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.

IN THE LAST FEW YEARS, A MARKED DECREASE IN MALE FERTILITY HAS BEEN REPORTED. ENVIRONMENTAL FACTORS WERE RECENTLY SUSPECTED FOR THIS EFFECT. AMONG THOSE FACTORS IS THE MISUSE OF DRUGS AND IN PARTICULAR ANTIBIOTICS. THE AIM STUDY ADVERSE TESTICULAR EFFECTS OF SOME QUINOLONE MEMBERS (OFLOXACIN, CIPROFLOXACIN) IN RATS, OFLOXACIN ARE A GROUP OF ANTIBACTERIAL AGENT S WITH BROOD SPECTRUM ACTIVITY. IN THE STUDY MALE WISTAR ALBINO RATS WERE GIVEN OFLOXACIN ORALLY AT A DOSE OF 20MG/KG BODY WEIGHT PER DAY, FOR 60 SAYS, AND WERE KILLED 24H AFTER THE LAST TREATMENT. PARAMETERS OF TESTICULAR Cytotoxicity INCLUDED GENITAL ORGAN WEIGHTS, TESTICULAR SPERM CONUTS, EPIDIDYMAL SPERM MOTILITY AND MORPHOLOGY AND HISTOPATHOLOGIC EXAMINATIONS (BY STANDARD HEMATOXYLIN-EOSIN STAINING). AT 20MG/KG, THE WEIGHTS OF TESTIES, EPIDIDYMIDES, AND SEMINAL VESICLES WERE NOT DIFFERENT AMONG THE CONTROL GROUPS. THE NUMBER OF TESTICULAR SPERM MOTILITY AND MORPHOLOGY OF EPIDIDYMAL SPERM WERE DECREASED. HISTOLOGICAL RESULTS OF TESTES MEDICATED ABNORMALITY IN SPERMATOGENESIS AND SPERMS PRODUCTION IN SOME OF THE SOMNIFEROUS TUBULES. MOREOVER, ADMINISTRATION OF OFLOXACIN RESULTED IN MARKED TESTICULAR HISTOPATHOLOGICAL CHANGES. IT IS CONCLUDED THAT OFLOXACIN SIGNIFICANTLY IMPAIRED BOTH TESTICULAR FUNCTION AND STRUCTURE IN RATS.