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Öğe 2,3-Dibromo-1-[4-(2,3-dibromo-4,5-dimethoxybenzyl)-2,5-dimethoxybenzyl]-4,5-dimethoxybenzene(WILEY-BLACKWELL, 2010) Şahin, Ertan; Balaydın, Halis Türker; Göksu, Süleyman; Menzek, AbdullahThe molecule of the title compound, C26H26Br4O6, is located around a crystallographic inversion center. The dihedral angle between the central benzene ring and the outer benzene ring is 89.26 (1)degrees.Öğe Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds(Taylor & Francis Inc, 2012) Balaydın, Halis Türker; Durağı, Serdar; Ekinci, Deniz; Şentürk, Murat; Göksoy, Süleyman; Menzek, AbdullahCarbonic anhydrase inhibitors (CAI) are valuable molecules as they have several therapeutic applications, including anti-glaucoma activity. In this study, inhibition of three human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and VI with a series of bisphenol and bromophenol derivatives was investigated. Molecular docking studies of a set of such inhibitors within CA I and II were also performed. K-I values of the molecules 2-9 were in the range of 10.025-892.109 mu M for hCA I, 1.437-59.107 mu M for hCA II and 11.143-919.182 mu M for hCA VI, respectively. Reported inhibitory activities of molecules 2-9 will assist in better understanding of structure-activity relationship studies of CAI.Öğe Selective O-demethylation during bromination of (3,4-dimethoxyphenyl)(2,3, 4-trimethoxyphenyl)methanone(ELSEVIER SCIENCE LTD, 2011) Çetinkaya, Yasin; Menzek, Abdullah; Şahin, Ertan; Balaydın, Halis Türker(3,4-Dimethoxyphenyl)(2,3,4-trimethoxyphenyl)methanone was synthesized and its bromination was investigated in different conditions. Nine new products (bromophenol derivatives) were isolated in the reactions. These bromophenol derivatives were obtained by selective O-demethylation in its bromination with bromine. The products and their formations were discussed.Öğe Synthesis and biological evaluation of novel bromophenol derivatives as carbonic anhydrase inhibitors(Wiley-V C H Verlag Gmbh, 2013) Akbaba, Yusuf; Balaydın, Halis Türker; Menzek, Abdullah; Göksu, Süleyman; Şahin, Ertan; Ekinci, DenizHere, we provide an alternative synthesis of the natural bromophenol 3,4-dibromo-5-(2,3-dibromo-4,5-dihydroxybenzyl)-6-(ethoxymethyl) benzene-1,2-diol (3) and the first synthesis of (4,5-dihydroxy-2methylphenyl)( 3,4-dihydroxyphenyl) methanone (18) and its brominated derivatives 19-21. The compounds were characterized and tested against the two most studied members of the pH regulatory enzyme family, carbonic anhydrase (CA). The inhibitory potencies of the novel compounds and two natural bromophenols 2, 3 were analyzed at the human isoforms hCA I and hCA II as targets and the K-I values were calculated. The K-I values of the novel compounds were measured in the range of 13.7-32.7 mu M for the hCA I isozyme and 0.65-1.26 mu M for the hCA II isozyme. The structurally related compound 14 was also tested in order to understand the structure-activity relationship, and the clinically used sulfonamide acetazolamide (AZA) was tested for comparison reasons. All of the compounds exhibited competitive inhibition with 4-nitrophenylacetate as substrate. The compounds showed strong inhibitory activity against hCA I, being more effective as compared to the clinically used AZA (K-I: 36.2 mu M), but rather less activity against hCA II.Öğe Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols and their derivatives including natural products: Vidalol B(Elsevier France-Editions Scientifiques Medicales Elsevier, 2012) Balaydın, Halis Türker; Şentürk, Murat; Göksoy, Süleyman; Menzek, AbdullahA series of bisphenol, bromophenol, and methoxyphenol derivatives (2–24) including the natural bromophenols vidalol B, 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (2) and 5,5?-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (3) were prepared. In the current study, inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, I, II, IV, and VI, with these compounds 2–24 was investigated. The compounds 2–24 were found to be promising carbonic anhydrase inhibitors, some of which showed interesting inhibitory activities. Some of the compounds investigated here showed effective hCA inhibitory activity, and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, and osteoporosis.Öğe Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products(Taylor and Francis Ltd., 2012) Balaydın, Halis Türker; Soyut, Hakan; Ekinci, Deniz; Göksu, Süleyman; Beydemir, Şükrü; Menzek, Abdullah; Şahin, Ertan(2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl) methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5-dibromo-3,4-dihydroxybenzyl) benzene-1,2-diol (3), and 5,5'-methylenebis(3,4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC50 values in the range of 0.7-372 mu M against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.Öğe Synthesis and carbonic anhydrase inhibitory properties of novel cyclohexanonyl bromophenol derivatives(Pergamon-Elsevier Science Ltd, 2012) Balaydın, Halis Türker; Şentürk, Murat; Menzek, AbdullahThe Naturally occurring novel cyclohexanonyl bromophenol 2(R)-2-(2,3,6-tribromo-4,5-dihydroxybenzyl)cyclohexanone (4) was synthesized as a racemic compound. Cyclohexylphenyl methane derivatives (10–17) with Br, OMe, CO, and OH were also obtained. Inhibition of four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II, IV, and VI, with compounds 2–4, 8, and 10–26 was investigated. These compounds were found to be promising carbonic anhydrase inhibitors and some of them showed interesting inhibitory activity. Some of the compounds investigated here showed effective hCA inhibitory activity, and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, and osteoporosis.
