ABSTRACT
The synthesis of multifunctional spirocycles was achieved from common cyclic carboxylic acids (cyclobutane carboxylate, cyclopentane carboxylate, l-proline, etc.). The whole sequence included only two chemical steps-synthesis of azetidinones, and reduction into azetidines. The obtained spirocyclic amino acids were incorporated into a structure of the known anesthetic drug Bupivacaine. The obtained analogues were more active and less toxic than the original drug. We believe that this discovery will lead to a wide use of spirocyclic building blocks in drug discovery in the near future.
Subject(s)
Azetidines/chemical synthesis , Azetidines/pharmacology , Drug Discovery , Spiro Compounds/chemical synthesis , Spiro Compounds/pharmacology , Anesthetics/chemistry , Azetidines/chemistry , Bupivacaine/chemistry , Carboxylic Acids/chemistry , Cyclopentanes/chemistry , Proline/chemistry , Spiro Compounds/chemistryABSTRACT
Among many and various products, born by the modern nanotechnology, gold nanoparticles roused a special interest of biomedical researchers. Unique features of the nanoparticles allow to use them not only as effective transporters for therapeutic agents but also as basic components of nanocomposite preparations intended for targeted photodynamic and photothermal therapy of tumours. In the review, physical, chemical and biological properties of gold nanoparticles which can promote PDT efficiency of a designed nanocomposite, are briefly characterized, and promising trends in creation of gold-containing composite photosensitizers are analysed.
