(3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase

Add time:07/14/2019    Source:sciencedirect.com

The HIV-1 Reverse Transcriptase (RT) is a validated and deeply explored biological target for the treatment of AIDS. However, only drugs targeting the RT-associated DNA polymerase (DP) function have been approved for clinical use. We designed and synthesised a new generation of HIV-1 RT inhibitors, based on the (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one scaffold. These compounds are active towards both RT-associated functions, DNA polymerase and ribonuclease H. The structure, biological activity and mode of action of the new derivatives have been investigated. In particular, the nature of the aromatic group in the position 4 of the thiazole ring plays a key role in the modulation of the activity towards the two RT-associated functions.

We also recommend Trading Suppliers and Manufacturers of 1-(1H-indol-2-yl)-2-methoxyethanone (cas 34559-71-2). Pls Click Website Link as below: cas 34559-71-2 suppliers

Prev:Synthesis, antimicrobial and antioxidant activities of 2-oxo-6-phenyl-2-yl-4-(2′-phenyl-5′-substituted 1H-indol-3′-yl)-1,2-dihydro pyridin-3-carbonitriles and their derivatives
Next:InCl3 mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis)