[Newer antimycotics. I. Derivatives of phenyl-hydrazine (author's transl)].
The author produced a number of derivatives of phenyl-hydrazine and its analogues, investigated their antimicrobial efficiency in vitro, and discussed the association of chemical structure with the fungistatic effect in the series of phenyl-hydrazine-derivatives. From the author's results it can be concluded that the halogen-substituted phenyl-hydrazines and their N-(acetyl)-derivatives exert a moderate fungistatic effect (Tab. 1). In the series of N-aryl-sulphonyl-N'-phenyl-hydrazines only the compounds derived from 3,4-dichloro-phenyl-hydrazine proved to be effective; the other representatives of this type were fully ineffective (Tab. 1). The majority of the halogen-substituted N-aroyl-N'-phenyl-hydrazines exerted a relatively strong fungistatic activity with a broad spectrum of efficiency (Tab. 2). On the contrary, their analogues having a -CO-NH- group in place of the -CO-NH-NH-group, were fully inactive (Tab. 3). From the investigated derivatives of phenyl-hydrazine, the N-benzoyl-, N-(2-chloro-benzoyl)-, N-(4-chloro-benzoyl)- and N-furoyl-derivatives of 3- and 4-chloro-phenyl-hydrazine, furthermore the N-benzoyl- and N-furoyl-derivatives of 3,4-dichloro-phenyl-hydrazine were most effective (Tab. 2). The acute toxicity in the mouse of these effective compounds was relatively small; they were found to be significantly less toxic than tetramethyl-thiuramdisulfide (Tab. 4). On the basis of an intensive fungistatic efficiency and small toxicity of the halogen-substituted N-aroyl-N'-phenyl-hydrazines, it seems that a number of representatives of these types of chemical compounds could be given a role in the chemotherapy of superficial human and animal dermatomycoses, and also in the chemoprophylaxis of certain phytomycoses.
D000528:Alternaria / Q000187:drug effects; D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects*; D001230:Aspergillus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D002963:Cladosporium / Q000187:drug effects; D003470:Culture Media; D005670:Fusarium / Q000187:drug effects; D051379:Mice; D003904:Mitosporic Fungi / Q000187:drug effects*; D010407:Penicillium / Q000187:drug effects; D010659:Phenylhydrazines / Q000494:pharmacology* / Q000633:toxicity; D012232:Rhizoctonia / Q000187:drug effects; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D013329:Structure-Activity Relationship; D014249:Trichophyton / Q000187:drug effects; D014588:Ustilago / Q000187:drug effects
D000935:Antifungal Agents; D003470:Culture Media; D010659:Phenylhydrazines
Neuere Antimycotika. I. Phenylhydrazin-Derivate