Synthesis and Antiviral Activity of 1-[(1,5-Dialkyl-1H-1,2,4-triazol-3-yl)methyl]thymines

Cycloaddition of the intermediates 2 with 1‐(cyanomethyl)‐thymine 3 furnished the 1,2,4‐triazolium salts 4, which rearranged spontaneously to the protonated salts 5. Hydrolysis of 5, in situ, afforded the title compounds 6. Compounds 6a‐c were screened against HIV‐1 (IIIB), HIV‐2 (ROD), and human cy...

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Veröffentlicht in:	Archiv der Pharmazie (Weinheim) 1999-04, Vol.332 (4), p.143-144
Hauptverfasser:	Al-Soud, Yaseen A., Al-Masoudi, Najim A.
Format:	Artikel
Sprache:	eng
Schlagworte:	AIDS/HIV Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Biological activity Biological and medical sciences cumulenes cycloaddition Humans Medical sciences nucleosides Pharmacology. Drug treatments pyrimidines Thymine - chemical synthesis Thymine - pharmacology
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Beschreibung
Zusammenfassung:	Cycloaddition of the intermediates 2 with 1‐(cyanomethyl)‐thymine 3 furnished the 1,2,4‐triazolium salts 4, which rearranged spontaneously to the protonated salts 5. Hydrolysis of 5, in situ, afforded the title compounds 6. Compounds 6a‐c were screened against HIV‐1 (IIIB), HIV‐2 (ROD), and human cytomegalovirus (HMCV) and showed poor or no activity, respectively.
ISSN:	0365-6233 1521-4184
DOI:	10.1002/(SICI)1521-4184(19994)332:4<143::AID-ARDP143>3.0.CO;2-C