Key result
Compound 16 demonstrates ~3-fold greater antiplatelet potency than picotamide against ADP.
Why the study?
The study aimed to design and evaluate new 4-ethoxyisophthalamide compounds for antiplatelet activity using in vitro models due to the need for more effective agents.
Novel 4-ethoxyisophthalamide derivatives, particularly compound 16, demonstrate potent in vitro antiplatelet activity superior to picotamide.
Answers are grounded in this paper and cite their sources.
New 4-ethoxyisophthalamide analogs show in vitro activity; leaves open any clinical role pending in vivo and human studies.
With the help of spatial quantitative structure‐activity relationships (QSAR) contour maps obtained by comparative molecular field analysis (CoMFA), a series of 4‐ethoxyisophthalamide compounds were prepared and some of them with higher activity were found. This paper continues the structural design, preparation, spectral confirmation of thirteen new 4‐ethoxyisophthalamide compounds and completes their preliminary screening of activity in response to the following inducers: adenosine diphosphate (ADP) and collagen. Among them, when ADP was used as an inducer, compounds whose activities are higher or close to picotamide, the IC 50 value also were calculated and revealed that one compound 16 (IC 50 : 0.26 μmol L −1 ) was more than three times more active than positive control drug picotamide. Meanwhile, cytotoxic effects in vitro of compound 11* and compound 16 on L929 cells were analyzed. The structure‐activity relationship showed that when electron‐withdrawing groups nitro or trifluoromethyl are introduced at the meta ‐ or para ‐ position of the two side chain benzene rings, it is beneficial on the whole to the improvement of antiplatelet activity.
No takes yet. Share an insight, caveat, or question.
Zhang et al. (2020) studied this question. 4-ethoxyisophthalamide compounds (e.g., compound 16) vs. picotamide was evaluated on Antiplatelet activity (IC50) in response to ADP. Compound 16 demonstrated an IC50 of 0.26 μmol/L for antiplatelet activity in response to ADP, which was more than three times more active than the positive control drug picotamide.
Synapse has enriched 10 related papers. Consider them for comparative context: