76751-95-6Relevant academic research and scientific papers
SUBSTITUTED BENZOXAZOLONE DERIVATIVES AS ACID CERAMIDASE INHIBITORS, AND THEIR USE AS MEDICAMENTS
-
Page/Page column 18; 38; 44, (2015/12/31)
The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.
Synthesis and antibacterial and antifungal properties of thiazolinoethyl-2(3H)-benzoxazolone derivatives. II
Erol,Aytemir,Yulug
, p. 731 - 734 (2007/10/03)
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 antimicrobiaI 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)
Erol,Aytemir,Yulug
, p. 521 - 524 (2007/10/02)
A number of thiazolinoalkyl-2(3H)-benzoxazolones have been synthesized by using cyano derivatives of 6-acyl-2(3H)-benzoxazolones with cysteamine HCl. Their antibacterial and antifungal activities have been evaluated. The chemical structures have been proved by means of their IR, 1H-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 μg/ml, and P aeruginosa and S faecalis, eg, compound 3c, MIC = 25 μg/ml.
CATALYTIC ACYLATION OF BENZOXAZOLIN-3-ONES IN THE PRESENSCE OF ZINC CHLORIDE
Mukhamedov, N. S.,Kristalovich, E. L.,Plugar, V. N.,Giyasov, K.,Aliev, N. A.,Abdullaev, N. D.
, p. 982 - 984 (2007/10/02)
In the acylation of benzoxazolin-2-ones by aromatic acid chlorides in the presence of 10-2 mole ZnCl2, the yields of the corresponding 6-aroylbenzoxazolin-2-ones depend on the electronegativity of the acylating agent and the nucleophilicity of
Analgesic and antiinflammatory activity screening of 6-acyl-3-piperidinomethyl-2(3H)-benzoxazolone derivatives
Erol,Demirdamar
, p. 663 - 666 (2007/10/02)
6-Acyl-2(3H)-benzoxazolone derivatives were reacted with appropriate piperidine derivatives and formaldehyde in methanol to give the corresponding 6-acyl-3-piperidinomethyl-2(3H)-benzoxazolones. The obtained compounds were screened for their analgesic and antiinflammatory activities. Analgesic activity of these compounds was investigated by modified Koster test. Antiinflammatory activity was assayed by using carrageenan induced mouse paw edema test and arachidonic acid edema. The 15 compounds synthesized showed good analgesic activities; compounds 1, 3 and 6 moved to be active inhibitors of edema.
Synthesis of some new Mannich bases derived from 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones and their biological activities
Erol,Rosen,Erdogan,Yulug
, p. 851 - 853 (2007/10/02)
A number of 6-acyl-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolones have been synthesized by Mannich reaction and their antibacterial and antifungal activities have been tested. Their chemical structures have been proved by means of their IR, NMR, mass spectroscopic data and by elementary analysis. Investigation of antimicrobial activity of compounds was done by tube dilution and paper disc techniques using bacteria (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus faecalis RSKK 10541) and yeast-like fungi (Candida parapsilosis, Candida albicans, Candida pseudotropicalis, Candida stellatoidea). Among the compounds tested 6-(2-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolone (Compound 2) and 6-(3-chlorobenzoyl)-3-(3,5-dimethylpiperidinomethyl)-2(3H)-benzoxazolone (Compound 3) showed the most favorable activity.
