170031-70-6Relevant articles and documents
Design and synthesis of novel enantiomerically enriched morpholino [4, 3–a] benzimidazole derivatives as potential bioactive agents
Tiwari, Pawankumar R.,John, Marina E.,Karnik, Anil V.
, p. 2575 - 2583 (2018)
A series of chiral morpholino [4, 3-a] benzimidazole derivatives were synthesized effectively from (S)-(-)-2-(α-hydroxyethyl)-benzimidazole and phenacyl bromide derivatives using an efficient synthetic protocol in good yields and moderate diastereoselectivities. The substrate controlled diastereoselective route makes available structurally attractive morpholine-fused benzimidazole derivatives with two chiral centers in enantiomerically enriched forms. The preliminary biological evaluation shows scope for potential applications.
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3
Hayes, Martin E.,Wallace, Grier A.,Grongsaard, Pintipa,Bischoff, Agnieszka,George, Dawn M.,Miao, Wenyan,McPherson, Michael J.,Stoffel, Robert H.,Green, David W.,Roth, Gregory P.
, p. 1573 - 1576 (2008/09/21)
High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both human and murine receptors.
Synthesis of some pyrido- and pyrazino-benzimidazole derivatives and their antifungal activity
Demirayak,Guven
, p. 527 - 529 (2007/10/02)
Some 2-aryl-4-hydroxypyrido[1,2-a]benzimidazole and 1-substituted 3-arylpyrazino-[1,2-a]benzimidazole derivatives were synthesized using 1-(2-arylethan-2-on)2-acylbenzimidazole derivatives as starting materials. Antifungal activities of the compounds obtained were examined in vitro.
