4-benzoil-1,5-difenil-N-(5-sülfamoil-1,3,4-tiyadiazol-2-il)-1H-pirazol-3-karboksamid`in bazı geçiş metalleriyle yeni kompleklerinin sentezi, karakterizasyonu ve biyolojik aktivitesinin incelenmesi

Abstract

Aromatik sulfonamidler karbonik anhidraz enzirninin inhibitorleri olarak olduk9a iyi bilinmektedirler. Ayni zamanda sulfonamidlerin metal kompleksleri de karbonik anhidrazin inhibitorleridir. Karbonik anhidraz inhibitorleri, glokomun tedavisinde goz i^i basincini (IOP) dusiirmekte kullanihrlar.Bu 9ahsmada 4-Benzoil-l ^-difenil-^S-siilfamoil-l ,3,4-tiyadiazol-2-il)-l//-pirazol-3-karboksamit'in Co(II), Ni(II), Cu(II), Zn(II) komplekslerinin sentezi ama9lanmistir. Sentezlenen bilesiklerin yapilari IR, 'H-NMR ve 13C-NMR spektroskopileri, X-isini difraksiyonu ve elementel analiz yontemleri kullanilarak aydinlatilmaya 9ahsilmistir. Sentezlenen komplekslerin, insan eritrosit karbonik anhidraz enzimleri (CA-I ve CA-II) iizerinde inhibisyon etkileri, pH-stat ve LTV spektroskopisi yontemleri ile incelenmistir.Anahtar Kelimeler: Glokom, inhibisyon, Karbonik anhidraz, metal kompleksleri, pirazol karboksilik asit riirevleri.

Aromatic sulfonamides are well known as inhibitors of the carbonic anhydrase enzyme.The metal complexes of sulfonamides are also potent inhibitors of the carbonic anhydrase. Carbonic anhydrase inhibitors, which reduce aqueous production with a corresponding decrease in intraocular pressure (IOP), have been used as ocular hypotensive agents for the treatment of glaucoma.In this study the syntheses of Co(II), Ni(II), Cu(II), Zn(II) complexes of the 4-Benzoyl-1,5-diphenyl-./V-(5 -sulfamoyl-1,3,4-thiadiazol-2-yl)-1 /f-pyrazole-3 -carboxamide were aimed. The structures of synthesized compounds were elucidated by using IR, 'H-NMR and 13C-NMR spectroscopies, X-ray diffraction method and elementel analysis. The inhibitory effect of synthesized compounds were experimented on human erythrocyte carbonic anhydrase (CA-I ve CA-II) by using pH-stat and UV spectroscopy methods.Keywords: Carbonic Anhydrase, glaucoma, inhibition, metal complexes, pyrazole carboxilic acid derivatives.