69921-48-8Relevant academic research and scientific papers
Design, synthesis, antimicrobial evaluation and docking studies of urea-triazole-amide hybrids
Kumar, Anil,Kumar, Ashwani,Lal, Kashmiri,Poonia, Nisha,Rani, Poonam
, (2020)
A series of urea-1,2,3-triazole-amide hybrids was designed and synthesized via click reaction of urea derivatives containing a propargyl unit with 2-bromo-N-phenylacetamide derivatives and characterized by FTIR, NMR and HRMS data. The antimicrobial evalua
Urea-thiazole/benzothiazole hybrids with a triazole linker: synthesis, antimicrobial potential, pharmacokinetic profile and in silico mechanistic studies
Baidya, Anurag T. K.,Kumar, Anil,Kumar, Ashwani,Kumar, Rajnish,Lal, Kashmiri,Poonia, Nisha,Sahu, Srikanta
, (2021/10/25)
Some urea-thiazole/benzothiazole hybrids with a triazole linker were synthesized via Cu(I)-catalysed click reaction. After successfully analysed by various spectral techniques including FTIR, NMR and HRMS, antimicrobial screening of the synthesized hybrid
Synthesis, evaluation, and molecular docking studies of aryl urea-triazole-based derivatives as anti-urease agents
Moghimi, Setareh,Goli-Garmroodi, Fereshteh,Allahyari-Devin, Maryam,Pilali, Hedieh,Hassanzadeh, Malihe,Mahernia, Shabnam,Mahdavi, Mohammad,Firoozpour, Loghman,Amanlou, Massoud,Foroumadi, Alireza
, (2018/05/30)
Considering the importance of urease inhibitors in the treatment of ureolytic bacterial infections, in this work, the synthesis of novel, aryl urea-triazole-based derivatives as effective urease inhibitors is described. Dichloro-substituted derivative 4o,
Novel VEGFR-2 kinase inhibitors identified by the back-to-front approach
Sanphanya, Kingkan,Wattanapitayakul, Suvara K.,Phowichit, Suwadee,Fokin, Valery V.,Vajragupta, Opa
, p. 2962 - 2967 (2013/06/27)
We report a novel VEGFR-2 inhibitor, developed by the back-to-front approach. Docking experiments indicated that the 3-chloromethylphenylurea motif of the lead compound occupied the back pocket of VEGFR-2 kinase. An attempt was made to enhance the binding affinity of 1 by expanding the structure to access the front pocket using a triazole linker. A library of 1,4-(disubstituted)-1H-1, 2,3-triazoles were screened in silico, and one compound (VH02) was identified with an IC50 against VEGFR-2 of 0.56 μM. VH02 showed antiangiogenic effects, inhibiting tube formation in HUVEC cells (EA.hy926) at 0.3 μM, 13 times lower than its cytotoxic dose. These enzymatic and cellular activities suggest that VH02 has potential as a lead for further optimization.
