Supervisors info:
Γεώργιος Κόκοτος, Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Summary:
Undoubtedly, the discovery of new anti-inflammatory drugs has been an active and emergent scientific field for several decades. Its ulterior aim is the discovery of anti-inflammatory drugs that diversify with the existent in terms of the mechanism of action. The reduction and even the elimination of gastrointestinal and cardiovascular side effects of non-steroidal anti-inflammatory drugs is additionally pursued. The already heightened interest in this issue, however, is increased, since the potential protection of anti-inflammatory drugs against certain types of cancer has been supported by several scientific data.
Simultaneously, riluzole, a 2-aminobenzothiazole derivative and clinically used drug, has had the utmost attention of the scientific community since its discovery, due to its wide variety of biological effects. As a result, analogs and riluzole derivatives are a potential target for the development of anti-inflammatory agents.
Recently, the Laboratory of Organic Chemistry of the University of Athens has taken action in the development of several synthetic inhibitors of PGE2 generation. Compounds that incorporate a 2-aminobenzothiazole scaffold into their structure, while containing a naphthalene ring, have been shown to potently inhibit PGE2 production at cellular level.
The aim of the present thesis was to synthesize riluzole derivatives as novel inhibitors of PGE2 production. In particular, these compounds were synthesized in order to study the role substituents such as the trifluoromethoxy group and the naphthalene ring in the activity of inhibitors. In addition, the synthesis of benzothiazolyl derivatives with reduced lipophilicity and a hydroxamic acid derivative where the skeleton of riluzole is included was sought.
Keywords:
benzothiazole, inhibitors, prostaglandin E2, riluzole
