Ethyl malonate amides: a diketo acid offspring fragment for HIV integrase inhibition
Serafin, K; Mazur, P; Bak, A; Laine, E; Tchertanov, L; Mouscadet, JF; Polanski, J
| HERO ID | 4924313 |
|---|---|
| In Press | No |
| Year | 2011 |
| Title | Ethyl malonate amides: a diketo acid offspring fragment for HIV integrase inhibition |
| Authors | Serafin, K; Mazur, P; Bak, A; Laine, E; Tchertanov, L; Mouscadet, JF; Polanski, J |
| Journal | Bioorganic & Medicinal Chemistry |
| Volume | 19 |
| Issue | 16 |
| Page Numbers | 5000-5005 |
| Abstract | While searching for new HIV integrase inhibitors we discovered that some ethyl malonate amides (EMA) are active against this enzyme. Surprisingly, the main function can only very rarely be found among the reported drug candidates. We synthesised a series of compounds in order to establish and analyse the structure-activity relationship. The similarity to the important classes of HIV integrase inhibitors as well as the synthetic availability of the different targets including this pharmacophore makes EMA compounds an interesting object of investigations. |
| Doi | 10.1016/j.bmc.2011.06.054 |
| Pmid | 21767953 |
| Wosid | 000293503000031 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |
| Keyword | Enzymes; Drug development; Progeny; Structure-activity relationships; amides; pharmacophores; Integrase; Human immunodeficiency virus; 2011) |
| Is Peer Review | Yes |
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