Synthesis and antiarrhythmic activity of new benzofuran derivatives

Abstract

Various 5-aminobenzofuran derivatives were prepared from khellin and screened intravenously in the dog for their potential antiarrhythmic activity against ouabain-induced ventricular arrhythmia and in the Harris test. From systematic structural variations it was found that two methoxy groups in positions 4 and 7 on the benzofuran ring, a tertiary aminoethoxy side chain in position 6, and a N-methylurea group in position 5 led to the most active compounds. These were then tested orally in the Harris test in the dog. The two long-acting derivatives N-[4,7-dimethoxy-6-(2-pyrrolidinoethoxy)-5-benzofuranyl]-N'-methylurea (8j) and N-[4,7-dimethoxy-6-(2-piperidinoethoxy)-5-benzofuranyl]-N'-methylurea (8m) showed advantages when compared to quinidine and disopyramide and have been selected for further studies.

Synthesis and antimicrobial activities of some (E)-N'-1-(substituted benzylidene)benzohydrazides

“…Some benzohydrazides derivatives were known to have a wide variety of pharmacological actions such as antimicrobial (Kirilimi et al 2008), antiarrhythmic (Bourgery et al 1981) and antitumor (Galal et al 2009). Many of the benzohydrazides are both natural and synthetic were known to exhibit various biological activities including antimalarial (Li et al 1995), antiinflammatory (Ballesteros et al 2010), antioxidant (Anto et al 1995;Mukerjee et al 2001), antileishmanial (Nielsen et al 1998), antifungal (Nielsen et al 1998) and antibacterial (Osorio et al 2012) activities.…”

Screening of benzofuran compound 3-acetamido-2-p-anisoyl benzofuran for anti-inflammatory activity in acute models of inflammation

“…Benzofuran derivatives have broad spectrum pharmacological activities like antibacterial, antifungal, antidepressant, and antiarrhythmic and anti-inflammatory properties. [1][2][3][4][5] Inflammation is a defensive response of body against the harmful stimuli. This is intended to remove the injury causing stimuli and initiate the process of repair.…”

Green and One-Pot Electrochemical Synthesis of New Benzofurans Based on an ECC Mechanism

“…The most recognised of the benzofurans are amiodarone, angelicin xanthotoxin, bergapten, nodekenetin and usnic acid compounds [4]. The benzofuran ring system is the basic skeleton of numerous compounds possessing cardiovascular activity [5].…”