title: Antimicrobial and anti-biofilm activity of thiourea derivatives incorporating a 2-aminothiazole scaffold.
abstract: 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).
authors.affiliation: Department of Pharmaceutical Microbiology, Medical University.
authors.forename: Joanna
authors.initials: J
authors.lastname: Stefanska
authors.forename: Grażyna
authors.initials: G
authors.lastname: Nowicka
authors.forename: Marta
authors.initials: M
authors.lastname: Struga
authors.forename: Daniel
authors.initials: D
authors.lastname: Szulczyk
authors.forename: Anna Eugenia
authors.initials: AE
authors.lastname: Koziol
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopec
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiorkowska
authors.forename: Anna
authors.initials: A
authors.lastname: Bielenica
authors.forename: Wojciech
authors.initials: W
authors.lastname: Filipowski
authors.forename: Anna
authors.initials: A
authors.lastname: Filipowska
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Drzewiecka
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.forename: Silvia
authors.initials: S
authors.lastname: Madeddu
authors.forename: Stefano
authors.initials: S
authors.lastname: Boi
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology; D018441:Biofilms / Q000187:drug effects* / Q000254:growth & development; D002417:Cattle; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000379:methods; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology; D013890:Thiourea / Q000737:chemistry* / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000890:Anti-Infective Agents; D013844:Thiazoles; C004483:2-aminothiazole; D013890:Thiourea