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

作者：Stefanska Joanna; Nowicka Grazyna; Struga Marta^*; Szulczyk Daniel; Koziol Anna Eugenia; Augustynowicz Kopec Ewa; Napiorkowska Agnieszka; Bielenica Anna; Filipowski Wojciech; Filipowska Anna; Drzewiecka Aleksandra; Giliberti Gabriele; Madeddu Silvia; Boi Stefano; La Colla Paolo; Sanna Giuseppina

来源：CHEMICAL & PHARMACEUTICAL BULLETIN, 2015, 63(3): 225-236.

DOI：10.1248/cpb.c14-00837

• antimicrobial activity
• antibiofilm activity
• antiviral activity
• 2-aminothiazole

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 H(37)Rv 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 mu g/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 mu M).

• 出版日期2015-3