50625-53-1Relevant academic research and scientific papers
Synthesis and paroxonase activities of novel bromophenols
Akbaba, Yusuf,Tuerkes, Cueneyt,Polat, Leyla,Soeyuet, Hakan,Sahin, Ertan,Menzek, Abdullah,Goeksu, Sueleyman,Beydemir, Suekrue
, p. 1073 - 1079 (2013)
Three novel bromophenols 10-12 were synthesized. Acylation of veratrole (4) with 2,3-dimethoxy benzoic acid (5) gave a kown diarylmethanone 6. Bromination of 6 with different equivalents of molecular bromine afforded new di and tribrominated compounds 7-9 which were converted to their corresponding bromophenols 10-12 via O-demethylation with BBr3. Paraoxonase-1 (PON1) was purified from human serum with approximately 42% and 3584 U × mg -1 specific activity. The synthesized compounds 6-12 showed inhibitory effects on paraoxonase-1 (PON1) which is an organophosphate (OP) hydrolyser and an antioxidant bioscavenger enzyme. IC50 values were determined in the range of 0.123-1.212 mM. Graphical abstract
Synthesis and carbonic anhydrase isoenzymes i and II inhibitory effects of novel benzylamine derivatives
?etinkaya, Yasin,G??er, Hülya,G?ksu, Süleyman,Gül?in, Ilhami
, p. 168 - 174 (2014/04/03)
Synthesis and carbonic anhydrase inhibitory properties of novel diarylmethylamines 22-25 and sulfonamide derivatives 26-28 were investigated. Acylation of methoxy-substituted benzenes with benzene carboxylic acids, reduction of ketones with NaBH4, conversion of alcohols to azides, Pd-C catalyzed hydrogenation of azides afforded title compounds 22-25. Compounds 22, 24 and 25 were converted to sulfonamide derivatives 26-28 with MeSO2Cl. The inhibitory effects of novel benzylamine derivatives 22-28 were tested on human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes hCA I and II. The results demonstrated that compound 28 was found to be the best inhibitor against both hCA I (Ki: 3.68 μM) and hCA II (Ki: 9.23 μM).
