Synthesis and In Vitro Evaluation of Some Novel Benzofuran Derivatives as Potential Anti-HIV-1, Anticancer, and Antimicrobial Agents

Rida, Samia M.,EI-Hawash, Soad A.M.,Fahmy, Hesham T.Y.,Hazza, Aly A.,EI-Meligy, Mostafa M.M. The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.1

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

Cultivation of a New Microalga, Micractinium reisseri, in Municipal Wastewater for Nutrient Removal, Biomass, Lipid, and Fatty Acid Production

Abou-Shanab, Reda A.I.,El-Dalatony, Marwa M.,EL-Sheekh, Mostafa M.,Ji, Min-Kyu,Salama, El-Sayed,Kabra, Akhil N.,Jeon, Byong-Hun 한국생물공학회 2014 Biotechnology and Bioprocess Engineering Vol.19 No.3

Coupling of advanced wastewater treatment with microalgae cultivation for low-cost lipid production was demonstrated in this study. The microalgal species Micractinium reisseri and Scenedesmus obliquus were isolated from municipal wastewater mixed with agricultural drainage. M. reisseri was selected based on the growth rate and cultivated in municipal wastewater (influent, secondary and tertiary effluents) which varied in nutrient concentration. M. reisseri showed an optimal specific growth rate (${\mu}_opt$) of 1.15, 1.04, and 1.01 1/day for the influent and the secondary and tertiary effluents, respectively. Secondary effluent supported the highest phosphorus removal (94%) and saturated fatty acid content (40%). The highest lipid content (40%), unsaturated fatty acid content, including monounsaturated and polyunsaturated fatty acids (66%), and nitrogen removal (80%) were observed for tertiary effluent. Fatty acids accumulating in the microalgal biomass (M. reisseri) were mainly composed of palmitic acid, oleic acid, linoleic acid, and ${\alpha}$-linolenic acid. Cultivation of M. reisseri using municipal wastewater served a dual function of nutrient removal and biofuel feedstock generation.

Synthesis and In Vitro Evaluation of Some Novel Benzofuran Derivatives as Potential Anti-HIV-1, Anticancer, and Antimicrobial Agents

Samia M. Rida,Soad A. M. El-Hawash,Hesham T. Y. Fahmy,Aly A. Hazza,Mostafa M. M. El-Meligy 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.1

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles (3a-c, 4a-f) and thiazolidin- 4-ones (5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran- 2-yl-ethylidene) hydrazide (7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones (8a-c); 2-thioxo-2,3-dihydro-thiazoles (9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations >2.0×10-4 M and 2.5×10-5 M respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

Synthesis of Novel Benzofuran and Related Benzimidazole Derivatives for Evaluation of In Vitro Anti-HIV-1, Anticancer and Antimicrobial Activities

Samia M. Rida,Soad A. M. El-Hawash,Hesham T. Y. Fahmy,Aly A. Hazzaa,Mostafa M. M. El-Meligy 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.10

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

A Four Leg Shunt Active Power Filter Predictive Fuzzy Logic Controller for Low-Voltage Unbalanced-Load Distribution Networks

A. M. Fahmy,Ahmed K. Abdelslam,Ahmed A. Lotfy,Mostafa Hamad,Abdelsamee Kotb 전력전자학회 2018 JOURNAL OF POWER ELECTRONICS Vol.18 No.2

Recently evolved power electronics’ based domestic/residential appliances have begun to behave as single phase non-linear loads. Performing as voltage/current harmonic sources, those loads when connected to a three phase distribution network contaminate the line current with harmonics in addition to creating a neutral wire current increase. In this paper, an enhanced performance three phase four leg shunt active power filter (SAPF) controller is presented as a solution for this problem. The presented control strategy incorporates a hybrid predictive fuzzy-logic based technique. The predictive part is responsible for the SAPF compensating current generation while the DC-link voltage control is performed by a fuzzy logic technique. Simulations at various loading conditions are carried out to validate the effectiveness of the proposed technique. In addition, an experimental test rig is implemented for practical validation of the of the enhanced performance of the proposed technique.

A Four Leg Shunt Active Power Filter Predictive Fuzzy Logic Controller for Low-Voltage Unbalanced-Load Distribution Networks

Fahmy, A.M.,Abdelslam, Ahmed K.,Lotfy, Ahmed A.,Hamad, Mostafa,Kotb, Abdelsamee The Korean Institute of Power Electronics 2018 JOURNAL OF POWER ELECTRONICS Vol.18 No.2

Recently evolved power electronics' based domestic/residential appliances have begun to behave as single phase non-linear loads. Performing as voltage/current harmonic sources, those loads when connected to a three phase distribution network contaminate the line current with harmonics in addition to creating a neutral wire current increase. In this paper, an enhanced performance three phase four leg shunt active power filter (SAPF) controller is presented as a solution for this problem. The presented control strategy incorporates a hybrid predictive fuzzy-logic based technique. The predictive part is responsible for the SAPF compensating current generation while the DC-link voltage control is performed by a fuzzy logic technique. Simulations at various loading conditions are carried out to validate the effectiveness of the proposed technique. In addition, an experimental test rig is implemented for practical validation of the of the enhanced performance of the proposed technique.

Synthesis, Anti-inflammatory, Analgesic, and Antibacterial Activities of Some Triazole, Triazolothiadiazole, and Triazolothiadiazine Derivatives

Mostafa A. Hussein,Refaat M. Shaker,Mohammed A. Ameen,Mohammed F. Mohammed 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.8

This study is concerned with the synthesis of new 1,2,4-triazoles, 1,3,4-thiadiazoles, and 1,3,4-thiadiazines derivatives. Derivatives 3a-i were obtained by condensation of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole 1 with the appropriate aldehyde. Compounds 4a-i were synthesized in a one pot reaction involving compounds 3a-i, formaldehyde, and morpholine. Condensation of compound 1 with the appropriate acids or 4-substituted phenacyl bromide gave compounds 6a-d and 8a-f respectively. The chemical structures of the newly synthesized derivatives were elucidated using different spectral and elemental methods of analysis. All compounds were evaluated for their anti-inflammatory activity and the most potent derivatives were tested for their analgesic activity using indomethacin as a reference drug. In addition, ulcerogenicity and LD_50 for the most active compounds were evaluated. Moreover, the antibacterial activities of the newly synthesized derivatives were investigated.

Synthesis of Novel Benzofuran and Related Benzimidazole Derivatives for Evaluation of In Vitro Anti-HIV-1, Anticancer and Antimicrobial Activities

Rida, Samia M.,El-Hawash, Soad A.M.,Fahmy, Hesham T.Y.,Hazzaa, Aly A.,El-Meligy, Mostafa M.M. The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.10

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

Synthesis, structural, TD-DFT, and optical characteristics of indole derivatives

Almutlaq N.,Elshanawany Mahmoud M.,Sayed Mostafa,Younis Osama,Ahmed Mostafa,Wachtveitl Josef,Braun Markus,Tolba Mahmoud S.,Al-Hossainy Ahmed F.,Abozeed Amina A. 한국물리학회 2023 Current Applied Physics Vol.45 No.-

New compounds of (E)-1-(3-chloro-1H-indol-2-yl)-N-(4-methoxyphenyl)methanimine [Indol-M] and (E)-1-(4- (((3-chloro-1H-indol-2-yl)methylene)amino)phenyl)ethan-1-one [Indol-A] were synthesized and subsequently converted to thin films via physical vapor deposition technique. Numerous characterization techniques were used including FTIR, nuclear magnetic resonance, X-ray diffraction, scanning electron microscope, and optical spectroscopy. Additionally, the optimization using TD-DFTD/Mol3 and Cambridge Serial Total Energy Bundle (TD-FDT/CASTEP) was performed. The XRD and FTIR spectra recorded experimentally were confirmed by TD-DFT calculations, proving their molecular structure. As determined by XRD, the crystallite size of [Indol-M]TF and [Indol-A]TF is 72.26 and 62.05 nm, respectively. SEM image depicts a one-dimensional morphological structure made up of tightly packed nanorods. The direct optical energy bandgaps computed using Tauc’s equation for the [Indol-M]TF and [Indol-A]TF are 4.49 eV and 3.31 eV, respectively. As predicted by CASTEP TD-DFT, the optical properties agree well with the experimental values. [Indol-M]TF and [Indol-A]TF present good candidates for optoelectronics and solar cell applications.

Novel nomogram-based integrated gonadotropin therapy individualization in in vitro fertilization/intracytoplasmic sperm injection: A modeling approach

Abdel Hameed I M Ebid,Sara M Abdel Motaleb,Mahmoud I Mostafa,Mahmoud M A Soliman 대한생식의학회 2021 Clinical and Experimental Reproductive Medicine Vol.48 No.2

Objective: This study aimed to characterize a validated model for predicting oocyte retrieval in controlled ovarian stimulation (COS) and to construct model-based nomograms for assistance in clinical decision-making regarding the gonadotropin protocol and dose.Methods: This observational, retrospective, cohort study included 636 women with primary unexplained infertility and a normal menstrual cycle who were attempting assisted reproductive therapy for the first time. The enrolled women were split into an index group (n=497) for model building and a validation group (n=139). The primary outcome was absolute oocyte count. The dose-response relationship was tested using modified Poisson, negative binomial, hybrid Poisson-Emax, and linear models. The validation group was similarly analyzed, and its results were compared to that of the index group. Results: The Poisson model with the log-link function demonstrated superior predictive performance and precision (Akaike information criterion, 2,704; λ=8.27; relative standard error (λ)=2.02%). The covariate analysis included women’s age (p<0.001), antral follicle count (p<0.001), basal follicle-stimulating hormone level (p<0.001), gonadotropin dose (p=0.042), and protocol type (p=0.002 and p<0.001 for short and antagonist protocols, respectively). The estimates from 500 bootstrap samples were close to those of the original model. The validation group (n=139) showed model assessment metrics comparable to the index model. Based on the fitted model, a static nomogram was built to improve visualization. In addition, a dynamic electronic tool was created for convenience of use.Conclusion: Based on our validated model, nomograms were constructed to help clinicians individualize the stimulation protocol and gonadotropin doses in COS cycles.