The voltage-gated potassium channel Kv1.5, which mediates the cardiac ultra-rapid delayed-rectifier (IKur) current in human cells, has a crucial role in atrial fibrillation. Therefore, the design of selective Kv1.5 modulators is essential for the treatment of pathophysiological conditions involving Kv1.5 activity. This review summarizes the progress of molecular structures and the functionality of different types of Kv1.5 modulators, with a focus on clinical cardiovascular drugs and a number of active natural products, through a summarization of 96 compounds currently widely used. Furthermore, we also discuss the contributions of Kv1.5 and the regulation of the structure-activity relationship (SAR) of synthetic Kv1.5 inhibitors in human pathophysiology. SAR analysis is regarded as a useful strategy in structural elucidation, as it relates to the characteristics that improve compounds targeting Kv1.5. Herein, we present previous studies regarding the structural, pharmacological, and SAR information of the Kv1.5 modulator, through which we can assist in identifying and designing potent and specific Kv1.5 inhibitors in the treatment of diseases involving Kv1.5 activity.

/pdf/challenges-faced-with-small-molecular-modulators-of-14p3tkyxnn.pdf

Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.

Optimization of substituted cinnamic acyl sulfonamide derivatives as tubulin polymerization inhibitors with anticancer activity.

The crystal structures of six adamantane derivatives of sulfonamides have been determined by X-ray diffraction. The molecular conformational states, packing architecture, and hydrogen bond networks were analyzed. The conformational flexibility of the bridge connecting the phenyl ring and the adamantane fragment was studied. The molecular packing architectures of the selected crystals can be for convenience divided into three different groups. The thermodynamic aspects of the sublimation processes of the compounds were studied by determining the temperature dependence of vapor pressure using the transpiration method. The thermophysical characteristics of the fusion processes of the molecular crystals were measured and analyzed. Correlations between the sublimation thermodynamic functions and physico-chemical descriptors were revealed. A regression equation correlating the sublimation Gibbs energies with the van der Waals molecular volumes was derived. The influence of various molecular fragments on the crystal lattice energy was analyzed. The relationship between the melting points of the studied substances and the free volume per molecule in the crystal lattices was evaluated.

Adamantane derivatives of sulfonamide molecular crystals: structure, sublimation thermodynamic characteristics, molecular packing, and hydrogen bond networks

Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents

Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

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Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel