ln a previousp aper( ColottaVe.t al.,J .M ed.C hem.20004, 3,1158-11 64)w e reported thes ynthesisa ndb indinga ctivityo f 4-cycloalkylamino-1,2,4-triazolol4,3-alquinoxalin- 1-ondee rivativesd,i fferentlsyu bstitutedo n the appended2 -phenyrl ing, someo fw hichw erep otenat nds electiveA 1a denosinere cepto(rA R)a ntagonistsIn. thep resenpt apers evera4l -cycloalkylamino-2-phen,2yl,-41- triazolo[4,3-a]quinoxalin- 1-ondee rivative(s1 -11 ),b earings imples ubstituenotsn t heb enzofusemd oiety, arer eported.Thbei ndingd atao f bovineA 1a ndA 2aa ndh umanA 3A R showt hatw e haveo btainedh ighlyp otentA 1A R antagonistsIn. particularth, e4 -cyclohexylamino derivative1s- 5 showh igherAlv s A2sselectivitthya nt hep arenct ompoundA , which lackss ubstituentosn theb enzofusemd oietyM. oreoverc,o mpounds1 -11 displayi,n generalg, oodA 3A R affinityF. inallyS, ARs tudiesp rovides omen ewi nsightsa bout thes tericr equirementosf theA 3r eceptopr ocketw, hicha ccommodatetsh e benzofusedm oietyo f our 4-amino-triazoloquinoxa-lionn-1e d erivatives
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 4-CYCLOALKYLAMINO-1,2,4-TRIAZOLO[4,3-A]QUINOXALIN-1-ONE DERIVATIVES AS A1 AND A3 ADENOSINE RECEPTOR ANTAGONISTS / V. COLOTTA; D. CATARZI; F. VARANO; G.FILACCHIONI; C. MARTINI; L. TRINCAVELLI; A. LUCACCHINI. - In: ARCHIV DER PHARMAZIE. - ISSN 0365-6233. - STAMPA. - 337:(2004), pp. 35-41.
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 4-CYCLOALKYLAMINO-1,2,4-TRIAZOLO[4,3-A]QUINOXALIN-1-ONE DERIVATIVES AS A1 AND A3 ADENOSINE RECEPTOR ANTAGONISTS.
COLOTTA, VITTORIA;CATARZI, DANIELA;VARANO, FLAVIA;FILACCHIONI, GUIDO;
2004
Abstract
ln a previousp aper( ColottaVe.t al.,J .M ed.C hem.20004, 3,1158-11 64)w e reported thes ynthesisa ndb indinga ctivityo f 4-cycloalkylamino-1,2,4-triazolol4,3-alquinoxalin- 1-ondee rivativesd,i fferentlsyu bstitutedo n the appended2 -phenyrl ing, someo fw hichw erep otenat nds electiveA 1a denosinere cepto(rA R)a ntagonistsIn. thep resenpt apers evera4l -cycloalkylamino-2-phen,2yl,-41- triazolo[4,3-a]quinoxalin- 1-ondee rivative(s1 -11 ),b earings imples ubstituenotsn t heb enzofusemd oiety, arer eported.Thbei ndingd atao f bovineA 1a ndA 2aa ndh umanA 3A R showt hatw e haveo btainedh ighlyp otentA 1A R antagonistsIn. particularth, e4 -cyclohexylamino derivative1s- 5 showh igherAlv s A2sselectivitthya nt hep arenct ompoundA , which lackss ubstituentosn theb enzofusemd oietyM. oreoverc,o mpounds1 -11 displayi,n generalg, oodA 3A R affinityF. inallyS, ARs tudiesp rovides omen ewi nsightsa bout thes tericr equirementosf theA 3r eceptopr ocketw, hicha ccommodatetsh e benzofusedm oietyo f our 4-amino-triazoloquinoxa-lionn-1e d erivativesFile | Dimensione | Formato | |
---|---|---|---|
ArchPharm 2004,337,35-41.pdf
Accesso chiuso
Tipologia:
Versione finale referata (Postprint, Accepted manuscript)
Licenza:
Tutti i diritti riservati
Dimensione
845.74 kB
Formato
Adobe PDF
|
845.74 kB | Adobe PDF | Richiedi una copia |
I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.