A New Efficient Convergent Synthesis of Conjugated Aryl-containing Dendrimers

Ibrahim Mustafa El-Deeb,이소하 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.6

New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening

Ibrahim Mustafa El-Deeb,한동근,김인태,이소하 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.7

Phenylaminopyrimidines represent a large group of new selective anticancer agents, the majority of which exert their action through the inhibition of specific kinases. In this study, a new series of N-substituted-2-aminopyrimidines has been designed and synthesized. A selected group of the synthesized derivatives was screened at a single dose concentration of 10 μM over a panel of 60 cancer cell-lines. Compound 12e has showed great inhibitory and strong lethal effect over almost all of the 60 cell-lines and accordingly was further tested in a 5-dose testing mode to determine its IC50 values,where it showed great efficacies with intermediate potencies over the tested cell-lines. The compound was also tested over a panel of 52 kinases to explore its kinase inhibitory profile, and was found to be a selective but moderate inhibitor over FLT3 kinase.

Synthesis of New N, N-Bis(5-acetylpyridin-2-yl)-phenylamine Derivatives and Their Solvatochromic Effects

( Ibrahim Mustafa Ei Deeb ),( So Ha Lee ) 한국유화학회 2008 한국응용과학기술학회지 Vol.25 No.4

Association of Syntax Score II with Contrast-induced Nephropathy and Hemodialysis Requirement in Patients with ST Segment Elevation Myocardial Infarction Undergoing Primary Percutaneous Coronary Intervention

Ibrahim Rencuzogullari,Metin Çağdaş,Süleyman Karakoyun,Yavuz Karabağ,Mahmut Yesin,Mustafa Ozan Gürsoy,İnanç Artaç,Doğan İliş,Süleyman Çağan Efe,Kevser Tural,Ibrahim Halil Tanboğa 대한심장학회 2018 Korean Circulation Journal Vol.48 No.1

Background and Objectives Contrast-induced nephropathy (CIN) is a common complication of primary percutaneous coronary intervention (pPCI) and is associated with high mortality and morbidity and long hospital stay in patients with ST elevation myocardial infarction (STEMI). The Syntax Score (SS) has previously been studied in STEMI patients, and it was associated with increased CIN development and long-term mortality. This study investigates a possible relationship between CIN development and Syntax Score II (SSII) and compares SS and SSII by assessing CIN risk in STEMI patients treated with pPCI. Methods A total of 1,234 patients who underwent pPCI were divided into 2 groups according to CIN development. Patients with CIN were further divided into 2 groups according to whether or not they required hemodialysis. Reclassification tables, net reclassification improvement, and integrated discriminative improvement methods were used to assess the additive predictive value of SSII for predicting CIN. Results In the present study, 166 patients (13.5%) had CIN. Although both SS and SSII were significantly higher in CIN patients, only SSII was an independent predictor of CIN (odds ratio [OR], 1.031; 95% confidence interval [CI], 1.012–1.051; p<0.001) and hemodialysis requirement (OR, 1.078; 95% CI, 1.046–1.078; p<0.001). When comparing SSII and SS in their ability to determine CIN risk, we found SSII to have a reclassification improvement of 27.59% (p<0.001) and an integrated discrimination improvement of 9.1% (p<0.001). Conclusions The combination of clinical and anatomic variables can more accurately identify patients who are at high risk for CIN after pPCI. While SSII is harder to calculate than SS, it provides better prediction for CIN and hemodialysis requirement than SS.

Synthesis of N,N-Diaryl-(pyridin-3-yl)pyrimidin-2-amine Derivatives and Their Photochemical Properties

Ibrahim Mustafa El-Deeb,So-Ha Lee 한국유화학회 2008 한국응용과학기술학회지 Vol.25 No.3

Although the pyrimidine derivatives were obtained in low yields ranging from 8% to 20%, we reported the successful preparation of N,N-diaryl-pyrimidin-2-amine derivatives starting from the corresponding 2-aminopyrimidines (1a-1c), by direct palladium-catalyzed arylation using different arylbromides. The reasons of low yields are thought to be the electronic and steric effects by the neighboring aromatic systems. The absorption spectra and photoluminescent spectra of compounds (3a 3g and 4a-4c) were measured using dichloromethane on the concentration of 25 mM by UV vis spectroscopy and luminescent spectroscopy. Pyrimidine derivatives 4a, 4b, and 4c showed moderate emission maxima at 474 nm, 481 nm, and 367 nm, respectively, while other compounds showed very weak photoluminescence or no photoluminescence at all.

Effects of different nitrogen doses and cultivars on fermentation quality and nutritive value of Italian ryegrass (Lolium multiflorum Lam.) silages

Ertekin Ibrahim,Atis Ibrahim,Aygun Yusuf Ziya,Yilmaz Saban,Kizilsimsek Mustafa 아세아·태평양축산학회 2022 Animal Bioscience Vol.35 No.1

Objective: The fermentation profile and silage quality of 3 Italian ryegrass (Lolium multiflorum Lam.) cultivars (cvs. Devis, Hellen, and Trinova) treated with 5 nitrogen doses (0, 50, 100, 150, and 200 kg/ha) were evaluated. Methods: The experiment was laid out in split plot in randomized complete block design with three replications. Annual ryegrass cultivars used in this study have been commonly grown in Turkey. Nitrogen doses were set in main plot and cultivars in split plot in the field. Plants were harvested at full-flowering stage with dry matter content about 220 g/kg for first cutting and 260 g/kg for second cutting. Harvested plants were chopped theoretically into 2 to 3 cm lengths for ensiling. Chopped fresh materials were ensilaged by compressing in 2 L plastic jars about 3±0.1 kg. Results: Effects of N doses on dry matter, neutral detergent fiber, acid detergent fiber, dry matter digestibility, relative feed value, crude protein, pH, ammonia nitrogen, lactic acid, acetic acid, and lactic acid/acetic acid were statistically significant while water soluble carbohydrate, ash and organic matter were not statistically different. Ammonia nitrogen, crude protein, ash, organic matter, lactic acid, and lactic acid/acetic acid were affected by cultivars, but the other parameters were not. Increasing nitrogen applications positively affected the chemical composition of annual ryegrass silage. The significant increase in protein content was remarkable, however, silage fermentation properties were adversely affected by the increasing nitrogen dose. Conclusion: It can be recommended 150 kg/ha nitrogen dose for annual ryegrass harvested at full blooming stage. Even though the silage fermentation properties of the used cultivars were similar, cv. Devis gave better results than the others in terms of silage pH and relative feed value. Objective: The fermentation profile and silage quality of 3 Italian ryegrass (Lolium multiflorum Lam.) cultivars (cvs. Devis, Hellen, and Trinova) treated with 5 nitrogen doses (0, 50, 100, 150, and 200 kg/ha) were evaluated.Methods: The experiment was laid out in split plot in randomized complete block design with three replications. Annual ryegrass cultivars used in this study have been commonly grown in Turkey. Nitrogen doses were set in main plot and cultivars in split plot in the field. Plants were harvested at full-flowering stage with dry matter content about 220 g/kg for first cutting and 260 g/kg for second cutting. Harvested plants were chopped theoretically into 2 to 3 cm lengths for ensiling. Chopped fresh materials were ensilaged by compressing in 2 L plastic jars about 3±0.1 kg.Results: Effects of N doses on dry matter, neutral detergent fiber, acid detergent fiber, dry matter digestibility, relative feed value, crude protein, pH, ammonia nitrogen, lactic acid, acetic acid, and lactic acid/acetic acid were statistically significant while water soluble carbohydrate, ash and organic matter were not statistically different. Ammonia nitrogen, crude protein, ash, organic matter, lactic acid, and lactic acid/acetic acid were affected by cultivars, but the other parameters were not. Increasing nitrogen applications positively affected the chemical composition of annual ryegrass silage. The significant increase in protein content was remarkable, however, silage fermentation properties were adversely affected by the increasing nitrogen dose.Conclusion: It can be recommended 150 kg/ha nitrogen dose for annual ryegrass harvested at full blooming stage. Even though the silage fermentation properties of the used cultivars were similar, cv. Devis gave better results than the others in terms of silage pH and relative feed value.

In silico molecular docking and molecular dynamic simulation of potential inhibitors of 3C-like main proteinase (3CLpro) from severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) using selected african medicinal plants

Isa Mustafa Alhaji,Mustapha Adam,Qazi Sahar,Raza Khalid,Allamin Ibrahim Alkali,Ibrahim Muhammad M.,Mohammed Mohammed M. 경희대학교 융합한의과학연구소 2022 Oriental Pharmacy and Experimental Medicine Vol.22 No.1

The Severe Acute Respiratory Syndrome 2 (SARS-CoV-2) is an infectious virus that causes mild to severe life-threatening upper respiratory tract infection. The virus emerged in Wuhan, China in 2019, and later spread across the globe. Its genome has been completely sequenced and based on the genomic information, the virus possessed 3C-Like Main Protease (3CLpro), an essential multifunctional enzyme that plays a vital role in the replication and transcription of the virus by cleaving polyprotein at eleven various sites to produce different non-structural proteins. This makes the protein an important target for drug design and discovery. Herein, we analyzed the interaction between the 3CLpro and potential inhibitory com- pounds identified from the extracts of Zingiber offinale and Anacardium occidentale using in silico docking and Molecular Dynamics (MD) Simulation. The crystal structure of SARS-CoV-2 main protease in complex with 02J (5-Methylisoxazole- 3-carboxylic acid) and PEJ (composite ligand) (PDB Code: 6LU7, 2.16 Å) retrieved from Protein Data Bank (PDB) and subject to structure optimization and energy minimization. A total of twenty-nine compounds were obtained from the extracts of Z. offinale and the leaves of A. occidentale. These compounds were screened for physicochemical (Lipinski rule of five, Veber rule, and Egan filter), Pan-Assay Interference Structure, and pharmacokinetic properties to determine the Pharmaceutical Active Ingredients. Of the 29 compounds, only nineteen (19) possessed drug-likeness properties with efficient oral bioavailability and less toxicity. These compounds subjected to molecular docking analysis to determine their binding energies with the 3CLpro. The result of the analysis indicated that the free binding energies of the compounds ranged between − 5.08 and − 10.24 kcal/mol, better than the binding energies of 02j (− 4.10 kcal/mol) and PJE (− 5.07 kcal/ mol). Six compounds (CID_99615 = − 10.24 kcal/mol, CID_3981360 = 9.75 kcal/mol, CID_9910474 = − 9.14 kcal/mol, CID_11697907 = − 9.10 kcal/mol, CID_10503282 = − 9.09 kcal/mol and CID_620012 = − 8.53 kcal/mol) with good bind- ing energies further selected and subjected to MD Simulation to determine the stability of the protein–ligand complex. The results of the analysis indicated that all the ligands form stable complexes with the protein, although, CID_9910474 and CID_10503282 had a better stability when compared to other selected phytochemicals (CID_99615, CID_3981360, CID_620012, and CID_11697907).

OPTIMIZED FAST TERMINAL SLIDING MODE CONTROL FOR A HALF-CAR ACTIVE SUSPENSION SYSTEMS

Ghazally Ibrahim Yousif Mustafa,Haoping Wang,Yang Tian 한국자동차공학회 2020 International journal of automotive technology Vol.21 No.4

This paper presents an optimized sliding mode controller (OPSMC) for vibration control of active suspension systems. The proposed controller consists of two parts: the first is the fast terminal sliding mode controller which performs fast convergence, and the second is the particle swarm optimization algorithm which is used to achieve the optimal controller’s\' parameters. The merit of OPSMC has quite simple structure and easy to be regulated, as well as improve the tracking performance. The half-car active suspension systems with non-linearity such as the parameters variation and external disturbance are simultaneously taken into account to provide a realistic framework. The control objective is to deal with the classical conflict between minimizing vertical and angular chassis accelerations to increase the ride comfort. Versus, to keep minimum dynamic wheel loads and suspension deflections to ensure the ride safety. Finally, to show the performance of the proposed OPSMC, the comparison with a recently developed efficient method called optimization and static output-feedback control (OPSOFC) is conducted with different roads disturbances.

Synthesis of N,N-Diaryl-(pyridin-3-yl)pyrimidin-2-amine Derivatives and Their Photochemical Properties

El-Deeb, Ibrahim Mustafa,Lee, So-Ha The Korean Society of Applied Science and Technolo 2008 한국응용과학기술학회지 Vol.25 No.3

Although the pyrimidine derivatives were obtained in low yields ranging from 8% to 20%, we reported the successful preparation of N,N-diaryl-pyrimidin-2-amine derivatives starting from the corresponding 2-aminopyrimidines (1a-1c), by direct palladium-catalyzed arylation using different arylbromides. The reasons of low yields are thought to be the electronic and steric effects by the neighboring aromatic systems. The absorption spectra and photoluminescent spectra of compounds (3a 3g and 4a-4c) were measured using dichloromethane on the concentration of 25 mM by UV vis spectroscopy and luminescent spectroscopy. Pyrimidine derivatives 4a, 4b, and 4c showed moderate emission maxima at 474 nm, 481 nm, and 367 nm, respectively, while other compounds showed very weak photoluminescence or no photoluminescence at all.

Synthesis of New N,N-Bis(5-acetylpyridin-2-yl)-phenylamine Derivatives and Their Solvatochromic Effects

El-Deeb, Ibrahim Mustafa,Lee, So-Ha The Korean Society of Applied Science and Technolo 2008 한국응용과학기술학회지 Vol.25 No.4

A group of new N,N-bis(5-acetylpyridin-2-yl)phenylamine derivatives was synthesized in good yield applying an optimized Buchwald-Hartwig amination protocol. The synthesized compounds showed UV absorption maxima in the range of 320-360 nm, and showed good luminescence at dilute concentrations in the blue region of the spectra (in the range of 480-497 nm). They showed also a bathochromic shift associating the increase in solvent polarity. The synthesized compounds could be investigated for use in OLEDs or as potential monomers for PLEDs.