Photo toxic

In addition to BAY X 8843 36, its 8-chlorine analogue 8-chloro-l-cyclopropyl-7-(S,S-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-l,4-dihydro-4-oxo-3-quinolinecarbo-xylic acid hydrochloride BAY Y 3118 45 was also an important developmental candidate. Due to its broad activity spectrum, which included anaerobic bacteria [129-136], it had the potential for becoming a problem-solver . Unfortunately, during the Phase I trials photo toxic side effects occurred [137] which were due to the chlorine substituent in the 8-position, and these led to an abandonment of the development of this compound. 

In the treatment of tuberculosis, resistant strains of M. tuberculosis (multidrug-resistant tuberculosis, MDRTB) present a growing problem, so that new antituber-culotic agents are required which act according to a different mechanism to that of standard agents such as isoniazid, rifampicin, pyrazinamide, and ethambutol. The more modern fluoroquinolones are of particular interest, and in particular moxifloxacin, which has powerful in vitro and in vivo activity and, in contrast to sparfloxacin and clinafloxacin, is not photo toxic [191]. 

Free of lingering photo-toxicity effects, cutaneous or otherwise... 

Furanocoumarins are extremely toxic. They are known to cause photo-toxicity if not used under medical supervision. Furanocoumarins bind to DNA of the cell and interacts with fats and proteins. Phenylalanine, Umbelliferon, a hydroxycoumarin and isoprene, are precursor compounds for furanocoumarin biosynthesis. The furanocoumarins have shown antibacterial activity against Escherichia coli and Micrococcus luteus. They are hepatotoxic also. 

They have also shown photosensitizing and photo-toxic effects in animals and humans and have been used in photochemotberapy for management of vitiligo, psoriasis, and mycosis fungoides, cf. T. F. Anderson, J. J. Voorhees, Ann. Rev. Pharmacol. Toxicol 20, 235 (1980) A. Korn-bauser et al, Science 217, 733 (1982). Review of psoralen photochemistry B. J. Parsons, Photochem. Photobiol. 32,... 

Methylcoumarin, a synthetic fragrance in a variety of cosmetics and toiletries, is alleged to be a potent experimental photocontact allergen but does not produce photo toxic reaction (Katoby and Kligman 1978). 

Adverse effects of cutaneous preparations may be undesirable systemic effects, (photo) toxicity, irritation or (photo) allergic responses after sensitisation. Substance monographs [15], package leaflets or SmPCs of licensed products and medicine databases give information about these adverse effects. 

No sensitization.-No photo-toxic properties. -Non-teratogenic. -Non-mutagenic. 

The irradiation conditions described in the experimental section were taken in order to closer resemble the conditions under which their photo-toxicity and the possible phototherapy applications are produced in biological media or in vitro or in vivo cellular systems. 

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