TY - JOUR
T1 - Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance
AU - Cascioferro, Stella
AU - Parrino, Barbara
AU - Carbone, Daniela
AU - Schillaci, Domenico
AU - Giovannetti, Elisa
AU - Cirrincione, Girolamo
AU - Diana, Patrizia
PY - 2020/8/13
Y1 - 2020/8/13
N2 - Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical application of thiazole and its benzofused derivatives, which act as inhibitors of mechanisms underlying antibiotic resistance in the treatment of severe drug-resistant infections. In addition, we examined all bacterial targets involved in their antimicrobial activity reporting, when described, their spontaneous frequencies of resistance.
AB - Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical application of thiazole and its benzofused derivatives, which act as inhibitors of mechanisms underlying antibiotic resistance in the treatment of severe drug-resistant infections. In addition, we examined all bacterial targets involved in their antimicrobial activity reporting, when described, their spontaneous frequencies of resistance.
UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85088653137&origin=inward
UR - https://www.ncbi.nlm.nih.gov/pubmed/32208685
U2 - https://doi.org/10.1021/acs.jmedchem.9b01245
DO - https://doi.org/10.1021/acs.jmedchem.9b01245
M3 - Review article
C2 - 32208685
SN - 0022-2623
VL - 63
SP - 7923
EP - 7956
JO - Journal of medicinal chemistry
JF - Journal of medicinal chemistry
IS - 15
ER -