AI Article Synopsis
- Researchers developed inhibitors for the HCMV protease using a monocyclic beta-lactam structure, which effectively modify the viral enzyme over time.
- Evidence from structure-activity relationship (SAR) studies on monocyclic beta-lactam N-ureas helped identify the optimal size and stereochemistry of the C-3 substituent.
- The resulting compound 17b emerged as a low micromolar inhibitor, demonstrating strong stability in water and selectivity compared to mammalian serine proteases.
Article Abstract
Mechanism based inhibitors of HCMV protease have been designed based on the monocyclic beta-lactam nucleus, which have been shown to acylate the viral enzyme in a time dependent manner. SAR in a series of monocyclic beta-lactam N-ureas, has defined the size and relative stereochemistry of the C-3 substituent producing a low micromolar inhibitor 17b with good aqueous stability and selectivity over the mammalian serine proteases.
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| http://dx.doi.org/10.1016/s0960-894x(98)00032-8 | DOI Listing |
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