3770-50-1. Name is Ethyl indole-2-carboxylate, belongs to indole-building-block compound, is a common compound. In an article, authors is Atwal, Karnail S., once mentioned the new application about 3770-50-1.
Cardioselective Anti-Ischemic ATP-Sensitive Potassium Channel Openers. 3. Structure-Activity Studies on Benzopyranyl Cyanoguanidines: Modification of the Cyanoguanidine Portion
Structure-activity relationships for the cyanoguanidine portion of the lead cardiac selective ATP-sensitive potassium channel (KATP) opener (3) are described.The cyanoguanidine moiety appears to be optimal since increasing or decreasing the distance between the aniline nitrogen and the pedant aromatic ring attenuates anti-ischemic potency/selectivity.Similarly, unfavorable results are obtained by replacement of the aniline nitrogen with other linkers (CH2, S, O).Replacement of the phenyl ring with a methyl group diminishes cardiac selectivity.Constraining the urea moiety into a benzimidazolone or imidazolone ring retains anti-ischemic potency with significant improvement the cardiac selectivity.As shown by the ratio of vasorelaxant and anti-ischemic potencies, the cardiac selectivity in vitro varies over 3 orders of magnitude.These data are in agreement with previous results indicating that distinct structure-activity relationships exist for the anti-ischemic and vasorelaxant activities.Since the anti-ischemic effects of this series of compounds are abolished by pretratment with structurally different KATP blockers (glyburide, sodium 5-hydroxydecanoate, meclofenamic acid), the mechanism for the anti-ischemic actions of these compounds still appears to involve the opening of KATP.
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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles