Radiosynthesis and biological evaluation of [111]in-tris [8-hydroxy-2-methylquinoline] complex as a possible imaging agent

Due to the interesting pharmacological properties of radiolabeled metal oxine derivatives such as cell internalization, tumor avidity and antiproteosome activity, [111]In-tris[8-Hydroxy-2-methylquinoline] [[111]In-HMQ] was developed in this study. [111]In-HMQ was prepared using [111]InCl[3] and 8-Hydroxy-2-methylquinoline [HMQ] for 60 min at 100[degree sign] C [radiochemical purity: >99% ITLC, >99% HPLC, specific activity: 13-14 GBq/mmol]. Stability of the complex was checked in final formulation and in the presence of human serum for 48 h. The partition coefficient was calculated for the compound [log P=0.68]. The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT up to 24 h. A detailed comparative pharmacokinetic study for [111] In cation and [111]In-HMQ are performed up to 24h. The complex is mostly cleaned from the circulation by kidneys and is a compound rapidly washing from the circulation. The biodistribution of the complex in tumor models is on-going

Derivados azoicos da oxina com sulfas potencialmente antimalaricas / Oxine azoic derivatives with potentially antimalarial sulfonamides

Com o objetivo de obter farmacos potencialmente antimalaricos prepararam-se, pelo processo de hibridacao molecular, cinco compostos mediante reacao do sal de diazonio e sulfas antimalaricas - sulfadiazina, sulfadoxina, sulfametoxipiridazina, sulfametoxazol e sulfamonometoxina - com a oxina (8-hidroxiquinolina). Submetidos a analises espectrometricas - IV, UV, RMP -, os derivados apresentaram caracteristicas das estruturas propostas