In vitro Antioxidant Properties of Novel ?3-Adrenoceptor Agonists Bearing Benzenesulfonamide Fragment

Abstract

As an extension of our research, the in vitro antioxidant efficiency of perspective agonists of ?3-adrenoceptors structurally based on the aryloxypropanolamine pharmacophore, chemically 3-{4- [(alkoxycarbonyl)amino]phenoxy}-N-{2-[4-(aminosulfonyl)phenyl]ethyl}-2-hydroxypropan-1-ammonium chlorides, was investigated. The potential of evaluated compounds to reduce relatively stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals in the spectrophotometric tests was dependent on the length of the alkyl substituent of alkoxycarbonylamino moiety directly attached to phenyl ring. The elongation of given string was accompanied by the increase in the effectiveness. From the entire analyzed set, the compound containing butoxycarbonylamino group has been able to act most markedly as the reduction agent towards the DPPH radicals showing the percentage of the DPPH reduction (% DPPH) of 11.34±0.02. On the other hand, the tested derivative has shown approximately ninefold decrease in the efficiency compared to applied Trolox standard, a water-soluble analogue of vitamin E, with its %DPPH=95.45±0.02. Dhaka Univ. J. Pharm. Sci. 12(1): 23-28, 2013 (June) DOI: http://dx.doi.org/10.3329/dujps.v12i1.16296

The Forty-Sixth Euro Congress on Drug Synthesis and Analysis: Snapshot †

“…The β3-adrenergic receptor is a frequently investigated target for pharmaceutical chemists and the derivatives of β3-adrenergic receptor agonists are being developed for their antioxidant, antimicrobial and other actions. A doctoral thesis on the synthesis and analysis of derivatives with potential action on β3-adrenergic receptors performed at the Department of Pharmaceutical Chemistry, Faculty of Pharmacy of the Comenius University in Bratislava [ 163 , 164 ] has motivated our research group to focus on the potential role of β3-adrenergic receptors in the stress response. In spite of the fact that catecholamines belong to the main stress hormones and they are acting via adrenergic receptors, no information has been available on possible changes of the β3-adrenergic receptors under stress conditions.…”