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Design and Synthesis of Sulfonamidophenylethylamides as Novel Cardiac Myosin Activator

Design and Synthesis of Sulfonamidophenylethylamides as Novel Cardiac Myosin Activator

Manoj Manickam, Thanigaimalai Pillaiyar, Vigneshwaran Namasivayam, Pulla Reddy Boggu, Niti Sharma, Hitesh B Jalani, Eeda Venkateswararao, You-Jung Lee, Eun-Seok Jeon, Min-Jeong Son, Sun-Hee Woo, Sang-Hun Jung

Bioorg Med Chem. 2019 Sep 15;27(18):4110-4123.

PMID: 31378598

Abstract:

The sulfonamidophenylethylamide analogues were explored for finding novel and potent cardiac myosin activators. Among them, N-(4-(N,N-dimethylsulfamoyl)phenethyl-N-methyl-5-phenylpentanamide (13, CMA at 10 µM = 48.5%; FS = 26.21%; EF = 15.28%) and its isomer, 4-(4-(N,N-dimethylsulfamoyl)phenyl-N-methyl-N-(3-phenylpropyl)butanamide (27, CMA at 10 µM = 55.0%; FS = 24.69%; EF = 14.08%) proved to be efficient cardiac myosin activators both in in vitro and in vivo studies. Compounds 13 (88.2 + 3.1% at 5 µM) and 27 (46.5 + 2.8% at 5 µM) showed positive inotropic effect in isolated rat ventricular myocytes. The potent compounds 13 and 27 were highly selective for cardiac myosin over skeletal and smooth muscle myosin, and therefore these potent and selective amide derivatives could be considered a new class of cardiac myosin activators for the treatment of systolic heart failure.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP139332642	4-(N,N-Dimethylsulfamoyl)-7-piperazino-benzofurazan		139332-64-2	Price

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