Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex

Synthesis and characterization of a proton transfer salt between 2,6-pyridinedicarboxylic acid and 2-aminobenzothiazole, and its complexes and their inhibition studies on carbonic anhydrase isoenzymes

“…While ABT and H 2 dipic do not show any inhibition effects on hCA I and hCA II, the proton transfer salt has considerable inhibition effect due to the structural changes leading to impressive differences of activity 24,26,66 . Similarly, compounds 2-5 have more potent effects than all simple metal complexes and compound 1 with nearly three times better inhibition (IC 50 values 0.241-0.299 mM for hCA I and 0.221-0.281 mM for hCA II) ( Table 5) 24, 26,66 . The inhibition potentials of 2-5 are close to each other; in addition, complex 2 has the most effective inhibition potential among all the newly synthesized compounds (IC 50 values 0.241 mM for hCA I and 0.221 mM for hCA II).…”

“…The metal complexes with mixed ligands of these compounds have shown better biological activities than the simple ones [19][20][21][22] . Two types of ligands, generally acids and bases, are brought together before coordination with the metal ion in order to prepare the mixed ligand complex compounds [23][24][25][26] . Pyridine-2,6-dicarboxylic acid (or dipicolinic acid) (H 2 dipic) forms stable chelates with simple metal ions and oxometal cations and can display a widely varying coordination behavior, functioning as a multidentate ligand.…”

Synthesis and characterization of complexes of a novel proton transfer salt and their inhibition studies on carbonic anhydrase isoenzymes

“…While H 2 DPC does not show any inhibition effects on hCA I and hCA II, the proton transfer salt (1) has inhibition effect due to structural changes leading to impressive differences of activity 20,21,44 . In addition, the salt has more effective inhibition effect than ClABT (IC 50 value of 1 for hCA I ¼ 0.76 ± 0.002 mM, for hCA II ¼ 0.82 ± 0.006 mM, IC 50 value of ClABT for hCA I ¼ 0.85 ± 0.02 mM, for hCA II ¼ 0.74 ± 0.007 mM).…”

“…The mixed ligand metal complexes of these compounds have shown better biological activities than the simple ones 4,18,19 . In order to prepare the mixed ligand complexes, two types of ligands, generally acids and bases, are brought together before coordination to the metal ion 1,6,20,21 .…”

Synthesis and characterization of some metal complexes of a proton transfer salt, and their inhibition studies on carbonic anhydrase isozymes and the evaluation of the results by statistical analysis

“…The mixed ligand metal complexes of these compounds have shown better biological activities than the simple ones [2][3][4] . In order to prepare the mixed ligand complexes, two types of ligands, generally acids and bases, are brought together before coordination to the metal ion [1][2][3][4][5]16,17 . In this study, a novel proton transfer compound (HMeOABT) Furthermore, we have investigated the potential use of these compounds as new inhibitors of human carbonic anhydrase (hCA I and hCA II) isozymes in the treatment of glaucoma, which is a group of diseases characterized by the gradual loss of visual field due to an elevation in intraocular pressure (IOP) 18,19 .…”