Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.
Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.
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吡咯烷二酮酸衍生物作为HIV-1整合酶双重抑制剂和逆转录酶核糖核酸酶H结构蛋白H结构域的结构活性关系。
DOI：
10.1021/jm501799k
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发表时间：
2015-02-26
影响因子：
7.3
通讯作者：
Di Santo R
中科院分区：
文献类型：
--
作者：
Cuzzucoli Crucitti G;Métifiot M;Pescatori L;Messore A;Madia VN;Pupo G;Saccoliti F;Scipione L;Tortorella S;Esposito F;Corona A;Cadeddu M;Marchand C;Pommier Y;Tramontano E;Costi R;Di Santo R
The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors.
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影响因子：
7.3
作者：
Brühlmann, C;Ooms, F;Carotti, A
通讯作者：
Carotti, A
影响因子：
4.9
作者：
Chung, Suhman;Wendeler, Michaela;Le Grice, Stuart F. J.
通讯作者：
Le Grice, Stuart F. J.
影响因子：
7.3
作者：
Costi R;Métifiot M;Chung S;Cuzzucoli Crucitti G;Maddali K;Pescatori L;Messore A;Madia VN;Pupo G;Scipione L;Tortorella S;Di Leva FS;Cosconati S;Marinelli L;Novellino E;Le Grice SF;Corona A;Pommier Y;Marchand C;Di Santo R
通讯作者：
Di Santo R
影响因子：
6.7
作者：
Billamboz, Muriel;Bailly, Fabrice;Cotelle, Philippe
通讯作者：
Cotelle, Philippe
影响因子：
4.9
作者：
Corona, Angela;Di Leva, Francesco Saverio;Tramontano, Enzo
通讯作者：
Tramontano, Enzo