Synthesis and Antiarrhythmic Activity of N‐Substituted 1‐(2,4,6‐Trimethylphenyl)‐2‐ [N‐(2′‐hydroxy‐3′‐phenyloxypropyl)aminomethyl]pyrroles.

Abstract

pyrroles. -Among the title compounds (V), (VII), (VIII) and (IX), prepared by condensation of mesidine (II) with furfural derivative (I) followed by reductive amination and N-acylation-reduction, the lowest toxicity is observed for N-non-acylated derivative (V). It possesses antiarrhythmic activity comparable to therapeutically applied substances like propranolol or novocainamide. -(LIKHOSHERSTOV, A. M.; FILIPPOVA, O. V.; PERESADA*, V. P.; KRYZHANOVSKII, S. A.; VITITNOVA, M. B.; KAVERINA, N. V.; REZNIKOV, K. M.; Khim.-Farm. Zh. 37 (2003) 10, 8-11; Nauchno-issled. inst. farmakol. Ross. Akad. med. nauk, Moskva 125315, Russia; Russ.) -Mischke 10-114

First practical synthesis of novel 1‐phosphonylated pyrrolo[1,2‐a]pyrazine derivatives

“…Among these, compounds exhibiting a pyrrole ring sharing a C‐N bond with another heterocycles have shown a wide spectrum of biological activities . In this regard, the 1,2,3,4‐tetrahydropyrrolo[1,2‐ a ]pyrazine core is present in a great number of molecules associated with a wide variety of biological activities, such as antihypoxic, antiarrhythmic, aldose reductase inhibitors, potassium channel ligands, serotonin reuptake inhibitors, and cannabinoid receptor agonists . Particularly, the 1,2,3,4‐tetrahydropyrrolo[1,2‐ a ]pyrazine‐1‐carboxylic acid 1 and its 3‐oxo derivative 2 have been used as key intermediates in the synthesis of bradykinin 1 receptor (B1R) inhibitors and potential physiologically active agents, respectively.…”

Grinding and Microwave‐assisted Synthesis of Heterocyclic Molecules in High Yields and Their Biological Evaluation

“…In light of the preceding discussion, there is an urgent need to search new biologically active molecules which can be developed as drugs. Isoindole derivatives exhibiting antifungal , antimalarial , anticonvulsant , anti‐asthamatic , antiplasmodial , and antimicrobial and pyrrolopyrazine derivatives exhibiting anti‐arrhythmic activity are reported in literature. Isoindole and pyrrolopyrazine derivatives possessing anti‐inflammatory , anticancer , and antibacterial activities are well‐documented in literature.…”