A new cyclopentanol as a side product in the reduction of the chalcone

As a part of an ongoing study on the synthesis of 1,3-diphenylpropanones, as key intermediates in the total synthesis of 11,12-dihydro-10,5-(iminomethano) -5H,10H-dibenzo[a,d]cyclooctenes with potential Central Nervous System activity, 3-(3,4-dimethoxyphenyl)-1-(3-tolyl)-2-propenone is obtained by the Claisen-Schmidt reaction of 3,4-dimethoxybenzaldehyde and 3-methylacetophenone. At the second step, the reduction of the olefinic bond of chalcone was attempted by using Zn/acetic acid. Although the desired saturated ketone was obtained during this reduction, the major product was a new cyclopentanol, formed by cyclodimerization. The structure and the stereochemistry of this new compound was elucidated by ID and 2D NMR analyses

Synthesis and antimicrobial activities of some pyridinium salts

Some pyridinium oxime ether derivatives comprising naphtyl, phytalimido, 2,6-dichlorophenyl and cyclohexyl rings linked to the ether function by a methylen bridge were synthesized and screened for possible antibacterial and antifungal activities using the microdilution method. Propyl and 3-phenylpropyl chains were chosen as side chains attached to the pyridinium nitrogen. Among these derivatives, NF-MFE containing naphtyl ring and 3-phenylpropyl chain exhibited highest antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Enterococcus faecalis, Staphylococcus aureus and Candida albicans in 312.5, 39.1, 9.8, 9.8 and 19.5 µg/ml concentrations respectively. The antimicrobial test results indicated that all the compounds have mild antibacterial activity against both Gram negative and Gram positive bacterial species. It can be hypothesized that bioactivity may be affected by electron density of pyridinium nitrogen atom and size of planar ring structure

Synthesis, biological evaluation and molecular docking study of hydrazone-containing pyridinium salts as cholinesterase inhibitors

PubMed ID: 27581632A series of pyridinium salts bearing alkylphenyl groups at 1 position and hydrazone structure at 4 position of the pyridinium ring were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. The cholinesterase (ChE) inhibitory activity studies were carried out by using the Ellman's colorimetric method. All compounds displayed considerable AChE and BuChE inhibitory activity and some of the compounds manifested remarkable anti-AChE activity compared to the reference compound, galantamine. Among the title compounds, the series including benzofuran aromatic ring exhibited the best inhibitory activity both on AChE and BuChE enzymes. Compound 3b, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-(3-phenylpropyl)pyridinium bromide, was the most active compound with IC50 value of 0.23 (0.24) µM against enantiomeric excess (ee)AChE (human (h)AChE) while compound 3a, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-phenethylpyridinium bromide, was the most active compound with IC50 value of 0.95 µM against BuChE. Moreover, 3a and b exhibited higher activity than the reference compound galantamine (eeAChE (hAChE) IC50 0.43 (0.52) µM; BuChE IC50 14.92 µM). Molecular docking studies were carried out on 3b having highest inhibitory activity against AChE. © 2016 The Pharmaceutical Society of Japan.Faculty of Pharmacy, Cairo University Ege Üniversitesi: 13/Ecz/026This study was supported by Research Grants from Ege University (Project Number: 13/Ecz/026). The authors would like to thank the Pharmaceutical Sciences Research Centre (FABAL) at Ege University Faculty of Pharmacy for spectral analyses of the compounds. -

Elimination of Multi-drug Resistant Acinetobacter baumannii Strain with Various Porphyrin Derivatives Stimulated by Red Light [Çeşitli Porfirin Türevlerinin Kirmizi Işik ile Uyarilarak Çoklu İlaç Dirençli Acinetobacter baumannii Suşunun Yok Edilmesi]

2018 Medical Technologies National Congress, TIPTEKNO 2018 -- 8 November 2018 through 10 November 2018 -- 144203In the study, it was aimed to investigate the photoinactivation effect of antimicrobial photodynamic therapy (aPDT) performed on in-vitro conditions with cationic-porphyrin derivatives (CPDs) on multidrug resistant (MDR) A. baumannii. In aPDT experiments using different photosensitizer concentrations and different energy densities, the reduction in bacterial survival reached to > 6 log10 values. aPDT carried out with CPDs at concentrations below the minimum inhibitory concentration (MIC) values has the potential to display a strong antimicrobial activity against the MDR A. baumannii clinical isolate. © 2018 IEEE

4-[(2E)-2-(4-Chlorobenzylidene)hydrazinylidene]-1-methyl-1, 4-dihydro-pyridine monohydrate

In the title compound, C13H12ClN3· H2O, the organic mol-ecule is almost planar, with a dihedral angle of 3.22 (10)° between the benzene and pyridine rings. The crystal structure is stabilized by O - H?N and C - H?O hydrogen bonding and ?-? stacking inter-actions [centroid-centroid distances = 3.630 (1) and 3.701 (1) Å]