Paper Information

Title: 

CYTOTOXICITY OF 3-ISOTHIAZOLONE DERIVATIVES

Type: SPEECH
Author(s): KHALAJ A.,ADIBPOUR N.
 
 
 
Name of Seminar: IRANIAN CONGRESS OF TOXICOLOGY
Type of Seminar:  CONGRESS
Sponsor:  SOCIETY OF TOXICOLOGY
Date:  2004Volume 8
 
 
Abstract: 

3-Isothiazolone derivatives have shown antibacterial, antimycotic, antialgual and pesticidal activity and have been used as preservatives for the control of living organisms in cosmetics, paints, soaps, fabrics, leather, swimming pools, etc. for many years. Considering the limited number of reports on the mechanism of action and toxicity of 3-isothiazolones some reported and novel N-phenyl 3-isothiazolones with or without chlorine atom at the 5-position and having substituents at the 4-position of the phenyl moiety with different physicochemical properties were prepared and their antibacterial and antifungal activity were determined.
The majority of compounds displayed moderate to high activity against some tested pathogenic bacteria and had MICs in the range of ciprofloxacin as the most active reference drugs and some compounds had either equal or higher antifungal activity in comparison with Itraconazole and Ketoconazole as standard drugs against the most tested fungi. These findings prompted us to determine the cytotoxicity of the most potent compounds of this investigation.
Cytotoxicity of compounds XXVIII, XXXIII, XXXV, XXXVII, LXIX, LXXI was determined by the MTT test on HFFFp-16 cells, in comparison with Itraconazole as the reference drug
.
5-Chloro-2(4-chlorophenyl)-4-isothiazoline-3-one XXXV which had highest activity against gram positive and gram negative bacteria and was one of the most active compounds of this study against tested fungi, had lower toxicity than Itraconazole and other synthsized compounds
.
Preparation of 3-isothiazolones having biological activity comparable to the widely used antibacterial and antifungal drug encourage further investigation on these compounds
.

 
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