2014), tiazofurin (antineoplastic) (Popsavin et al. 2014), bleomycin (anticancer) (Rahmutulla et al. 2012), penicillin derivatives (antibacterial) (Ye et al. Moreover, the 1,3-thiazole scaffold is commonly utilized in drug development, and found in many commercially available drugs, including tenonitrozole (an antiparasitic) (Cohen et al. 2013), antiarthritic (Nishikaku and Koga 1993), neuroprotective (Zhang et al. 2014), antipsychotropic (Zablotskaya et al. 2013), antioxidant (Shih and Ying 2004), antitubercular (Romagnoli et al. Thiazole analogues have continued to attract interest in medicinal chemistry field during the past decades due to their wide ranging biological activities, which include antibacterial (Alam et al. The thiazole scaffold is found in a variety of natural bioactive compounds used as pharmaceuticals and agrochemicals. Thiazoles and their derivatives are an important class of five-member heterocyclic compounds, and contain sulfur and nitrogen at positions 1 and 3 of the thiazole ring, respectively. Molecules possessing the small and ostensibly simple 1,3-thiazole heterocyclic substructure often have surprisingly complex biological properties.
coli FabH receptor, an attractive target for the development of new antibacterial agents, showed it has good binding properties. In addition, a docking study of compound 3i into the active site of E. In silico drug-likeness, pharmacokinetic (ADME) properties, toxicity effects, and drug scores were also evaluated, and none of the sixteen compounds were found to violate Lipiniski’s rule of five or Veber’s rule, indicating potential for development as oral drug candidates.
Compound 3g showed highest antibacterial activity against E. sakazakii with MIC values ranging from 50 to 100 μg mL −1.
salina, whereas compound 3i exhibited the most potent antibacterial activities against L. Of the tested compounds, 3g demonstrated highest cytotoxicity with a LC 50 value of 54 ppm followed by compound 3h (LC 50 = 85 ppm), in a short-term bioassay using A. A series of sixteen 2-arylidenehydrazinyl-4-arylthiazole analogues ( 3a– p) were evaluated for cytotoxic activity against brine shrimp ( Artemia salina) nauplii and their minimum inhibitory concentrations were determined against two Gram-positive ( Listeria monocytogenes and Enterococcus faecalis) and two Gram-negative bacterial strains ( C. Thiazoles are an important class of heterocyclic compounds that possess a sulfur and nitrogen containing five-membered ring, which acts as a pharmacophore, and show a wide range of complex biological activities.
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