New Synthesis of 2-Substituted Imidazo[2, 1-b]thiazoles and their Antimicrobial Activities

Mahfouz, A.Abdel Aziz,Elhabashy, F.M. The Pharmaceutical Society of Korea 1990 Archives of Pharmacal Research Vol.13 No.1

4, 5-Diphenyl-2-mercaptiomidazole (I) was reacted with hydraziodyl halides IIa-d togive the S-alkyl derivatives III-a-d. Cyclization of IIIa-d afforded imidazo[2, 1-b]-thiazole derivatives Vla, b and VII. Treatment of 1 with a-chloroethylacetoaccetate (IV) gave ethyl 2(4, 5-diphenyl-2-imidazolinylthio)-3-keto-butyrate (V). Compound V coupled with benzendiazonium chloride to give the corresponding phenylhydrazo compound IIId. On heating V with polyphosphoric acid, cyclization took place and 2-acetyl-5, 6-diphenyl-imidazo [2, 1-b] thiazol-3-one (VIII) was obtained. The compound VIII was condensed with aromatic aldehydes to yield the cinnamoyl derivatives 1Xa, b. The antimicrobial activities of compounds IIIa-d, V, VIa, VII were examined.

New Synthesis of Chromonopyrroloimidazolinones and Arylidene Thioxoimidazolinones -Study of their antimicrobial activities-

Abdel Aziz, Mahfouz A.,Riad, Bahia Y.,Shalaby, A.M. The Pharmaceutical Society of Korea 1989 Archives of Pharmacal Research Vol.12 No.1

6-Formyl-5-methoxy-2-methyl chromone derivatives condensed with 2-thiox-4-imidazolinone derivatives to form the corresponding '10-methoxy-7-methyl-3-thioxo-chromone[6,7-b]pyrrolo[1,2-a-]-imidazolin-1-one derivatives (IIIa-f) or the 5-arvlidene-2-thioxo-4-imidazolinone derivatives(IVa-f). The activity of the NH in the imidazol moiety of (IIIa) was confirmed by formation of the Mannich bases (Va, b). Moreover, alkylation of (IIIa) was undertaken to give the alkylmercapto derivatives (VIa, b). The antimicrobial activities of compounds IIIb-e, IVa, IVe were studied.

Effectiveness and early postoperative outcomes of palliative endoluminal stenting versus Hartmann’s procedure in acute malignant bowel obstruction in high-risk patients

Mohammed Fayek Mahfouz,Tamer M. Saeid Salama,Amr H. Afifi,Hany Mansour Khalil Dabous 대한대장항문학회 2022 Annals of Coloproctolgy Vol.38 No.2

Purpose: The emergency intervention for acute malignant left-sided colonic obstruction remains controversial. Conflicting reports exist regarding the efficacy and safety of endoscopic placement of self-expandable metallic stents (SEMS) vs. primary surgery. Most reports focus on SEMS insertion as a bridge to surgery. Methods: An observational nonrandomized study at a single center in Cairo, Egypt included 65 high-risk patients (American Society of Anesthesiologists physical status classification ≥III, age >60 years) with acute malignant metastatic (stage IV) colonic obstruction. Twenty-nine patients underwent primary surgery (Hartmann’s procedure, HP), and 35 patients underwent SEMS insertion. Results: All cases that underwent SEMS insertion were technically successful. The 2 procedures were comparable in clinical success rates but a statistically significant difference existed between them regarding the duration of postoperative hospital stay in the HP and SEMS group (7.7±3.1 days vs. 3.5±0.6 days, retrospectively; P<0.001), the interval before regaining oral feeding (41.8±26.8 hours vs. 27.6±18.5 hours, retrospectively; P=0.015), and the duration of intensive care unit (ICU) admission (5.0±1.7 days vs. 1.5±0.7 days, retrospectively; P=0.035). Six patients (20.7%) in the HP group and 2 patients (5.7%) in the SEMS group required postoperative ICU admission. Conclusion: SEMS placement provides comparable efficacy and safety to HP in managing acute malignant obstruction of the rectosigmoid region in high-risk individuals, with faster recovery and less hospital and ICU admission time.

Numerical investigation of the three-dimensional dynamic process of sabot discard

HUANG Zhen-gui,WESSAM Mahfouz Elnaggar,CHEN Zhi-hua 대한기계학회 2014 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.28 No.7

The sabot discard process of an armor-piercing, fin-stabilized discarding sabot (APFSDS) is crucial for the flight stability of the projectile. In this paper, the sabot discard behavior after projectile ejection from the muzzle is investigated at Mach number 4.0 and angle ofattack of 0°. 3D compressible equations implemented with a dynamic unstructured tetrahedral mesh are numerically solved with a commercialcomputational fluid dynamics (CFD) code (FLUENT 12.0). Six-degrees-of-freedom (6DOF) rigid-body motion equations issolved with the CFD results through a user-defined function to update the sabot trajectory at every time step. A combination of springbasedsmoothing and local re-meshing is employed to regenerate the meshes around the sabot and describe its movement at each timestep. Computational results show three different separation processes during the sabot discard process. Furthermore, the aerodynamicforces of APFSDS are calculated, and the trajectories of the three sabots are illustrated through the numerical solution of 6DOF equations. The results of the present study agree well with typical experimental results and provide detailed parameters that are important for analyzingthe stability of the projectile. The present computations confirm that the numerical solution of the governing equations of aerodynamicsand 6DOF rigid-body equations are a feasible method to study the sabot discard processes of APFSDS.

Genome editing: the road of CRISPR/Cas9 from bench to clinic

Ayman Eid,Magdy M Mahfouz 생화학분자생물학회 2016 Experimental and molecular medicine Vol.48 No.-

Molecular scissors engineered for site-specific modification of the genome hold great promise for effective functional analyses of genes, genomes and epigenomes and could improve our understanding of the molecular underpinnings of disease states and facilitate novel therapeutic applications. Several platforms for molecular scissors that enable targeted genome engineering have been developed, including zinc-finger nucleases (ZFNs), transcription activator-like effector nucleases (TALENs) and, most recently, clustered regularly interspaced palindromic repeats (CRISPR)/CRISPR-associated-9 (Cas9). The CRISPR/Cas9 system’s simplicity, facile engineering and amenability to multiplexing make it the system of choice for many applications. CRISPR/Cas9 has been used to generate disease models to study genetic diseases. Improvements are urgently needed for various aspects of the CRISPR/Cas9 system, including the system’s precision, delivery and control over the outcome of the repair process. Here, we discuss the current status of genome engineering and its mplications for the future of biological research and gene therapy.

Alanine and serine functionalized magnetic nano-based particles for sorption of Nd(III) and Yb(III)

Galhoum, Ahmed A.,Mahfouz, Mohammad G.,Atia, Asem A.,Gomaa, Nabawia A.,Abdel-Rehem, Sayed T.,Vincent, Thierry,Guibal, Eric Techno-Press 2016 Advances in environmental research Vol.5 No.1

Magnetic nano-based sorbents have been synthesized for the recovery of two rare earth elements (REE: Nd(III) and Yb(III)). The magnetic nano-based particles are synthesized by a one-pot hydrothermal procedure involving co-precipitation under thermal conditions of Fe(III) and Fe(II) salts in the presence of chitosan. The composite magnetic/chitosan material is crosslinked with epichlorohydrin and modified by grafting alanine and serine amine-acids. These materials are tested for the binding of Nd(III) (light REE) and Yb(III) (heavy REE) through the study of pH effect, sorption isotherms, uptake kinetics, metal desorption and sorbent recycling. Sorption isotherms are well fitted by the Langmuir equation: the maximum sorption capacities range between 9 and 18 mg REE $g^{-1}$ (at pH 5). The sorption mechanism is endothermic (positive value of ${\Delta}H^{\circ}$) and contributes to increase the randomness of the system (positive value of ${\Delta}S^{\circ}$). The fast uptake kinetics can be described by the pseudo-second order rate equation: the equilibrium is reached within 4 hours of contact. The sub-micron size of sorbent particles strongly reduces the contribution of resistance to intraparticle diffusion in the control of uptake kinetics. Metal desorption using acidified thiourea solutions allows maintaining sorption efficiency for at least four successive cycles with limited loss in sorption capacity.

Recent advances in the synthesis and applications of magnetic polymer nanocomposites

Abdullatif Jazzar,Haleema Alamri,Yassine Malajati,Remi Mahfouz,Mohamed Bouhrara,Aziz Fihri 한국공업화학회 2021 Journal of Industrial and Engineering Chemistry Vol.99 No.-

The rapid growth of the global population, urbanization, and environmental awareness resulted in asignificant increase of the demand for clean water. As a result, water pollution associated with industrialactivities became a major global concern, and organic pollutants in addition to heavy metals are the mainculprits when it comes to industrial waste. Significant advancements were achieved in the last twodecades in wastewater purification techniques, and among them, the use of solid adsorbents is probablythe process that attracts the most scientific interests. This technique has the advantage of being simpleand efficient while remaining cost-effective. This review provides an overview on the different synthesismethods of magnetic particles and corresponding polymer nanocomposites, as well as recent advances inthe use of these adsorbents in water decontamination. The deficiencies and challenges pertaining to theapplication of this type of adsorbent materials at large industrial scales are highlighted andrecommendations for future research focus areas are suggested.

Synthesis and Three-dimensional Qualitative Structure Selectivity Relationship of 3,5-Disubstituted-2,4- Thiazolidinedione Derivatives As COX2 Inhibitors

Ali, Ahmed M.,Saber, Gamal E.,Mahfouz, Nadia M.,EI-Gendy, Mahmoud A.,Radwan, Awwad A.,Hamid, Mohamed A.-EI. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10

In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]-2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-I, 10o and 10p. Compounds (9a-I, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.

Synthesis and Three-dimensional Qualitative Structure Selectivity Relationship of 3,5- Disubstituted-2,4-Thiazolidinedione Derivatives As COX2 Inhibitors

Ahmed M. Ali,Gamal E. Saber,Nadia M. Mahfouz,Mahmoud A. El-Gendy,Awwad A. Radwan,Mohamed A.-El. Hamid 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.10

In our effort for synthesis of selective COX2 inhibitors, certain new 2,4-thiazolidinedione derivatives were synthesized. It necessitates preparation of potassium salt of 2,4-thiazolidinedione 2, which condensed with intermediate 4a. The resulting 3-[2-(4-methylphenyl)-2-oxo-1-phenylethyl]- 2,4-thiazolidinedione 8 was condensed with appropriate aldehyde to afford compounds 10a, 10i-l, 10o and 10p. Compounds (9a-l, 10a-n, 10p, 11 and 12) were obtained through the preparation of 5-arylmethylidene-2,4-thiazolidinediones 6a-p and reaction of its potassium salt 7a-p with compounds 4a, 4b, and 5. Some compounds displayed significant analgesic activity as compared to reference standards. The anti-inflammatory activity of the synthesized compounds revealed that intermediate 8 and compounds 9c, 10c and 10d showed good results. Compound 10c produced no significant mucosal injury. HipHop methodology of Catalyst program was used to build up hypothetical model of selective COX2 inhibitors followed by fitting the synthesized compounds to this model. Compounds 10c and 10d were suspected to be promising selective COX2 inhibitors. Also, compounds (6c, 8, 9a,c,d,k, 10a,c,d,k, 11 and 12) were docked into COX1 and COX2 X-ray structures, using DOCK6 program. Docking results suggested that several of these derivatives are active COX inhibitors with a significant preference for COX2.

Hollow Spherical Curcumin Nanomicelles CUR@PLA@PF127: A New Trial on Breast Cancer Cells

Fatma S. El-Banna,Nemany A. N. Hanafy,Magdy E. Mahfouz,Maged El Kemary 한국생물공학회 2023 Biotechnology and Bioprocess Engineering Vol.28 No.5

Curcumin (CUR) nanomicelles were developed by solvent-evaporation method using Poly (lactic acid) (PLA) for the first time with Pluronic F127 (PF127) to produce CUR@PLA@PF127 nanomicelles. The X-ray diffraction (XRD) spectra confirmed the encapsulation of CUR into the produced nanomicelles (CUR@PLA@PF127). Fourier transform infrared spectroscopy (FTIR) analysis showed the interactions of CUR with PLA and PF127. Scanning electron microscope (SEM) and transmission electron microscope (TEM) analysis showed the formation of spherical shape of CUR@PLA@PF127 with a diameter around 130-160 nm. To investigate the anticancer effect of the encapsulated CUR, the activity of CUR@PLA@PF127 nanomicelles, free CUR and blank nanomicelles (PLA@PF127) were assayed against two cell lines in-vitro, human breast adenocarcinoma cells (MCF-7) and human breast skin fibroblast cells. The cytotoxicity assay of CUR@PLA@PF127 nanomicelles, revealed an IC50 value of 159.7 ± 1.36 μg/mL for MCF-7 cells which is much lower than that observed for free CUR. This result suggests that CUR@PLA@PF127 nanomicelles increased CUR potency due to improving its water solubility, resulting in longer release profile, and increasing antiproliferative effect on breast cancer cells (MCF-7). We anticipate that CUR@PLA@PF127 in drug delivery, improving drugs design and that the developed nanomicelles will be regarded one of the most promising nanocarriers for the treatment of breast cancer, and opening the door to future applications in cancer therapies.