No abstract

Abstract:A novel series of dihydropyrimidines (DHPMs) 4a-j; 2-oxopyran-3-carboxylate 7a,b; 1-amino-1,2-dihydropyridine-3-carboxylate 8; and 1,3,4-oxadiazole derivatives 12 with quinolinyl residues have been synthesized in fairly good yields. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. In vitro antimalarial evaluation of the synthesized quinoline derivatives against Plasmodium falciparum revealed them to possess moderate to high antimalarial activities, with IC 50 values ranging from 0.014-5.87 µg/mL. Compounds 4b,g,i and 12 showed excellent antimalarial activity against to Plasmodium falciparum compared with the antimalarial agent chloroquine (CQ).

A novel series of substituted 4,6-dimethyl-2-oxo-1-(thiazol-2-ylamino)-1,2-dihydropyridine-3-carbonitrile derivatives 6, 9, 13, 15, and 17 was synthesized in a good to excellent yield from the reaction of 1-(3-cyano-4,6-dimethyl-2-oxopyridin-1(2H)-yl)thiourea with 2-oxo-N'-arylpropanehydrazonoyl chloride, chloroacetone, α-bromoketones, ethyl chloroacetate, and 2,3-dichloroquinoxaline, respectively. The potential DNA gyrase inhibitory activity was examined using in silico molecular docking simulation. The novel thiazoles exhibit dock score values between − 6.4 and − 9.2 kcal/mol and they were screened for their antimicrobial activities. Compound 13a shown good antibacterial activities with MIC ranged from 93.7–46.9 μg/mL, in addition, it shown good antifungal activities with MIC ranged from 7.8 and 5.8 μg/mL.

No abstract

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.

Due to the growing demand for hydrogen, the photocatalytic hydrogen production from alcohols present an intriguing prospect as a potential source of low-cost renewable energy. The noble metals (Ag, Au, Pd and Pt) deposited LaMnO3 nanocomposites were synthesized by a non-conventional green bio-reduction method using aqueous lemon peel extract, which acts as both reducing and capping agent. The successful deposition of the noble metals on the surface of LaMnO3 was verified by using powder XRD, FTIR, TEM, N2-physisorption, DR UV-vis spectroscopy, and XPS techniques. The photocatalytic activity of the synthesized nanocomposites was tested for photocatalytic H2 production under visible light irradiation. Different photocatalytic reaction parameters such as reaction time, pH, catalyst mass and reaction temperature were investigated to optimize the reaction conditions for synthesized nanocomposites. Among the synthesized noble metal deposited LaMnO3 nanocomposites, the Pt-LaMnO3 nanocomposite offered superior activity for H2 production. The enhanced photocatalytic activity of the Pt-LaMnO3 was found as a result from low bandgap energy, high photoelectrons generation and enhanced charge separation due to deposition of Pt nanoparticles. The effective noble metal deposition delivers a new route for the development of plasmonic noble metal-LaMnO3 nanocomposites for photocatalytic reforming of aqueous methanol to hydrogen.

2-Cyano-N-(3-cyano-4,6-dimethyl-2-oxopyridin-1-yl)acetamide (3) was prepared via two routes and its reactions with various aldehydes and diazonium salts were studied. When compound 3 was treated with arylidenemalononitrile in either ethanol or dioxane using piperidine as a catalyst in a trial to prepare bispyridone derivatives 7, there was no reaction and the reason for this was investigated using molecular modeling. Furthermore, coumarin derivatives 9 and 10 were prepared by reaction of acetamide 3 with salicylaldehyde derivatives. Finally, aminopyrazole derivatives 15 were synthesized by reaction of acetamide 3 with N,N-dimethylformamide dimethyl acetal (DMFDMA) then with hydrazine derivatives and their mechanisms was discussed.

No abstract