M, Müller R, Abdel-Halim M, Hamed MM. Megahed SH, et al. Bioorg Med Chem Lett. 2022 Mar 1;59:128531. doi: 10.1016/j.bmcl.2022.128531. Epub 2022 Jan 7. Bioorg Med Chem Lett. 2022. PMID: 35007723
Compound 12 showed a 2-4 fold improvement in activity than I against S. aureus Newman, S. pneumoniae DSM-20566 and E. faecalis DSM-20478. ...
Compound 12 showed a 2-4 fold improvement in activity than I against S. aureus Newman, S. pneumoniae DSM-20566 and E. f …
Synthesis of novel 1,2-diarylpyrazolidin-3-one-based compounds and their evaluation as broad spectrum antibacterial agents.
Mokbel SA, Fathalla RK, El-Sharkawy LY, Abadi AH, Engel M, Abdel-Halim M. Mokbel SA, et al. Bioorg Chem. 2020 Jun;99:103759. doi: 10.1016/j.bioorg.2020.103759. Epub 2020 Mar 14. Bioorg Chem. 2020. PMID: 32220665
The oxime derivative 24 exhibited promising antibacterial activity against E. coli TolC, B. subtilis and S. aureus with MIC values of 4, 10 and 20 g/mL, respectively. The new lead compound 24 was found to exhibit a weak dual inhibitory activity against both the E …
The oxime derivative 24 exhibited promising antibacterial activity against E. coli TolC, B. subtilis and S. aureus with MIC va …
Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity.
El-Gamil DS, ElHady AK, Chen PJ, Hwang TL, Abadi AH, Abdel-Halim M, Engel M. El-Gamil DS, et al. Eur J Med Chem. 2023 Feb 5;247:115019. doi: 10.1016/j.ejmech.2022.115019. Epub 2022 Dec 15. Eur J Med Chem. 2023. PMID: 36580731
Clk1 kinase is a key modulator of the pre-mRNA alternative splicing machinery which has been proposed as a promising target for treatment of various tumour types, Duchenne's muscular dystrophy and viral infections such as HIV-1 and influenza. ...
Clk1 kinase is a key modulator of the pre-mRNA alternative splicing machinery which has been proposed as a promising target for treatment of …
Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker.
El-Gamil DS, ElHady AK, Chen PJ, Hwang TL, Abadi AH, Abdel-Halim M, Engel M. El-Gamil DS, et al. Eur J Med Chem. 2022 Aug 5;238:114411. doi: 10.1016/j.ejmech.2022.114411. Epub 2022 Apr 26. Eur J Med Chem. 2022. PMID: 35635953
Potency of this series was found to be mainly dependent on the presence of an intramolecular H-bond between an ortho-methoxy group and the imide NH, that stabilizes a nearly coplanar conformation of high affinity to the ATP binding pocket(s) of Clk1/4. The two most potent …
Potency of this series was found to be mainly dependent on the presence of an intramolecular H-bond between an ortho-methoxy group and the i …