Dilek Demir Erol

New analgesic and antiinflammatory agents 4(1H)-pyridinone derivatives.

A series of 1,2,5-trisubstituted 4(1H)-pyridinone derivatives (7-14) were synthesised by using 4-pyrone derivatives with primary amines in ethanol. The structures of the synthesised compounds were confirmed by analytical and spectral data (UV, IR and 1H-NMR and microanalysis). Analgesic and antiinflammatory activities of the synthesised compounds were investigated by acetic acid-induced writhing syndrome and carrageenan rat paw edema tests. All of the test compounds exhibited higher analgesic activities than acetyl salicylic acid and showed higher antiinflammatory activities than indomethacin. The anti-inflammatory activity and gastric ulceration potential of the compounds were tested using indomethacin as reference drug.

Synthesis of 4(1H)-pyridinone derivatives and investigation of analgesic and antiinflammatory activities

This paper describes recent results of a research program aimed at the synthesis and pharmacological evaluation of new 4(1H)-pyridinone derivatives belonging to the 1,3-disubstituted series (4-11). These compounds were structurally planned by applying the molecular hybridization strategy on previously described 1,2-disubstituted-4(1H)-pyridinone derivatives, considered as lead compounds, which present potent analgesic properties (M.D. Aytemir, T. Uzbay, D.D. Erol, Arzneim. Forsch. (Drug Res.) 49 (1999) 250). Their chemical structures have been proved by means of their IR and 1H NMR data and by elemental analysis. The analgesic profile of the title compounds (4-11), evaluated by the model of abdominal constrictions induced by acetic acid, showed that all the 4(1H)-pyridinone derivatives were active, exhibiting an analgesic activity comparable with that of aspirin (acetyl salicylic acid) used as a standard. The antiinflammatory profile of the synthesized compounds, evaluated by the model of carrageenan rat paw edema, showed that all compounds were active and were comparable with indomethacin used as a standard.

Synthesis and antimicrobial investigation of thiazolinoalkyl-4(1H)-pyridones

Abstract A number of thiazolinoalkyl-4(1 H )-pyridones have been synthesized using 4-pyrone derivatives with cysteamine HCl, and their antibacterial and antifungal activities have been tested. Their chemical structures have been proved by means of their IR, 1 H-NMR, mass spectroscopic data and by elemental analysis. Investigation of antimicrobial activity of compounds was done by tube dilution and disk tecniques using bacteria ( Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Streptococcus faecalis RSKK 10541) and yeast-like fungi ( Candida parapsilosis, C albicans, C pseudotropicalis, C stellatoidea ). A significant inhibitory effect was recorded for many compounds against C albicans ( 7a, c, d ; minimal inhibitory concentration (MIC) = 12.5-25 μg/ml), S aureus ATCC 25923 ( 4c, 7a ; MIC = 25 μg/ml), P aeruginosa ATCC 27923 ( 7a ; MIC = 25 μg/ml), S faecalis RSKK 10541 ( 4c ; MIC = 25 μg/ml), C pseudotropicalis ( 4d, 6d, 7c ; MIC = 25 μg/ml) and C stellatoidea ( 4d ; MIC = 25 μg/ml).

Synthesis and antibacterial and antifungal properties of thiazolinoethyl-2(3H)-benzoxazolone derivatives. II

Summary Cyano derivatives of 6-acyl-2(3H)-benzoxazolones were reacted with cysteamine HCl in ethanol to give the corresponding 6-acyl-3-thiazolinoethyl-2(3H)-benzoxazolones and their antibacterial and antifungal activities were investigated. The chemical structures were proved by means of their IR and 1H-NMR spectra and elemental analysis. Investigation of antimicrobial activity of the compounds was carried out by tube dilution and disc techniques using bacteria (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853 and Streptococcus faecalis ATCC 29212) and yeast-like fungi (Candida parapsilosis, C albicans, C pseudotropicalis and C stellatoidea). Inhibitory effects were observed for many compounds against S aureus and Bacillus subtilis. Compounds 13 and 15 had minimum inhibitory concentrations (MIC) of 8.4 and 4.2 μg/mL respectively. The antifungal studies against C albicans (10 and 16, MIC = 67.5 μg/mL), C parapsilosis (15, MIC = 67.5 μg/mL) and C stellaatoidea (9, MIC = 67.5 μg/mL) were more successful in comparison.

Synthesis and antimicrobial activity of thiazolinomethyl-2(3H)-benzoxazolone derivatives (I)

Summary A number of thiazolinoalkyl-2(3 H )-benzoxazolones have been synthesized by using cyano derivatives of 6-acyl2 (3 H )-benzoxazolones with cysteamine HCl. Their antibacterial and antifungal activities have been evaluated. The chemical structures have been proved by means of their IR, 1 H-NMR and mass spectroscopic data and by elemental analysis. The antimicrobial activity of compounds was investigated by tube dilution and disk techniques using bacteria ( Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Streptococcus faecalis RSKK 10541) and yeast-like fungi ( Candida parapsilosis, C albicans, C pseudotropicalis, C stellatoidea ). Inhibitory effects were observed for many compounds against C albicans eg, compounds 3b and 3c MIC = 25 μg/ml, C pseudotropicalis , eg, compound 3b MIC = 12.5 βg/ml, and P aeruginosa and S faecalis , eg , compound 3c , MIC = 25 μg/ml.