Κατεύθυνση Σχεδιασμός και Ανάπτυξη νέων Φαρμακευτικών Ενώσεων - Φαρμακευτική Χημεία
Library of the School of Science

2019-01-23

2019

Georgiadis Markos-Orestis

Παπαναστασίου Ιωάννης, Επίκουρος Καθηγητής, Φαρμακευτικής, ΕΚΠΑ

ΣΧΕΔΙΑΣΜΟΣ, ΣΥΝΘΕΣΗ ΚΑΙ ΑΠΟΤΙΜΙΣΗ ΤΗΣ ΑΝΤΙΤΡΥΠΑΝΟΣΩΜΙΑΚΗΣ ΔΡΑΣΗΣ ΝΕΩΝ ΑΔΑΜΑΝΤΑΝΙΚΩΝ ΘΕΙΑΖΟΛΙΩΝ

Greek

DESIGN, SYNTHESIS AND TRYPANOCIDAL ACTIVITY OF NOVEL ADAMANTANE THIAZOLES

In the context of the present MSc dissertation, the design, synthesis and pharmacological evaluation, against T. brucei, of a series of novel adamantane thiazoles is described. Specifically, the 4-substituted-2-[3-(adamant-1-yl)-4-flurophenyl]thiazoles 12 and 13a-i were designed and synthesized. In order to test the effect of the adamantane substitution of the aromatic ring, as well as the spatial arrangement of the side thiazole chain on to the antitrypanosomial activity, the homologues 4-substituted-2-[4-(adamant-1-yl-phenyl]thiazoles 18, και 19a-c were synthesized. Additionally, the 2-ethylene-4-[4-(adamant-1-yl)phenyl]thiazoles 31c,d were designed and synthesized in an attempt to probe how the antirypanosomial activity is affected when the substituents of the thiazole moiety interchanged positions. Moreover, the effect of the distance between the polar cationic head and the thiazole moiety, on the antiparasitic activity, was tested via the aminothiazole 31a and the aminomethylethiazole 31b. The preliminary pharmacological evaluation revealed the potency of the amine 12 (IC50 420 nM).

Science

Trypanosoma brucei, Trypanosoma cruz, NMR

Yes

1

Yes

120

96

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https://pergamos.lib.uoa.gr/uoa/dl/object/2843791