6632-65-1Relevant articles and documents
Synthesis, antiamoebic and molecular docking studies of furan-thiazolidinone hybrids
Ansari, Mohammad Fawad,Siddiqui, Shadab Miyan,Ahmad, Kamal,Avecilla, Fernando,Dharavath, Sudhaker,Gourinath, Samudrala,Azam, Amir
, p. 393 - 406 (2016)
In continuation of our previous work, a series of furan-thiazolidinone hybrids was prepared by Knoevenagel condensation of 3-(furan-2-ylmethyl)-2-(phenylimino)-1, 3-thiazolidin-4-one with different aryl aldehydes in presence of strong base. Some members o
Synthesis of metronidazole based thiazolidinone analogs as promising antiamoebic agents
Ansari, Mohammad Fawad,Inam, Afreen,Ahmad, Kamal,Fatima, Shehnaz,Agarwal, Subhash M.,Azam, Amir
supporting information, (2020/10/12)
Metronidazole and its derivatives are widely used for the treatment of amoebiasis. However, metronidazole is considered as the standard drug but it has many side effects. The present study describes the synthesis of a series of metronidazole based thiazolidinone analogs via Knoevenagel condensation of 4-[2-(2-methyl-5-nitro-1H-imidazole-1-yl)ethoxy]benzaldehyde 1 with various thiazolidinone derivatives 2–14 to get the new scaffold (15–27) having better activity and lesser toxicity. Six compounds have shown better efficacy and lesser cytotoxicity than the standard drug metronidazole towards HM1: IMSS strain of Entamoeba histolytica. These compounds may combat the problem of drug resistance and might be effective in identifying potential alternatives for future drug discovery against EhOASS.
Synthesis and in vitro urease inhibitory activity of N,N′- disubstituted thioureas
Khan, Khalid Mohammed,Naz, Farzana,Taha, Muhammad,Khan, Ajmal,Perveen, Shahnaz,Choudhary,Voelter, Wolfgang
, p. 314 - 323 (2014/02/14)
Thiourea derivatives (1-38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02-91.50 ± 0.08 μM, most of which are superior to the standard thiourea (IC50 = 21.00 ± 0.11 μM). In order to ensure the mode of inhibition of these compounds, the kinetic study of the most active compounds has been carried out. Most of these inhibitors were found to be mixed-type of inhibitors, except compounds 13 and 30 which were competitive, while compound 19 was identified as non-competitive inhibitor with Ki values between 8.6 and 19.29 μM.