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An increasing activity cutoff results in more selective compounds for FXa and fewer compounds that also target one of the secondary targets.
During the last five years, several groups have made continuous efforts to improve this class of compounds, designing more selective compounds or compounds with multiple capacities.
Notably, our results suggest that the modification of the N-capping region could alter the binding specificity of PACAP without altering its biological activity, thereby opening the way for the design of more selective compounds.
The identification of more selective compounds that act more NR- and tissue-specifically has the potential to circumvent these problems.
Moreover, radio/chemotherapy of EBV-positive tumors in vivo is associated with the induction of lytic replication in a significant portion of tumor cells, and more selective compounds for reactivating EBV from latency are currently evaluated [51], [52].
Improved specificity will need to be achieved through the development of more selective compounds or tissue-targeted drug delivery.
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Following the results we previously reported on a series of ethyl 2-phenylthiomethyl 5-hydroxyindole-3-carboxylate derivatives as 5-lipoxygenase (5-LOX) inhibitors, in order to obtain a more selective compound with respect to the previous generation of derivatives, we decided to modify the structure of the core ligand.
Definitely, a more precise evaluation of the structure-function relationship for both antimicrobial and antitumor activity of crotamine might allow for the discovery and proposal of potential novel mechanisms or of new structural models for the treatment of cancer and/or for the development of a more selective antimicrobial compounds that might not act on mammals host cells.
These results provide a better understanding of the molecular events involved in GLP-1 receptor pleiotropic signalling and establish the yeast platform as a robust tool to screen for more selective, efficacious compounds acting at this important class of receptors in the future.
Pyridine-containing compounds were more selective toward BChE; compounds with the para-OMe substituent in one of the two dibenzyl fragments were more selective toward CaE.
As a continuation of previous work on quinoline derivatives, which showed some preference (2 3 times) for the α7 with respect to α4β2 acetylcholine nicotinic receptors (nAChRs), we synthesized a series of novel azabicyclic or diazabicyclic compounds carrying a quinoline or isoquinoline ring, with the aim of searching for more selective α7 nAChR compounds.
More suggestions(15)
more phenolic compounds
more populated compounds
more oxygenated compounds
more complex compounds
more active compounds
more similar compounds
more volatile compounds
more interesting compounds
more aromatic compounds
more gaseous compounds
more abundant compounds
more polar compounds
more selective drugs
more bioactive compounds
more effective compounds
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