Abstract
| - The synthesis of some new aminoadamantane derivatives isdescribed. The new compoundswere evaluated against a wide range of viruses [influenza A H1N1,influenza A H2N2, influenzaA H3N2, influenza B, parainfluenza 3, herpes simplex virus type 1(HSV-1) and type 2 (HSV-2), thymidine kinase-deficient (TK-) HSV-1, vaccinia,vesicular stomatitis, polio 1, CoxsackieB4, Sindbis, Semliki forest, Reo 1, varicella-zoster virus (VZV),TK- VZV, human cytomegalovirus (HCMV), and human immunodeficiency virus type 1 (HIV-1) and type 2(HIV-2)]. Someof them proved markedly active against the influenza A H2N2 (compounds4a,b, 5a, 6a,and7a), H3N2 (compounds 5a, 6a, and7a), and H1N1 (compounds 4b,c and6d). Since compounds5a, 6a, and 7a, amantadine, andrimantadine showed the same comparative pattern of potencyagainst influenza strains H2N2, H3N2, and B, it may postulated thatthey act according to asimilar mechanism, with regard to their “amine” effect, on the M2ion channel of influenza A(H1N1, H2N2, or H3N2). In general, no significant activity wasnoted with any of the newcompounds against any of the other viruses tested, making theiractivity against influenzavirus more specific and striking. Borderline activity was notedwith some of the compounds(4b,c, 5a−c, and8a) against HIV-1.
|