1310090-18-6Relevant articles and documents
4-Thiazolidinone derivatives as potent antimicrobial agents: Microwave-assisted synthesis, biological evaluation and docking studies
Pitta, Eleni,Tsolaki, Evangelia,Geronikaki, Athina,Petrovi, Jovana,Glamolija, Jasmina,Sokovi, Marina,Crespan, Emmanuele,Maga, Giovanni,Bhunia, Shome S.,Saxena, Anil K.
, p. 319 - 326 (2014)
As a part of our ongoing research in the development of new antimicrobials, herein, we report the synthesis of ten compounds which combine three bioactive moieties: thiazole, adamantane and 4-thiazolidinone. Evaluation of their antibacterial activity revealed that the newly synthesized compounds exhibited remarkable growth inhibition of a wide spectrum of Gram-positive bacteria, Gram-negative bacteria and fungi. The majority of the compounds displayed greater antibacterial activity than the reference drugs (ampicillin and streptomycin), while the antifungal activity was significantly higher than that of the reference drugs bifonazole and ketoconazole. Additionally, the title compounds were screened for HIV-1 reverse transcriptase inhibitory activity, showing no significant activity. Moreover, docking studies were performed in order to explore possible binding modes at the MurB protein of S. aureus. This journal is
Novel thiazolidinone derivatives with an uncommon mechanism of inhibition towards HIV-1 reverse transcriptase
Pitta, Eleni,Crespan, Emmanuele,Geronikaki, Athina,Giovanni, Maga,Samuele, Alberta
experimental part, p. 228 - 234 (2011/02/25)
Here, we show that novel 2-aryl-3-(4-adamantyl-thiazol-21,3-thiazolidin-4- one derivatives have a mixed- or fully competitive mechanism of inhibition towards HIV-1 Reverse Transcriptase with respect to the substrates of the reaction. Thus, they are interesting starting points for the development of novel NNRTIs with an uncommon mechanism of action.