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1 Wiadomości Chemiczne

1 2018

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Terapeutyczny potencjał pochodnych izotiazolowych : wpływ struktury związku na aktywność

Jęśkowiak I., Mączyński M., Ryng S.

Wiadomości Chemiczne

2018

[Z] 72, 11-12

867--885

Isothiazole derivatives are compounds with potentially interesting biological activity. The work on the isothiazole ring was successfully conducted by Machoń from the Department of Organic Chemistry at Wrocław Medical University. Machoń received an isothiazole derivative – Denotivirum, which is an original Polish drug. This compound has antiviral, anti-inflammatory and bacteriostatic activity against Staphylococcus aureus. Within the group of isothiazolpyrimidine derivatives, Machoń selected a compound with a very strong antitumor effect (IP-10). This combination has gone through a preclinical study. The high antitumor activity was confirmed by the Bethesda USA Research Center, which qualified him for clinical trials [1–5]. The aim of the study was to review and evaluate the latest scientific works in the field of isothiazole derivatives and, above all, the dependence of their structure on activity. The Chemical Abstracts Database and Reaxys, together with other sources of information, was searched using isothiazole keyword. As a result of the search, the majority of works describing isothiazole derivatives for the anticancer (Tab. 1), immunological among other anti-inflammatory, immunosuppressive (Tab. 2) and antiviral (Tabs 3 and 4) activity were selected. Some substances have been tested for antibacterial, antifungal, insecticidal, antiparasitic, analgesic, antidiabetic and neuroprotective properties (Tab. 5). Analyzed were only compounds containing the isothiazole ring, which are not belong to condensed heterocyclic compounds such as benzoisothiazoles, isothiazolpyridines or furoisothiazoles. In conclusion, the most interesting works presented herein illustrate a wide range of activities of isothiazole derivatives depending on their structure, which also extend the scope of biological research revealing previously barren activities of this group of compounds.