In this study, new derivatives of pyrazole, isoxazole, pyrazolylthiazole, and azolopyrimidine having a thiophene ring were synthesized under microwave irradiation. Their pharmacological activity toward bacteria and fungi inhibition was screened and compared to the references Chloramphenicol and Trimethoprim/sulphamethoxazole. The antimicrobial results of the investigated compounds revealed promising results and some derivatives have activities similar to the references used.
Multicloud computing is a strategy that helps customers to reduce reliance on any single cloud provider (known as the vendor lock-in problem). The value of such strategy increases with proper selection of qualified service providers. In this paper, a constrained multicriteria multicloud provider selection mathematical model is proposed. Three metaheuristics algorithms (simulated annealing[SA], genetic algorithm [GA], and particle swarm optimization algorithm [PSO]) were implemented to solve the model, and their performance was studied and compared using a hypothetical case study. For the sake of comparison, Taguchi's robust design method was used to select the algorithms' parameters values, an initial feasible solution was generated using analytic hierarchy process (AHP)-as the most used method to solve the cloud provider selection problem in the literature, all three algorithms used that solution and, in order to avoid AHP limitations, another initial solution was generated randomly and used by the three algorithm in a second set of performance experiments. Results showed that SA, GA, PSO improved the AHP solution by 53.75%, 60.41%, and 60.02%, respectively, SA and PSO are robust because of reaching the same best solution in spite of the initial solution.
K E Y W O R D Scloud service provider, genetic algorithm, multicloud, particle swarm optimization, simulated annealing, Taguchi method 1 Softw: Pract Exper. 2020;50:925-947.wileyonlinelibrary.com/journal/spe
1,3‐Di(thiophen‐2‐yl)prop‐2‐en‐1‐one (1) was utilized in the synthesis of 4,6‐di(thiophen‐2‐yl)‐3,4‐dihydropyrimidine‐2(1H)‐thione (2) and 5,7‐di(thiophen‐2‐yl)‐2‐thioxo‐2,3‐dihydropyrido[2,3‐d]pyrimidin‐4(1H)‐one (4). The latter thiones were used in the synthesis of two new series of [1,2,4]triazolo[4,3‐a]pyrimidines 10a–i and pyrido[2,3‐d][1,2,4]triazolo[4,3‐a]pyrimidinones 5a–i via reaction with the appropriate hydrazonoyl halides using triethylamine as a basic catalyst in dioxane. The mechanism of formation of the synthesized compounds was discussed, and the assigned structure was established via microanalysis, spectral data (infrared, 1H NMR, and Mass), and density functional calculations. Moreover, the newly synthesized products were evaluated for their antimicrobial activities, and the results show that some derivatives have been well with mild activities. Finally, quantum chemistry calculations confirmed the mechanism and structure of the products.
BackgroundPyridopyrimidines are of current interest because of their extensive variety of biological and pharmacological activities.ResultsA series of pyrido[2′,3′:4,5]pyrimido[2,1-b][1,3,5]thiadiazinones was obtained by aminomethylation of pyridopyrimidinethione with formaldehyde solution (37%) and different primary aromatic amines. Another series of pyrido[2′,3:4,5]pyrimido[2,1-b][1,3]thiazinones was prepared by Michael addition reaction of pyridopyrimidinethione to the activated double bond of a number of arylidene malononitrile and 2-(benzo[d][1,3]dioxol-5-ylmethylene)malononitrile. The mechanisms of formation of the synthesized compounds were discussed and the assigned structure was established via microanalysis and spectral data (IR, 1H NMR, and Ms.). A comparative study of the biological activity of the synthesized compounds with chloramphenicol and trimethoprim/sulphamethoxazole is shown in Table 1. Generally, all synthesized compounds showed adequate inhibitory effects on the growth of Gram-positive and Gram-negative bacteria.
ConclusionsIn this study, we use a simple (synthetic) strategy for the synthesis of pyrimidothiadiazines, based on their aminomethylation through the Mannich reaction; they have also been synthesized by the application of the Michael addition to activated nitriles. Mechanisms and structures of the newly synthesized compounds were examined: the antimicrobial activity of some selected compounds was evaluated, which demonstrated adequate inhibitory effects. Graphical abstractThe strategic structures of the products (7a–g).
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