Published January 1, 2017 | Version v1
Journal article Open

Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors

  • 1. Istanbul Medeniyet Univ, Dept Chem, Fac Sci, TR-34730 Istanbul, Turkey
  • 2. Artvin Coruh Univ, Vocat Sch Hlth Serv, Pharm Serv Program, TR-08000 Artvin, Turkey
  • 3. Sinop Univ, Dept Bioengn, Fac Engn & Architecture, TR-57000 Sinop, Turkey
  • 4. Mus Alparslan Univ, Fac Sci & Arts, Dept Mol Biol & Genet, TR-49250 Mus, Turkey
  • 5. Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkey
  • 6. TUBITAK UME, Chem Grp Labs, POB 54, TR-41470 Gebze, Turkey

Description

Secondary sulfonamides (4a-8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a peroxidase enzyme secreted from salivary, mammary, and other mucosal glands. In the present study, the in vitro inhibitory effects of some secondary sulfonamide derivatives (4a-8h) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (4a-8h) are effective LPO inhibitors. The K-i values of secondary sulfonamide derivatives (4a-8h) were found in the range of 1.096 x 10(-3) to 1203.83 mu M against LPO. However, the most effective inhibition was found for N-(sulfathiazole)-3,4,5-triacetoxybenzamide (6a), with K-i values of 1.096 x 10(-3) +/- 0.471 x 10(-3) mu M as non-competitive inhibition.

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