Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products

Balaydın, Halis Türker; Söyüt, Hakan; Ekinci, Deniz; Göksu, Süleyman; Beydemır, Şükrü; Menzek, Abdullah; Şahin, Ertan

doi:10.3109/14756366.2011.574131

Cited by 40 publications

(28 citation statements)

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“…It has been reported that naturally occurring bromophenol 1 shows enzyme inhibition 3 , cytotoxicity 4 , feeding deterrent 5 , anti-microbial 6 , anti-cancer 7 and anti-oxidant 8 activities. Aldose reductase 9 and carbonic anhydrase 10 inhibitory properties of natural products 2-3 have also been noted ( Figure 1). The high-density lipoprotein associated serum esterase, paraoxonase (arylesterase, EC 3.1.8.1, PON1) is a key enzyme for protection against atherosclerosis in metabolism.…”

Section: Introductionmentioning

confidence: 93%

Synthesis and paroxonase activities of novel bromophenols

Akbaba

Türkeş

Polat

et al. 2012

Journal of Enzyme Inhibition and Medicinal Chemistry

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Section: Introductionmentioning

confidence: 93%

Synthesis and paroxonase activities of novel bromophenols

Akbaba

Türkeş

Polat

et al. 2012

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…These compounds showed a good inhibition activity (K i of 10.2, 7.41, and 36 mM, respectively) ( Table 1) 3, [22][23][24][25] . In this study, the inhibition effect of the synthesized compound 9 was less than that of the compounds 1 and 2.…”

Section: Resultsmentioning

confidence: 99%

Synthesis of two phloroglucinol derivatives with cinnamyl moieties as inhibitors of the carbonic anhydrase isozymes I and II: anin vitrostudy

Burmaoğlu

Dilek

Yılmaz

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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Two cinnamyl-substituted phloroglucinols, 4-p-methoxycinnamyl phloroglucinol (9) and 4,6-bis-p-methoxycinnamyl phloroglucinol (10) were synthesized. Two carbonic anhydrases, human carbonic anhydrase I and II (hCA I and II), were purified. Kinetic interactions between these isozymes with 9 and 10 were investigated. These new compounds exhibited inhibitory effects on the hCA I and II enzymes' activity in vitro. The combination of the inhibitory effects of both phloroglucinol and p-coumaric acid groups in a single compound was explored. However, relative to the inhibitory effects of the two groups separately, compounds 9 and 10 demonstrated comparable inhibitory effects. More effective inhibitors of CAs could be created by testing these compounds on other CA isozymes.

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“…For instance, inhibition and activation effects of various drugs on the activities of different enzymes have been studied in our laboratory up to now. [30][31][32][33][34][35][36][37][38][39] Considering the above mentioned information, we aimed in the present study to purify PON1 from human serum and to investigate the kinetic interactions between the enzyme and some antibiotic drugs, namely oxytetracycline hydrochloride, netilmycin sulfate, lincomycin hydrochloride, clindamycin phosphate, streptomycin sulfate. To this end, hPON1 was purified using simple methods.…”

Section: Discussionmentioning

confidence: 99%