Volumen XLIV, Fasciculus 111 (1961) -No. 86-87 753 SUMMARY The interaction between polymyxin B and the ions Cu2+ and Ni2+ has been investigated by means of potentiometric and spectrophotometric studies. Stability constants and absorption spectra of the complexes formed suggest that proton removal from amide and y-amino groups takes place with formation of two normal and one macrocyclic chelate rings. Mg2+ did not show any direct interaction with the polymyxin .Adenosinetriphosphate on the other hand has been found to form a complex of moderate strength with polymyxinium cation.In einer ersten Mitteilung') haben wir uber basisch alkylierte und basisch acylierte Derivate des Iminodibenzyls (Ia) 2, berichtet. Einer dieser Stoffe, das 5-y-Dimethylaminopropyl-iminodibenzyl-hydrochlorid. ist als Thymolepticum3) in die Therapie eingefuhrt worden 4). Seither sind auch durch Substitution und Oxydation modifizierte Iminodibenzyle hergestellt und z. T. beschrieben wordens). Im Rahmen unserer Arbeiten in der Iminodibenzylreihe gelang es vor langerer Zeit, dieses in den Grundkorper, das 5H-Dibenz[b, flazepin (Va), das wir der Kurze halber als Iminostilben bezeichnen, uberzufiihren6) und analog aus substituierten Iminodibenzylen substituierte Iminostilbene zu bereiten. Damit wurde eine Reihe neuer und nutzlicher Zwischenprodukte fur die Arzneimittelsynthese erschlossen. Nun haben vor kurzem HUISGEN et. al.?) die Dehydrierung von Ia und dessen 5-Methylderivat zu Va resp. dem in 5-Stellung methylierten Derivat beschrieben und die physikalischen Eigenschaften dieser Stoffe zur Abschatzung der Bindungsverhaltnisse in diesem System herangezogen. Ungefahr gleichzeitig berichteten BERGMANN & RABINOWITZ~)
Reaction of the tricyclic psychotropic drug opipramoi (1) with an excess of HNO, affords a product mixture mutagenic for Salmonella typhimurium. The main product is a tetracyclic furoxan 2 (yield ca. 80%), resulting from nitrosation at C(10) and C(11) of 1. Compound 2 is not mutagenic. The essential mutagen is a nitroarene 3 formed via contraction of the central ring of 1, and nitrosation at C(2). Its yield is extremely low ( < 0.1 %). Nitroarenes have previously not been encountered as mutagenic products o f the interaction of drugs with nitrite.
256ChemInform Abstract In vitro C-nitrosation of the psychotropic drug opipramol (I) leads to the non-mutagenic main product (II) and the main mutagen (III). In vivo the formation of (III) is assumed to be 105 times slower than under in vitro conditions.
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