Portal de Periódicos da CAPES

Antimicrobial and Anti-biofilm Activity of Thiourea Derivatives Incorporating a 2-Aminothiazole Scaffold

2015; Pharmaceutical Society of Japan; Volume: 63; Issue: 3 Linguagem: Inglês

10.1248/cpb.c14-00837

1347-5223

Joanna Stefańska, Grażyna Nowicka, Marta Struga, Daniel Szulczyk, A.E. Kozioł, Ewa Augustynowicz‐Kopeć, Agnieszka Napiórkowska, Anna Bielenica, Wojciech Filipowski, Anna Filipowska, Aleksandra Drzewiecka‐Antonik, Gabriele Giliberti, Silvia Madeddu, Stefano Boi, Paolo La Colla, Giuseppina Sanna,

Click Chemistry and Applications

A series of new thiourea derivatives of 1,3-thiazole have been synthesized. All obtained compounds were tested in vitro against a number of microorganisms, including Gram-positive cocci, Gram-negative rods and Candida albicans. Compounds were also tested for their in vitro tuberculostatic activity against the Mycobacterium tuberculosis H37Rv strain, as well as two 'wild' strains isolated from tuberculosis patients. Compounds 3 and 9 showed significant inhibition against Gram-positive cocci (standard strains and hospital strain). The range of MIC values is 2–32 µg/mL. Products 3 and 9 effectively inhibited the biofilm formation of both methicillin-resistant and standard strains of S. epidermidis. The halogen atom, especially at the 3rd position of the phenyl group, is significantly important for this antimicrobial activity. Moreover, all obtained compounds resulted in cytotoxicity and antiviral activity on a large set of DNA and RNA viruses, including Human Immunodeficiency Virus type 1 (HIV-1) and other several important human pathogens. Compound 4 showed activity against HIV-1 and Coxsackievirus type B5. Seven compounds resulted in cytotoxicity against MT-4 cells (CC50<10 µM).