22927-54-4Relevant academic research and scientific papers
Silica-tethered cuprous acetophenone thiosemicarbazone (STCATSC) as a novel hybrid nano-catalyst for highly efficient synthesis of new 1,2,3-triazolyl-based metronidazole hybrid analogues having potent antigiardial activity
Soltani Rad, Mohammad?Navid,Behrouz, Somayeh,Mohammadtaghi-Nezhad, Javad,Zarenezhad, Elham,Agholi, Mahmoud
, (2019)
The preparation, characterization and application of silica-tethered cuprous acetophenone thiosemicarbazone (STCATSC) as a novel hybrid nano catalyst for synthesis of new 1,2,3-triazolyl-based metronidazole hybrid analogues is described. STCATSC is fully
Design, synthesis, and evaluation of metronidazole-1,2,3-triazole derivatives as potent urease inhibitors
Rezaei, Elham Babazadeh,Abedinifar, Fahimeh,Azizian, Homa,Montazer, Mohammad Nazari,Asadi, Mehdi,Hosseini, Samanesadat,Sepehri, Saghi,Mohammadi-Khanaposhtani, Maryam,Biglar, Mahmood,Larijani, Bagher,Amanlou, Massoud,Mahdavi, Mohammad
, p. 4217 - 4226 (2021/04/26)
A new series of metronidazole-1,2,3-triazole derivatives 6a–o was synthesized and evaluated as Helicobacter pylori urease inhibitors. All the synthesized compounds were more potent than standard inhibitor thiourea against urease. Among the synthesized compounds, compound 6f (IC50 = 1.975 ± 0.25?μM) with inhibitory activity around 11-fols more than thiourea (IC50 = 22.00 ± 0.14?μM) was the most potent compound. Kinetic study of this compound revealed that compound 6f inhibited urease in an uncompetitive mode. Based on molecular modeling study, compound 6f pointed toward the bi-nickel center and stabilized by H-bond and T-shape π–π hydrophobic interactions with the critical residues His492 and Asp633. Moreover, it anchored to the helix-turn-helix motif in the active site cavity through interaction with His593 and Arg609. Consequently, it proposed that compound 6f through stabilization of active site flap inhibited urease activity.
A fluorous and click approach for screening potential PET probes: Evaluation of potential hypoxia biomarkers
Bejot, Romain,Carroll, Laurence,Bhakoo, Kishore,Declerck, Jér?me,Gouverneur, Veronique
supporting information; experimental part, p. 324 - 329 (2012/03/10)
Radiopharmaceuticals for nuclear imaging are essentially targeting molecules, labeled with short-lived radionuclides (e.g., F-18 for PET). A significant drawback of radiopharmaceuticals development is the difficulty to access radiolabeled molecule libraries for initial in vitro evaluation, as radiolabeling has to be optimized for each individual molecule. The present paper discloses a method for preparing libraries of 18F-labeled radiopharmaceuticals using both the fluorous-based 18F-radiochemistry and the Huisgen 1,3-dipolar (click) conjugation reaction. As a proof of concept, this approach allowed us to obtain a series of readily accessible 18F-radiolabeled nitroaromatic molecules, for exploring their structure-activity relationship and further in vitro evaluation of their hypoxic selectivity.
