Current Issue : October - December Volume : 2020 Issue Number : 4 Articles : 6 Articles
Alzheimerâ??s disease (AD) is a multifactorial neurodegenerative disorder that involves\ndifferent pathogenic mechanisms. In this regard, the goal of this study was the design and synthesis\nof new compounds with multifunctional pharmacological activity by molecular hybridization of\nstructural fragments of curcumin and resveratrol connected by anN-acyl-hydrazone function linked to\na 1,4-disubstituted triazole system. Among these hybrid compounds, derivative 3e showed the ability\nto inhibit acetylcholinesterase activity, the intracellular formation of reactive oxygen species as well\nas the neurotoxicity elicited by AB42 oligomers in neuronal SH-SY5Y cells. In parallel, compound 3e\nshowed a good profile of safety and ADME parameters. Taken together, these results suggest that 3e\ncould be considered a lead compound for the further development of AD therapeutics....
The inverse correlation observed between Alzheimerâ??s disease (AD) and cancer has\nprompted us to look for cholinesterase-inhibiting activity in phenothiazine derivatives that possess\nanticancer properties. With the use of in silico and in vitro screening methods, our study found a\nnew biological activity in anticancer polycyclic, tricyclic, and tetracyclic compounds. The virtual\nscreening of a library of 120 ligands, which are the derivatives of azaphenothiazine, led to\nthe identification of 25 compounds that can act as potential inhibitors of acetylcholinesterase\n(AChE) and butyrylcholinesterase (BuChE). Biological assays revealed the presence of selective\ninhibitors of eeAChE (electric eel AChE) or eqBuChE (equine serum BuChE) and nonselective inhibitors\nof both enzymes among the tested compounds..............................................................................................
Alkyl quinolone has been proven to be a privileged scaffold in the antimicrobial drug\ndiscovery pipeline. In this study, a series of new 4-hydroxy-2-quinolinone analogs containing a long\nalkyl side chain at C-3 and a broad range of substituents on the C-6 and C-7 positions were synthesized.\nThe antibacterial and antifungal activities of these analogs against Staphylococcus aureus, Escherichia coli,\nand Aspergillus flavus were investigated. The structure-activity relationship study revealed that the\nlength of the alkyl chain, as well as the type of substituent, has a dramatic impact on the antimicrobial\nactivities. Particularly, the brominated analogs 3j with a nonyl side chain exhibited exceptional\nantifungal activities against A. flavus (half maximal inhibitory concentration (IC50) = 1.05 microg/mL),\nwhich surpassed that of the amphotericin B used as a positive control. The antibacterial activity\nagainst S. aureus, although not as potent, showed a similar trend to the antifungal activity. The data\nsuggest that the 4-hydroxy-2-quinolone is a promising framework for the further development of\nnew antimicrobial agents, especially for antifungal treatment....
A new series of s-triazine hydrazone derivatives was prepared based on the reaction\nof 6-hydrazino-2,4-disubstituted-s-triazine with p-substituted benzaldehyde derivatives using\na straightforward synthetic pathway. The antiproliferative activity of all synthesized compounds was\nevaluated against two human cancer cell lines; breast cancer MCF-7 and colon carcinoma HCT-116\nusing MTT assay. Among all, 11 compounds have shown strong to moderate antiproliferative activity\nwith IC50 values in the range 1.01â??18.20....................................................................................................
Some substituted benzimidazole derivatives were synthesized by condensation of o-phenylenediamine with aromatic acids in presence of water. A total of six compounds have been synthesized and the chemical structures were identified by spectral analysis. The synthesized compounds were screened for their in-vitro antibacterial activity against standard strains by cup plate method and also for anthelmintic activity and all the compounds showed good activities when compared with the standard except compound 4 of the series of compounds....
Coumarin-based 1,3,4-oxadiazoline ring is well acknowledged to possess significant anticancer and antimicrobial activities. In an attempt to find more effective and selective chemotherapeutic agents against cancer and microbial infections, a series of 7-((4-acetyl-5-(substituted phenyl)-4,5-dihydro-1,3,4-oxadiazolin-2-yl)methoxy)-4-methyl-2H-chromen-2-one [IIa-e] were synthesized by heterocyclization of coumarin Schiff bases Ia-e and characterised by IR, NMR and mass spectral data. The title compounds were evaluated for in-vitro anticancer activity at different concentrations against non-small lung cancer cell line A549 by MTT assay, in-vitro antitubercular activity against M. Tuberculosis H37Rv strain in DMSO by almar blue method and antibacterial activity against Gram positive bacteria S. aureus and Gram negative bacteria E. coli by serial dilution method; 5-flurouracil, streptomycin and ciprofloxacin were used as standard drugs respectively. Among the synthesized compounds, IIe with 1,2-dioxymethlyene group on phenyl ring showed maximum anticancer and antitubercular activity. However, all the compounds exhibited feeble activity when compared to standard drugs used in the study, warranting further study....
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