480446-80-8Relevant academic research and scientific papers
An efficient one-pot conversion of carboxylic acids into benzimidazoles via an HBTU-promoted methodology
Barasa, Leonard,Yoganathan, Sabesan
, p. 35824 - 35830 (2018/10/31)
Benzimidazole is a privileged, and routinely used pharmacophore in the drug discovery process. Herein, we report a mild, acid-free and one-pot synthesis of indole, alkyl and alpha-amino benzimidazoles through a novel HBTU-promoted methodology. An extensive library of indole-carboxylic acids, alkyl carboxylic acids and N-protected alpha-amino acids has been converted into the corresponding benzimidazoles in 80-99% yield. Since alpha-aminobenzimidazoles are highly useful synthons as chiral ligands for chemical catalysis, as well as for drug discovery endeavors, our reported method provides direct access to this scaffold in a simple, one-pot operation from commercially available carboxylic acids.
Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic
Balboni, Gianfranco,Fiorini, Stella,Baldisserotto, Anna,Trapella, Claudio,Sasaki, Yusuke,Ambo, Akihiro,Marczak, Ewa D.,Lazarus, Lawrence H.,Salvadori, Severo
body text, p. 5109 - 5117 (2009/08/16)
Some reference opioids containing the Dmt-Tic pharmacophore, especially the δ agonists H-Dmt-Tic-GlyNH-Ph (1) and H-Dmt-TiC-NH-(S)CH(CH 2-COOH)-Bid (4) (UFP-512) were evaluated for the influence of the substitution of Gly with aspartic acid, it
Potent δ-opioid receptor agonists containing the Dmt-Tic pharmacophore
Balboni, Gianfranco,Salvadori, Severo,Guerrini, Remo,Negri, Lucia,Giannini, Elisa,Jinsmaa, Yunden,Bryant, Sharon D.,Lazarus, Lawrence H.
, p. 5556 - 5563 (2007/10/03)
Conversion of δ-opioid receptor antagonists containing the 2′,6′-dimethyl-L-tyrosine (Dmt)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) pharmacophore into potent δ-agonists required a third heteroaromatic nucleus, such as 1H-benzimidazole-2-yl (
