Thiadiazolidinones: Antimicrobial Activity against MRSA

Thiadiazolidinones: Antimicrobial Activity against MRSA

Postby PharmD » Wed Mar 21, 2012 3:43 pm

Thiadiazolidinones = new class of alanine racemase inhibitors; antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA). Targets S. aureus cell wall synthesis enzyme, alanine racemase (Alr); novel enzyme inhibitors (inhibit bacterial growth). Thiadiazolidones inhibited Alr activity with 50% inhibitory concentrations (IC₅₀) ranging from 0.36 to 6.4 μM, and they appear to inhibit the enzyme irreversibly. The series inhibited the growth of S. aureus, including MRSA strains, with minimal inhibitory concentrations (MICs) ranging from 6.25 to 100 μg/ml. The antimicrobial activity showed selectivity against Gram-positive bacteria and fungi, but not Gram-negative bacteria. The series inhibited human HeLa cell proliferation.

Adapted from: Biochem Pharmacol. 2012; 83(3):368-77, Ciustea M; Mootien S; Rosato AE; Perez O; Cirillo P; Yeung KR; Ledizet M; Cynamon MH; Aristoff PA; Koski RA; Kaplan PA; Anthony KG et. al.
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