3995-42-4Relevant articles and documents
Docking, synthesis and antimalarial activity of novel 4-anilinoquinoline derivatives
Vijayaraghavan, Shilpa,Mahajan, Supriya
, p. 1693 - 1697 (2017/04/04)
A series of 4-anilinoquinoline triazine derivatives were designed, synthesized and screened for in vivo antimalarial activity against a chloroquine-sensitive strain of Plasmodium berghei. The compounds were further subjected to in vitro antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum and β-haematin inhibition studies. All the compounds exhibited in vivo antimalarial activity better than that shown by the standard drug, chloroquine. Twelve out of fifteen compounds showed better inhibition than that of chloroquine against chloroquine-resistant W2 strain of Plasmodium falciparum. Ten compounds showed β-haematin inhibition, better than that of chloroquine, with IC50 values in the range of 18–25?μM. One compound, 3k, was found to be better than artemisinin against W2 strain of Plasmodium falciparum and also displayed the best β-haematin inhibitory activity, thereby becoming eligible to be explored as a potential lead for antimalarial chemotherapy.
Bis(hydroxyamino)triazines: Versatile and high-affinity tridentate hydroxylamine ligands for selective iron(III) chelation
Ekeltchik, Irina,Gun, Jenny,Lev, Ovadia,Shelkov, Rimma,Melman, Artem
, p. 1285 - 1293 (2007/10/03)
A new versatile family of chelating agents based on bis(hydroxyamino)-1,3, 5-triazines, BHTs, is described. The properties of different BHT ligands are determined by electrochemistry, spectroscopy and titrimetry revealing high redox stability, transparenc
Synthesis and aromatase-inhibitory activity of imidazolyl-1,3,5-triazine derivatives
Matsuno, Toshiyuki,Kato, Masanobu,Tsuchida, Yoshio,Takahashi, Masayuki,Yaguchi, Sin-Ichi,Terada, Sumio
, p. 291 - 296 (2007/10/03)
Triamino-substituted 1,3,5-triazine derivatives were synthesized and tested for inhibitory activities against the aromatase of human placental microsomes and the cytochrome P450 side chain cleavage of cholesterol (P450(SCC)) of pig adrenal mitochondria. The compounds having imidazolyl and tertiary amino groups as substituents in the 1,3,5-triazine ring showed significant aromatase-inhibitory activity. Among them, compounds 17, 23, 26, 27 and 28 were more active than the reference compound, CGS 16949A. The inhibitory activities of these compounds against P450(SCC) were much weaker than their aromatase-inhibitory activities. These compounds may be regarded as selective aromatase inhibitors.
