Benzothiazole and Benzoxazole Derivatives Synthesis as Prostaglandin E2 Production Inhibitors

Postgraduate Thesis uoadl:2879675 322 Read counter

Unit:
Κατεύθυνση Οργανική Σύνθεση και Εφαρμογές της στη Χημική Βιομηχανία
Library of the School of Science
Deposit date:
2019-07-24
Year:
2019
Author:
Theodoropoulou Maria
Supervisors info:
Γεώργιος Κόκοτος, Καθηγητής, Τμήμα Χημείας, ΕΚΠΑ
Original Title:
Σύνθεση Βενζοθειαζόλυλο και Βενζοξαζόλυλο Παραγώγων ως Αναστολέων της Παραγωγής Προσταγλαδίνης Ε2
Languages:
English
Greek
Translated title:
Benzothiazole and Benzoxazole Derivatives Synthesis as Prostaglandin E2 Production Inhibitors
Summary:
Recently, there has been high interest in the discovery of new anti-inflammatory drugs which, unlike existing non-steroidal anti-inflammatory drugs, would present a new mechanism of action and would, as far as possible, be deprived of gastrointestinal and cardiovascular side effects. In addition, the potential protection that anti-inflammatory drugs may provide against certain types of cancer has come to light.
As a result, in addition to cyclooxygenase-2 (COX-2) inhibitors, phospholipases A2 (PLA2) and microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors have been designed and synthesized in recent years, in an effort to find new means to combat inflammatory conditions.
Recently, in the Laboratory of Organic Chemistry of the University of Athens, several synthetic inhibitors of PGE2 production have been developed, including inhibitors of various PLA2 subclasses. Compounds based on a 2-aminobenzothiazole backbone, containing a naphthalene ring, have been found to exhibit strong inhibition of PGE2 production at cellular level.
In the present thesis, the aim was to synthesize new inhibitors of PGE2 production in order to study their structure-activity relationship as anti-inflammatory agents. In particular, compounds were synthesized to study the substitution position of the naphthalene ring, the reduction of lipophilicity and the role of the benzothiazole ring. Also, the compounds synthesized have been studied for their cytotoxicity against diverse cell lines.
Main subject category:
Science
Keywords:
prostaglandin E2, inhibitors, benzothiazole
Index:
Yes
Number of index pages:
3
Contains images:
Yes
Number of references:
186
Number of pages:
152
Σύνθεση Βενζοθειαζόλυλο και Βενζοξαζόλυλο Παραγώγων ως Αναστολέων της Παραγωγής Προσταγλαδίνης Ε2.pdf (3 MB) Open in new window