| Id |
Subject |
Object |
Predicate |
Lexical cue |
| T161 |
0-110 |
Sentence |
denotes |
Table 4 summarizes this effort where two of the optimal P2 residues (Leu and β-tert-butyl-Ala) were conserved. |
| T162 |
111-368 |
Sentence |
denotes |
Removal of the methoxy group from the indole generally led to slightly weaker potency in both the enzymatic and antiviral assays across pairs (43 vs 36, 44 vs 37, 50 vs 48 and 49 vs 4) and therefore no improvement in the antiviral/protease inhibition ratio. |
| T163 |
369-480 |
Sentence |
denotes |
The impact of more significant changes to the P3 cap is illustrated by tetrahydrofuranyl derivatives 46 and 47. |
| T164 |
481-655 |
Sentence |
denotes |
These derivatives lack the lipophilic aryl ring and NH hydrogen bond donor present in the indole P3 cap and exhibit a pronounced reduction in enzymatic and antiviral potency. |
| T165 |
656-819 |
Sentence |
denotes |
A noteworthy reduction in biochemical and antiviral potency was observed in comparing each hydroxymethylketone derivative with its corresponding ether counterpart. |
| T166 |
820-993 |
Sentence |
denotes |
These results suggest that modest structural and physicochemical alterations of 4 fail to significantly decrease the high EC50/IC50 ratios for this class of peptidomimetics. |
| T167 |
994-1301 |
Sentence |
denotes |
However, in vitro analysis of 4 revealed this derivative to possess high levels of metabolic stability in human liver microsomes (t1/2 = 107 min).45 Further evaluation of this breakthrough derivative in several aqueous-based formulations suitable for IV administration indicated high levels of solubility.46 |
