Download PDF by Boschke F.L. : Bioactive Organo-Silicon Compounds

By Boschke F.L.

ISBN-10: 0387093478

ISBN-13: 9780387093475

ISBN-10: 3540093478

ISBN-13: 9783540093473

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

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They have a similar structure to that of the benzhydrylether antihistamines (Chap. 1), but tend to lack strong antihistaminic activity, while they retain some of the sedative and antiparkinson activities. In vitro tests (guinea pig ileum) show a stronger anticholinergic and a weaker histaminolytic action as compared to the benzhydrylether antihistamines. 3 ] I/-~/ CH~-CH~-N__/OJ 1 77a: El = C 177b: El=Si 178a: EI=C 178b: E1= Si totype, difenidol (1 73a), is used as an antiemetic. The lower homologue, pridinol (1 74a), is effective chiefly as a central muscle relaxant and as antiparkinson agent.

2). Sila-substitution Fig. 2. Steric parameter of tricyclic psychotropic drugs: dihedral angle a; taken from Ref. 92) 40 Syntheses and Properties of Bioactive Organo-Silicon Compounds in the dimetacrine framework and melitracene skeleton should lead to different stereochemical structures for the sila-analogues 120b and 121b, because of the greater Si-C bond length (compared with the C-C bond length) and the ability of the silicon atom to interact with the n-electrons of aryl substituents (Chap.

_CH3 rat CH3 rabbit fiR3 \)-'Si-H 87b ~H3 CH 3 CH 3 31% 89 ~Y--C-OH + C-H 50% rat ~ CH3 CH3 17% 90 H2o-@ ~ ~t 87a (/ CIH3 88 86b C--H @ = glucuronide @ = unknown conjugate ~90% 86a Si-CH @ ~""~ ~- ~k CIH3 )/~---Si--OH 91 ~90% cooH + C-H 25% -- 1/2 H2% 1/2 35% 25% ~ ~ CH3 I ~ |13 ~]~'--Si-O-S i - - ~ 92 Scheme 9. Metabolisms of phenyltrimethylsilane, phenyldimethylsilane, and their carbon analogues 31 R. Tacke and U. 3 Silicon Containing Esters with Different Types of Bioactivity Further examples for relatively small changes in biological activity caused by silasubstitution, were found by Henderson et al.

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