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.

Towards automatic EEG cyclic alternating pattern analysis: a systematic review analysis: a systematic review

Fábio Mendonça,Sheikh Shanawaz Mostafa,Fernando Morgado-Dias,Antonio G. Ravelo-García,Ivana Rosenzweig 대한의용생체공학회 2023 Biomedical Engineering Letters (BMEL) Vol.13 No.3

This study conducted a systematic review to determine the feasibility of automatic Cyclic Alternating Pattern (CAP)analysis. Specifically, this review followed the 2020 Preferred Reporting Items for Systematic reviews and Meta-Analyses(PRISMA) guidelines to address the formulated research question: is automatic CAP analysis viable for clinical application?From the identified 1,280 articles, the review included 35 studies that proposed various methods for examining CAP,including the classification of A phase, their subtypes, or the CAP cycles. Three main trends were observed over timeregarding A phase classification, starting with mathematical models or features classified with a tuned threshold, followedby using conventional machine learning models and, recently, deep learning models. Regarding the CAP cycle detection,it was observed that most studies employed a finite state machine to implement the CAP scoring rules, which depended onan initial A phase classifier, stressing the importance of developing suitable A phase detection models. The assessment ofA-phase subtypes has proven challenging due to various approaches used in the state-of-the-art for their detection, rangingfrom multiclass models to creating a model for each subtype. The review provided a positive answer to the main researchquestion, concluding that automatic CAP analysis can be reliably performed. The main recommended research agendainvolves validating the proposed methodologies on larger datasets, including more subjects with sleep-related disorders,and providing the source code for independent confirmation.

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.

Effect of variable viscosity on combined forced and free convection boundary-layer flow over a horizontal plate with blowing or suction

Mostafa A.A. Mahmoud 한국산업응용수학회 2007 Journal of the Korean Society for Industrial and A Vol.11 No.1

The effects of variable viscosity, blowing or suction on mixed convection flow of a viscous incompressible fluid a semi-infinite horizontal flat plate aligned parallel to a uniform stream in the presence of the wall temperature distribution inversely proportional to the square root of the distance from the leading edge have been investigated. The equations governing the flow are transformed into a system of coupled non-linear ordinary differential equations by using similarity variables. The similarity equations have been solved numerically. The effect of the viscosity temperature parameter, the buoyancy parameter and the blowing or suction parameter on the velocity and temperature profiles as well as on the skin-friction coefficient and the Nusselt number are discussed.

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.

Heat Generation/Absorption and Viscous Dissipation Effects on MHD Flow of a Micropolar Fluid Over a Moving Permeable surface Embedded in a Non-Darxian Porous Medium

Mostafa A. A. Mahmoud 한국물리학회 2009 THE JOURNAL OF THE KOREAN PHYSICAL SOCIETY Vol.54 No.4

The flow and heat transfer of an electrically conducting micropolar fluid on a continuously moving porous plate embedded in a non-Darcian porous medium in the presence of a transverse magnetic field and heat generation or absorption has been considered. Ohmic heating and a new model for viscous dissipation are taken into account. The transformed coupled non-linear ordinary differential equations are solved numerically by employing a fourth-order Rung-Kutta integration scheme coupled with the shooting technique. The effects of various physical parameters on the velocity, micro-rotation velocity and temperature are shown graphically. Moreover, the numerical values of the local skin-friction, the local wall couple stress and the local Nusselt number are displayed in a tabular form and are discussed.

A new approach for solving global optimization and engineering problems based on modified sea horse optimizer

Hashim Fatma A,Mostafa Reham R,Khurma Ruba Abu,Qaddoura Raneem,Castillo Pedro A 한국CDE학회 2024 Journal of computational design and engineering Vol.11 No.1

Sea horse optimizer (SHO) is a noteworthy metaheuristic algorithm that emulates various intelligent behaviors exhibited by sea horses, encompassing feeding patterns, male reproductive strategies, and intricate movement patterns. To mimic the nuanced locomotion of sea horses, SHO integrates the logarithmic helical equation and Levy flight, effectively incorporating both random movements with substantial step sizes and refined local exploitation. Additionally, the utilization of Brownian motion facilitates a more comprehensive exploration of the search space. This study introduces a robust and high-performance variant of the SHO algorithm named modified sea horse optimizer (mSHO). The enhancement primarily focuses on bolstering SHO’s exploitation capabilities by replacing its original method with an innovative local search strategy encompassing three distinct steps: a neighborhood-based local search, a global non-neighbor-based search, and a method involving circumnavigation of the existing search region. These techniques improve mSHO algorithm’s search capabilities, allowing it to navigate the search space and converge toward optimal solutions efficiently. To evaluate the efficacy of the mSHO algorithm, comprehensive assessments are conducted across both the CEC2020 benchmark functions and nine distinct engineering problems. A meticulous comparison is drawn against nine metaheuristic algorithms to validate the achieved outcomes. Statistical tests, including Wilcoxon’s rank-sum and Friedman’s tests, are aptly applied to discern noteworthy differences among the compared algorithms. Empirical findings consistently underscore the exceptional performance of mSHO across diverse benchmark functions, reinforcing its prowess in solving complex optimization problems. Furthermore, the robustness of mSHO endures even as the dimensions of optimization challenges expand, signifying its unwavering efficacy in navigating complex search spaces. The comprehensive results distinctly establish the supremacy and efficiency of the mSHO method as an exemplary tool for tackling an array of optimization quandaries. The results show that the proposed mSHO algorithm has a total rank of 1 for CEC2020 test functions. In contrast, the mSHO achieved the best value for the engineering problems, recording a value of 0.012 665, 2993.634, 0.01 266, 1.724 967, 263.8915, 0.032 255, 58 507.14, 1.339 956, and 0.23 524 for the pressure vessel design, speed reducer design, tension/compression spring, welded beam design, three-bar truss engineering design, industrial refrigeration system, multi-product batch plant, cantilever beam problem, and multiple disc clutch brake problems, respectively. Source codes of mSHO are publicly available at https://www.mathworks.com/matlabcentral/fileexchange/135882-improved-sea-horse-algorithm.

Closed-Loop Transmit Diversity Techniques for Small Wireless Terminals and Their Performance Assessment in a Flat Fading Channel

Raqibul Mostafa,Ramesh C. Pallat,Uwe Ringel,Ashok A. Tikku,Jeffrey H. Reed 한국전자통신연구원 2012 ETRI Journal Vol.34 No.3

Closed-loop transmit diversity is considered an important technique for improving the link budget in the third generation and future wireless communication standards. This paper proposes several transmit diversity algorithms suitable for small wireless terminals and presents performance assessment in terms of average signal-to-noise ratio (SNR) and outage improvement,convergence, and complexity of operations. The algorithms presented herein are verified using data from measured indoor channels with variable antenna spacing and the results explained using measured radiation patterns for a two-element array. It is shown that for a two-element array, the best among the proposed techniques provides SNR improvement of about 3 dB in a tightly spaced array (inter-element spacing of 0.1wavelength at 2 GHz) typical of small wireless devices. Additionally, these techniques are shown to perform significantly better than a single antenna device in an indoor channel considering realistic values of latency and propagation errors. Closed-loop transmit diversity is considered an important technique for improving the link budget in the third generation and future wireless communication standards. This paper proposes several transmit diversity algorithms suitable for small wireless terminals and presents performance assessment in terms of average signal-to-noise ratio (SNR) and outage improvement,convergence, and complexity of operations. The algorithms presented herein are verified using data from measured indoor channels with variable antenna spacing and the results explained using measured radiation patterns for a two-element array. It is shown that for a two-element array, the best among the proposed techniques provides SNR improvement of about 3 dB in a tightly spaced array (inter-element spacing of 0.1wavelength at 2 GHz) typical of small wireless devices. Additionally, these techniques are shown to perform significantly better than a single antenna device in an indoor channel considering realistic values of latency and propagation errors.

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.

Reliability and Safety of Cross-Leg Free Latissmus Dorsi Muscle Flap in Reconstruction of Mutilating Leg Injuries Using End-to-Side Anastomosis

Abdelmegeed Ahmed Gaber,Hifny Mahmoud A.,Abulezz Tarek A.,Saied Samia,Ellabban Mohamed A.,Abo-Saeda Mohamed Abdel-Al,Allam Karam A.,Haredy Mostafa Mamdoh,Mazeed Ahmed S. 대한성형외과학회 2023 Archives of Plastic Surgery Vol.50 No.5

Background Free tissue transfer is considered the gold standard option for the reconstruction of distal leg defects. Free tissue transfer using recipient vessels in the contralateral leg (cross-leg bridge) is a potential option to supply the flap if there are no suitable recipient vessels in the injured leg. Most studies have described this technique using end-to-end anastomosis which sacrifices the main vessel in the uninjured leg. This study evaluated the use of a cross-leg free latissimus dorsi muscle flap for the reconstruction of defects in single-vessel legs, using end-to-side anastomosis to recipient vessels in the contralateral leg without sacrificing any vessel in the uninjured leg.Methods This is a retrospective study that included 22 consecutive patients with soft tissue defects over the lower leg. All the reconstructed legs had a single artery as documented by CT angiography. All patients underwent cross-leg free latissimus dorsi muscle flap using end-to-side anastomosis to the posterior tibial vessels of the contralateral leg.Results The age at surgery ranged from 12 to 31 years and the mean defect size was 86 cm2. Complete flap survival occurred in 20 cases (91%). One patient had total flap ischemia. Another patient had distal flap ischemia.Conclusion Cross-leg free latissimus dorsi muscle flap is a reliable and safe technique for the reconstruction and salvage of mutilating leg injuries, especially in cases of leg injuries with a single artery. As far as preservation of the donor limb circulation is concerned, end-to-side anastomosis is a reasonable option as it maintains the continuity of the donor leg vessels.