Abstract:
:A series of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo[4,5-e] [1,2,4]thiadiazines (PTDs) was synthesized, structurally confirmed by spectral analysis, and evaluated for their anti-HIV activities by inhibition of HIV-induced cytopathogenicity in MT-4 cell culture. The results showed that some compounds exhibited inhibitory activity specifically against HIV-2 replication. The most active HIV-2 inhibitor was compound 7i (R1 = benzyl, R2 = 4-t-butyl-benzyl) with an EC50 value of 18.7 microM and SI=15, which may provide a useful lead for further molecular optimization.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Liu XY,Yan RZ,Wang Y,Zhan P,De Clercq E,Pannecouque C,Witvrouw M,Molina MT,Vega Sdoi
10.1002/ardp.200700216subject
Has Abstractpub_date
2008-04-01 00:00:00pages
216-22issue
4eissn
0365-6233issn
1521-4184journal_volume
341pub_type
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