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Bioactive Organo-Silicon Compounds by Boschke F.L.

By Boschke F.L.

Content material: Tacke, R. and Wannagat, U. Syntheses and houses of bioactive organo-silicon compunds. -- Voronkow, M. G. organic task of silatianes

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Compounds of type 155 exhibit in contrast to their carbon analogue only a short duration of activity (because of hydrolytic inactivation), which is even shorter than that of the basic sila-benzhydrylethers themselves. Sila-ciclonium bromide (156b), which was synthesized 1~ 107) according to Scheme 19, is a silicon analogue of the spasmolytic ciclonium bromide (156a). It exhibits also a strong spasmolytic ac|ivity like the carbon analogue 112). However, its biological effect is of shorter duration than that of ciclonium bromide itself.

4) there is only a slight activity, which corresponds approximately to the silanol 168. This fragment exhibits also a weak non-specific activity 118). In vitro tests at the isolated left auricle of guinea pigs have shown that 15 7b and some of its derivatives prolong the functional refractory period, which can be compared approximately with that of the drug quinidine. Between the analogues 15 7a and 15 7b no significant differences were observed at all with this pharmacological model 118). 8 mg/kg (570/lmol/kg)].

CHa)aEI~o_CO_NHCH 3 103a: EI = C 103b: El= Si (CH 3)3El ""~ ~x-''O-CO-N HCH3 105a: El = C 105b: El= Si 34 104a: E1 = C 104b: El = Si Syntheses and Properties of BioactiveOrgano-SiliconCompounds Compound 103b was found to be more active than the isomeric silicon derivatives 104b and 105b. This structure-activity relationship is comparable to that of the corresponding carbon analogues 104a resp. 105a. Comparative investigations of insecticidal properties of the analogous compounds 103a and 103b against Culex pipiens quinquefasciatus and Musca domestica also led to similar results.

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