Thiazole is a well-known five-membered heterocyclic compound. Various methods have been worked out for its synthesis. In the last few decades, a lot of work has been done on thiazole ring in order to find new compounds related to this scaffold acting as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective and antitumor or cytotoxic drugs with lesser side effects. This review presents the up to date development of different thiazole derivatives. The present review gives an account of the recent therapeutic patent literature (2008-2012) describing the applications of thiazole and its derivatives on selected activities. In this review many of relevant biological properties and the therapeutic applications of thiazole derivatives reported in international patents from all companies have been discussed; an overview of the chemical matter has also been given. Because of the huge amount of patents registered in this period relative to thiazole derivatives, we focused our attention, in the first part of the review just published, on inhibitors of phosphatidylinositol-3-kinase, inhibitors of protein kinase and derivatives modulating enzymes related to metabolism, whereas in this second part we focused on thiazole derivatives having pharmacological activity towards receptors. Based on the large variety of possible therapeutic applications proposed in patents for thiazole derivatives having pharmacological activity towards receptors, it is possible to point out the unpredictability of pharmacological activity consequent to structural modification, more or less simple, of a prototype drug molecule. In any case the thiazole scaffold remains one of great potential for the chemical pharmaceutical research.
Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi (2014). Novel thiazole derivatives: a patent review (2008-2012. Part.2). EXPERT OPINION ON THERAPEUTIC PATENTS, 24(7), 759-777 [10.1517/13543776.2014.910196].
Novel thiazole derivatives: a patent review (2008-2012. Part.2)
LEONI, ALBERTO;LOCATELLI, ALESSANDRA;MORIGI, RITA;RAMBALDI, MIRELLA
2014
Abstract
Thiazole is a well-known five-membered heterocyclic compound. Various methods have been worked out for its synthesis. In the last few decades, a lot of work has been done on thiazole ring in order to find new compounds related to this scaffold acting as antioxidant, analgesic, anti-inflammatory, antimicrobial, antifungal, antiviral, diuretic, anticonvulsant, neuroprotective and antitumor or cytotoxic drugs with lesser side effects. This review presents the up to date development of different thiazole derivatives. The present review gives an account of the recent therapeutic patent literature (2008-2012) describing the applications of thiazole and its derivatives on selected activities. In this review many of relevant biological properties and the therapeutic applications of thiazole derivatives reported in international patents from all companies have been discussed; an overview of the chemical matter has also been given. Because of the huge amount of patents registered in this period relative to thiazole derivatives, we focused our attention, in the first part of the review just published, on inhibitors of phosphatidylinositol-3-kinase, inhibitors of protein kinase and derivatives modulating enzymes related to metabolism, whereas in this second part we focused on thiazole derivatives having pharmacological activity towards receptors. Based on the large variety of possible therapeutic applications proposed in patents for thiazole derivatives having pharmacological activity towards receptors, it is possible to point out the unpredictability of pharmacological activity consequent to structural modification, more or less simple, of a prototype drug molecule. In any case the thiazole scaffold remains one of great potential for the chemical pharmaceutical research.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.