Publication Date:
2018-03-06
Description:
The design and synthesis of ethyl 4-(6-amino-7-cyano-2,3-dihydro-1 H -pyrrolizine-5-carboxamido)-benzoate (KH16) were discussed, and its structure was determined. The anti-inflammatory activity of a new compound was evaluated using in vitro cyclooxygenase (COX) inhibitory assay. KH16 exhibits higher selectivity to COX-2 than to COX-1 with the selectivity index of 3.46. KH16 was labeled with 99 m Tc with the maximum radiochemical yield of 99 m Tc-KH16 of 90.5 ± 1.5%. Biodistribution of 99 m Tc-KH16 in normal, infected, and inflamed mice was studied. The uptake in inflamed muscle was higher than that in normal muscle throughout the examined time interval. This work is a step ahead in the direction of using pyrrolizine derivatives for site-specific delivery to the inflamed tissue.
Print ISSN:
1066-3622
Electronic ISSN:
1608-3288
Topics:
Chemistry and Pharmacology
