Id |
Subject |
Object |
Predicate |
Lexical cue |
T480 |
124-329 |
Sentence |
denotes |
The in vitro kinetic plasma solubility has been increased by a factor of ~19 (from 6 µM for the lead to 112 µM for best derivative), and the thermodynamic solubility by a factor of ~13 (from 41 to 530 µM). |
T481 |
330-394 |
Sentence |
denotes |
Compound 66 also showed reduced binding to mouse plasma protein. |
T482 |
395-572 |
Sentence |
denotes |
However, compared to the lead (IC50, 0.18 µM), the structural modifications caused a reduction of activity against SARS‐CoV‐2 Mpro (IC50, 2.39 µM) and enteroviral 3 C proteases. |
T483 |
573-717 |
Sentence |
denotes |
Nevertheless, the introduction of a cyclopropyl group as in 67 instead of P2‐cyclohexyl enhanced the antiviral activity against β‐coronaviruses. |