title: Synthesis and biological activity of some 4-substituted 1-[1-(2,3-dihydroxy-1-propoxy)methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
abstract: Cycloaddition of 7a, b with 6 gave, after separation and deprotection, two regioisomers 10a, b and 11a, b. The deprotected acyclic nucleoside 10a used as the precursor for the preparation of 4-amino (12), 4-methylamino (13), 4-benzylamino (14), 4-methoxy (15) and 4-hydroxy (16) analogues. All acyclic nucleosides were evaluated for their inhibitory effects against HIV-1(IIIB), HIV-2(ROD) in MT-4 cells, for their anti-tumor activity and for their inhibitory effects against Mycobacterium tuberculosis. No marked activity was found.
authors.affiliation: Laboratoire de Chimie Bio-Organique, Faculté des Sciences, Agadir, Morocco.
authors.forename: Omar
authors.initials: O
authors.lastname: Moukha-chafiq
authors.forename: Mohamed Labd
authors.initials: ML
authors.lastname: Taha
authors.forename: Hassan Bihi
authors.initials: HB
authors.lastname: Lazrek
authors.forename: Jean-Jacques
authors.initials: JJ
authors.lastname: Vasseur
authors.forename: Christophe
authors.initials: C
authors.lastname: Pannecouque
authors.forename: Myriam
authors.initials: M
authors.lastname: Witvrouw
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D009705:Nucleosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D009705:Nucleosides; D011743:Pyrimidines; D014230:Triazoles