Novel 2-arylthiazolidin-4-one-thiazole hybrids with potent activity against Mycobacterium tuberculosis

An Overview of the Structure–Activity Relationship in Novel Antimicrobial Thiazoles Clubbed with Various Heterocycles (2017–2023)

“…Othman et al designed a series of novel 2-(thiazol-2-yl)- N -thiazolidin-4-ones, variably substituted in the second position of the thiazolidin-4-one ring ( Figure 26 ) [ 41 ].…”

“…Three compounds ( 133 , 135 , and 137 ) showed activity against the MDR strain (MICs = 1.95–7.81 µg/mL), and one ( 135 ) showed activity against the XDR strain (MIC = 7.81 µg/mL). Concerning antibacterial activity, all five compounds showed similar activity (MICs = 0.48–7.81 µg/mL) against Mycoplasma pneumoniae ATCC 15531, S. pneumoniae ATCC 1659, and K. pneumoniae ATCC 43816, while four compounds ( 133 and 135 – 137 ) showed similar activity against Bordetella pertussis ATCC 9340 (MICs = 1.95–7.81 µg/mL), compared to azithromycin (MICs = 0.49–7.81 µg/mL) [ 41 ].…”

“…Mono-substitution ( 133 , 134 , and 136 ) was associated with MDR antituberculosis activity. Supplementarily, the presence of a voluminous halogen in the fourth position ( 135 ) was associated with XDR antituberculosis activity, most likely due to increased molecular lipophilicity ( Figure 26 ) [ 41 ].…”

“…Concerning the activity against bronchitis-causing bacteria, SAR studies showed that the best antibacterial activity was associated with the grafting of methoxy groups in the meta position ( 134 and 136 ) ( Figure 26 ) [ 41 ].…”

Synthesis, antimycobacterial, cytotoxicity, anti‐inflammatory, in silico studies and molecular dynamics of pyrazole‐embedded thiazolidin‐4‐one hybrids

“…Sharma et al [ 23 ] reported the thiazolidin‐4‐one molecules targeting to the DevR/DosR dormancy regulator. Othman et al [ 24 ] reported some 2‐arylthiazolidin‐4‐one clubbed with thiazole hybrids as antimycobacerial agents.…”