56643-72-2Relevant academic research and scientific papers
Synthesis and antitubercular screening of imidazole derivatives
Pandey, Jyoti,Tiwari, Vinod K.,Verma, Shyam S.,Chaturvedi, Vinita,Bhatnagar,Sinha,Gaikwad,Tripathi, Rama P.
experimental part, p. 3350 - 3355 (2009/12/01)
A series of imidazole based compounds were synthesized by reacting simple imidazoles with alkyl halides or alkyl halocarboxylate in presence of tetrabutylammonium bromide (TBAB). The compounds bearing carbethoxy group undergo amidation with different amines in the presence of DBU to give respective carboxamides. The synthesized compounds were screened against Mycobacterium tuberculosis where compound 17 exhibited very good in vitro antitubercular activity and may serve as a lead for further optimization.
Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17α-hydroxylase/17,20-lyase (P45017α)
Owen, Caroline P.,Dhanani, Sachin,Patel, Chirag H.,Shahid, Imran,Ahmed, Sabbir
, p. 4011 - 4015 (2007/10/03)
The cytochrome P-450 enzyme, 17α-hydroxylase/17,20-lyase (P45017α), is a potential target in hormone-dependent cancers. Here, we report the synthesis and biochemical evaluation of a range of benzyl imidazole-based compounds which have been targeted against the two components of this enzyme, that is, 17α-hydroxylase (17α-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are good inhibitors, with N-4-iodobenzyl imidazole (5) (IC50 = 10.06 μM against 17α-OHase and IC50 = 1.58 μM against lyase) showing equipotent activity against lyase compared to the standard compound, ketoconazole (KTZ) (IC50 = 3.76 ± 0.01 μM against 17α-OHase and IC50 = 1.66 ± 0.15 μM against lyase). Furthermore, the compounds tested are less potent towards the 17α-OHase component, a desirable property in the development of novel inhibitors of P45017α.
N-(3,4-dichlorobenzyl)azoles - Investigations regarding synthesis, NMR-spectroscopy and affinity towards sigma-1 and sigma-2 receptors
Holzer, Wolfgang,Brandst?tter, Bettina,J?ger, Christine,Kaun, Michael,Langer, Thierry,Bowen, Wayne D.
, p. 197 - 211 (2007/10/03)
A series of azoles and aminoazoles with a 3,4-dichlorobenzyl moiety attached to a ring nitrogen atom was synthesized via reaction of the parent systems with 3,4-dichlorobenzyl chloride. Regioisomeric products were discriminated on the basis of 13C-NMR data or by NOE-difference spectroscopy. The affinities of some representatives towards sigma-1 and sigma-2 receptors were determined by receptor binding assays.
