NEW N6-OR N(9)-HYDROXYALKYL SUBSTITUTED 8-AZAADENINES OR ADENINES AS AFFECTIVE A1 ADENOSINE RECEPTOR LIGANDS

In this paper we describe synthesis and biological assays of some A, ligands more water-soluble than the effective, but very lipophilic. 8-azaadenines and adenines discovered in the past and obtained introducing on N-6 or N(9) substituent a hydroxy group. Five of the new N-6-hydroxyalkyl- and N-6-hydroxycycloalkyl-2-phenyl-9-benzyl-8-azaadenines showed very high affinity (Ki < 40 nM) and selectivity for A, adenosine receptors. Among the 2-phenyl-9-(2-hydroxy-3-alkyl)-8-azaadenines or adenines prepared, the compounds with the higher A, affinity and selectivity resulted 2-phenyl-9-(2-hydroxy-3-propyl)-N-6-cyclopentyl- and cyclohexyl-8-azaadeninewith Ki 2.2 +/- 0.2 nM and 2.8 +/- 0.3 nM respectively. From the point of view of water-solubility, 2-phenyl-9-(2-hydroxy-3-propyl)-8-azaadenine was the most interesting compound, having a CLogP of 1.066991 and a water-solubility of 1.2 mg in L-1. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved

1H MRS in vivo e in vitro e correlazioni anatomo-patologiche in neoplasie extracerebrali: considerazioni su due casi.

Da anni molti lavori della letteratura sono dedicati al tentativo di tipizzare istologicamente i tumori cerebrali mediante l'utilizzo della spettroscopia RM del protone (1HMRS) in vivo. scopo dello studio \ue8 verificare l'affidabilit\ue0 della 1HMRS single voxel nei tumori extracerebrali per la diagnosi differenziale fra meningiomi della volta e metastasi durali, descritte in letteratura come caratterizzate dalla presenza di lipidi