Metal‐Based Compounds as Prospective Antileishmanial Agents: Inhibition of Trypanothione Reductase by Selected Gold Complexes

• DOI: 10.1002/cmdc.201300276
• Publication Date: 2013-08-23T10:57:33Z
• Authors: Gianni Colotti; Andrea Ilari; Annarita Fiorillo; Paola Baiocco; Maria Agostina Ci...; Laura Maiore; Federica Scaletti; Chiara Gabbiani; Luigi Messori
• Keywords: Leishmania; 0301 basic medicine; Gold Compounds; antiprotozoal agents; Leishmania; Trypanothione reductase; Antiprotozoal Agents; gold drugs; anti-Leishmania agents; tripanothione reductase; trypanothione reductase; gold; Crystallography, X-Ray; 3. Good health; Molecular Docking Simulation; Kinetics; 03 medical and health sciences; Coordination Complexes; Antiprotozoal agents; Gold; Inhibitors; Leishmania; Trypanothione reductase; Antiprotozoal Agents; Catalytic Domain; Coordination Complexes; Crystallography, X-Ray; Enzyme Inhibitors; Gold; Kinetics; Leishmania; Molecular Docking Simulation; NADH, NADPH Oxidoreductases; Protein Binding; Molecular Medicine; Pharmacology, Toxicology and Pharmaceutics (all); Organic Chemistry; Catalytic Domain; inhibitors; [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology; [SDV.MP.PAR]Life Sciences [q-bio]/Microbiology and Parasitology/Parasitology; NADH, NADPH Oxidoreductases; Gold; Enzyme Inhibitors; antiprotozoal agents; Protein Binding

Picking a fight with parasites! Trypanothione reductase (TR) is a validated drug target for the development of antileishmanial agents. A group of structurally diverse gold-containing compounds was evaluated in vitro for TR inhibition. A number of compounds exhibited potent activity and deserve further pharmacological evaluation.