DRUGS IN THE TETRAZOLE SERIES REVIEW四氯呋喃类药物审查中的药物.pdfVIP

Chemistry of Heterocyclic Compounds, Vol. 43, No. 1, 2007 DRUGS IN THE TETRAZOLE SERIES. (REVIEW)* 1 2 1 L. V. Myznikov , A. Hrabalek , and G. I. Koldobskii Data on drugs of the tetrazole series published over the last decade are reviewed. The use of tetrazoles as isosteric substituents of various functional groups is examined. Keywords: tetrazole, biological activity, isosteric substituent. The outstanding achievements of the pharmaceutical chemistry in the last decade are due in no small way to the creation of novel drugs containing a tetrazole ring as structural fragment. Tetrazoles have not been found in nature. With rare exceptions these compounds do not exhibit appreciable biological activity, but they are at the same time resistant to biological degradation. It is this property that makes it possible to use tetrazoles as isosteric substituents of various functional groups in the development of biologically active substances. In spite of the fact that the number of papers in which tetrazoles are mentioned in connection with the creation of new pharmaceutical products is increasing there have been no reviews on the use of tetrazoles in this field. The aim of the present review was to classify the abundant data on this subject published in the last decade. 1-SUBSTITUTED TETRAZOLES 1-Substituted tetrazoles have not yet been widely used for the creation of pharmaceutical products. The best known are certain derivatives of β-lactam antibiotics and optically active tetrazole-containing antifungal preparations of the azole type, such as TAK-456 (1) [ 1,2]. Me Me O N