Synthesis and Antimicrobial Activity of Certain New 1,2,4-Triazolo[1,5-a]Pyrimidine Derivatives

Mostafa, Yaser A.H.,Hussein, Mostafa A.,Radwan, Awwad A.,Krafy, Abd El-Hamid 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.3

Certain new derivatives of 1,2,4-triazolo[1,5-a]pyrimidines were synthesized through the reaction of 1,2,4-triazolo[1,5-a]pyrimidine-7-o1 with ethyl bromoacetate to afford the ethyl acetate ester, which upon hydrazinolysis gives the corresponding hydrazide. The hydrazide is the key intermediate which was used for the synthesis of the target compounds. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable results with those of ampicillin and fluconazole reference drugs.

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 and Antimicrobial Activity of Certain New 1,2,4-Triazolo[1,5-a]Pyrimidine Derivatives

Yaser A.H. Mostafa,Mostafa A. Hussein,Awwad A. Radwan,Abd El-Hamid N. Kfafy 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.3

Certain new derivatives of 1,2,4-triazolo[1,5-a]pyrimidines were synthesized through the reaction of 1,2,4-triazolo[1,5-a]pyrimidine-7-ol with ethyl bromoacetate to afford the ethyl acetate ester, which upon hydrazinolysis gives the corresponding hydrazide. The hydrazide is the key intermediate which was used for the synthesis of the target compounds. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable results with those of ampicillin and fluconazole reference drugs.

Design, Synthesis, and Antimicrobial Activity, of New 1,4-disubstituted Octahydroquinoxaline-2,3-dione Derivatives

Mostafa A. Hussein 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.5

A series of 1,4-disubstituted octahydroquinoxaline-2,3-dione derivatives was prepared through two steps reaction. The latter involves the formation of N,N-disubstituted cyclohexane-1,2-diamine derivatives (la-j)through reductive alkylation of 1,2-cyclohexanediamine with different aldehydes in presence of sodium cyanoborohydride. Fusion of compounds (1a-j) with diethyl oxalate affording the target compounds (2a-j). Elucidation of structures of compounds (2a-j) was based upon different spectral data as well as the elemental methods of analyses. In addition, mass spectrometry and X-ray diffraction analyses were carried out. Moreover, the lipophilicity of the target compounds as expressed from the Clog P. Most of the test compounds (2a-j) showed weak to moderate antibacterial and antifungal activities against most of the used bacterial and fungal strains in comparison to chloramphenicol and clotrimazole as reference drugs respectively.

Enhancing feature selection with GMSMFO: A global optimization algorithm for machine learning with application to intrusion detection

Hussein Nazar K,Qaraad Mohammed,Amjad Souad,Farag M.A.,Hassan Saima,Mirjalili Seyedali,Elhosseini Mostafa A 한국CDE학회 2023 Journal of computational design and engineering Vol.10 No.4

The paper addresses the limitations of the Moth-Flame Optimization (MFO) algorithm, a meta-heuristic used to solve optimization problems. The MFO algorithm, which employs moths' transverse orientation navigation technique, has been used to generate solutions for such problems. However, the performance of MFO is dependent on the flame production and spiral search components, and the search mechanism could still be improved concerning the diversity of flames and the moths' ability to find solutions. The authors propose a revised version called GMSMFO, which uses a Novel Gaussian mutation mechanism and shrink MFO to enhance population diversity and balance exploration and exploitation capabilities. The study evaluates the performance of GMSMFO using the CEC 2017 benchmark and 20 datasets, including a high-dimensional intrusion detection system dataset. The proposed algorithm is compared to other advanced metaheuristics, and its performance is evaluated using statistical tests such as Friedman and Wilcoxon rank-sum. The study shows that GMSMFO is highly competitive and frequently superior to other algorithms. It can identify the ideal feature subset, improving classification accuracy and reducing the number of features used. The main contribution of this research paper includes the improvement of the exploration/exploitation balance and the expansion of the local search. The ranging controller and Gaussian mutation enhance navigation and diversity. The research paper compares GMSMFO with traditional and advanced metaheuristic algorithms on 29 benchmarks and its application to binary feature selection on 20 benchmarks, including intrusion detection systems. The statistical tests (Wilcoxon rank-sum and Friedman) evaluate the performance of GMSMFO compared to other algorithms. The algorithm source code is available at https://github.com/MohammedQaraad/GMSMFO-algorithm.

Design, Synthesis, and Antimicrobial Activity, of New 1,4-disubstituted Octahydroquinoxaline-2,3-dione Derivatives

Hussein, Mostafa A. Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.5

A series of 1,4-disubstituted octahydroquinoxaline-2,3-dione derivatives was prepared through two steps reaction. The latter involves the formation of N,N-disubstituted cyclohexane-1,2-diamine derivatives (la-j) through reductive alkylation of 1,2-cyclohexanediamine with different aldehydes in presence of sodium cyanoborohydride. Fusion of compounds (1a-j) with diethyl oxalate affording the target compounds (2a-j). Elucidation of structures of compounds (2a-j) was based upon different spectral data as well as the elemental methods of analyses. In addition, mass spectrometry and X-ray diffraction analyses were carried out. Moreover, the lipophilicity of the target compounds as expressed from the Clog P. Most of the test compounds (2a-j) showed weak to moderate antibacterial and antifungal activities against most of the used bacterial and fungal strains in comparison to chloramphenicol and clotrimazole as reference drugs respectively.

Evaluation of required seismic gap between adjacent buildings in relation to the Egyptian Code

Manar M. Hussein,Ahmed A. Mostafa,Walid A. Attia 국제구조공학회 2021 Structural Engineering and Mechanics, An Int'l Jou Vol.78 No.2

International seismic codes stipulate that adjacent buildings should be separated by a specified minimum distance, otherwise the pounding effect should be considered in the design. Recent researches proposed an alternative method (Double Difference Combination Rule) to estimate seismic gap between structures, as this method considers the cross relation of adjacent buildings behavior during earthquakes. Four different criteria were used to calculate the minimum separation distance using this method and results are compared to the international codes for five separation cases. These cases used four case study buildings classified by different heights, lateral load resisting systems and fundamental periods of vibrations to assess the consistency in results for the alternative methods. Non-linear analysis was performed to calculate the inelastic displacements of the four buildings, and the results were used to evaluate the relation between elastic and inelastic displacements due to the ductility of structural elements resisting seismic loads. A verification analysis was conducted to guarantee that the separation distance calculated is sufficient to avoid pounding. Results shows that the use of two out of the four studied methods yields separation distances smaller than that calculated by the code specified equations without under-estimating the minimum separation distance required to avoid pounding.

Addressing constrained engineering problems and feature selection with a time-based leadership salp-based algorithm with competitive learning

Qaraad Mohammed,Amjad Souad,Hussein Nazar K,Elhosseini Mostafa A 한국CDE학회 2022 Journal of computational design and engineering Vol.9 No.6

Like most metaheuristic algorithms, salp swarm algorithm (SSA) suffers from slow convergence and stagnation in the local optima. The study develops a novel Time-Based Leadership Salp-Based Competitive Learning (TBLSBCL) to address the SSA’s flaws. The TBLSBCL presents a novel search technique to address population diversity, an imbalance between exploitation and exploration, and the SSA algorithm’s premature convergence. Hybridization consists of two stages: First, a time-varying dynamic structure represents the SSA hierarchy of leaders and followers. This approach increases the number of leaders while decreasing the number of salp’s followers linearly. Utilizing the effective exploitation of the SSA, the position of the population’s leader is updated. Second, the competitive learning strategy is used to update the status of the followers by teaching them from the leaders. The goal of adjusting the salp swarm optimizer algorithm is to help the basic approach avoid premature convergence and quickly steer the search to the most promising likely search space. The proposed TBLSBCL method is tested using the CEC 2017 benchmark, feature selection problems for 19 datasets (including three high-dimensional datasets). The TBLSBCL was then evaluated using a benchmark set of seven well-known constrained design challenges in diverse engineering fields defined in the benchmark set of real-world problems presented at the CEC 2020 conference (CEC 2020). In each experiment, TBLSBCL is compared with seven other state-of-the-art metaheuristics and other advanced algorithms that include seven variants of the salp swarm. Friedman and Wilcoxon rank-sum statistical tests are also used to examine the results. According to the experimental data and statistical tests, the TBLSBCL algorithm is very competitive and often superior to the algorithms employed in the studies. The implementation code of the proposed algorithm is available at: https://github.com/MohammedQaraad/TBLSBCL-Optimizer.

Design, synthesis and molecular docking of some new 1,2,4-triazolobenzimidazol-3-yl acetohydrazide derivatives with anti-inflammatory-analgesic activities

Anber F. Mohammed,Samia G. Abdel-Moty,Mostafa A. Hussein,Abdel Alim M. Abdel Alim 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.12

The present work describes the synthesis andevaluation of some new acetohydrazones, 1,3,4-oxadiazolesand 1,2,4-triazoles of 1,2,4-triazolo[1,5-a]benzimidazole asanti-inflamm atory-analgesic agents. Structure elucidation ofthese compounds was confirmed by IR, 1H NMR, and massspectrometry along with elemental microanalyses. Mostcompounds exhibited significant anti-inflammatory activityin comparison to indomethacin. Further, some compoundswere tested for their analgesic effects where two compoundsshowed results comparable to indomethacin at 4 h interval. The most active anti-inflammatory and analgesic compounds(4c and 11a) were examined on gastric mucosa and didn’tshow any gastric ulcerogenic effect compared with the referenceindomethacin. Moreover, LD50 of compounds (4c and11a) were determined in mice; they were found non toxic upto 240 and 300 mg/kg (i.p.). Also, docking simulation ofsome compounds into COX active sites was studied.