Silapharmaka
Silapharmaka are silicon analogues of drugs in which one (sometimes several) carbon atom has been replaced by a silicon atom. Silapharmaka are so isosteric to their corresponding drugs.
The drug pridinol (X = C) and the silapharmacon sila-pridinol (X = Si)
One example is the ( R ) -Sila-venlafaxine, which isoelectronic with ( R ) - venlafaxine is, but has no activity at the SERT, this preserves the NAT and antiemetic effect. A number of other examples of silapharmaceuticals can be found in the scientific literature. The concept of the development and investigation of Silipharmaka by Reinhold Tacke (* 1949) et al. examined at the Technical University of Braunschweig.
Individual evidence
- ↑ Showell GA, Barnes MJ, Daiss JO, et al : (R) -sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis . In: Bioorg. Med. Chem. Lett. . 16, No. 9, 2006, pp. 2555-2558. doi : 10.1016 / j.bmcl.2005.12.062 . PMID 16513343 .
- ↑ Reinhold Tacke, Haryanto Linoh, Ludger Ernst, Ulrich Moser, Günter Lambrecht, Ernst Mutschler , Stefan Sarge and Heiko K. Cammenga: Sila- Pharmaka, Part 37: Representation and properties of the enantiomers of the antimuscarinic drugs sila-procyclidine and sila-tricyclamol iodide: Optically active silanols with silicon as the center of chirality , Chemischeberichte 120 , 1987, 1229-1237.
- ↑ Reinhold Tacke, Michael Strecker, Günter Lambrecht, Ulrich Moser, Ernst Mutschler: Sila-Pharmaka, 36th part: Bioisosteric C / Si exchange in parasympatholytic drugs of the Pridinol | Pridinol type , Archiv der Pharmazie 317 , 1984, 207-214.