A step-economical access to polysubstituted aminoimidazoles has been accomplished via alkene vicinal C-N bonds formation of 2-bromo-2-alkenones with guanidine avoiding its NH-protection/derivatization prerequisite for electronic modulation. The approach has excellent substrate scope, is amenable to diverse guanidine-containing substrates, and introduces distinctive substitutions/functionalities into aminoimidazole core. It is also applicable to preparation of fused-imidazoles. The reaction involves a tandem pathway of aza-Michael addition, S2, and a unique redox-neutral process, as evident by spectroscopic study and control experiments.
A Core‐Linker‐Polyamine (CLP) strategy has been exploited to develop new antileishmanial agents. It involves the linker‐based assembly of alkyl‐polyamine side chain as a potential pharmacophore motif with a privileged heterocyclic motif, 4‐arylquinoline. A series of aminoalkyl 4‐arylquinoline‐2‐carboxamides and their analogs were synthesized and tested against L. donovani promastigotes. Among all synthesized derivatives, 10 compounds showed significant antipromastigote activities with more efficacy (IC50: 4.75–8 μM) than an antileishmanial oral drug Miltefosine (IC50: 8.9±1.55 μM). Most active aminoalkyl‐quinoline‐carboxamides 9 a and 9 b, displayed negligible cytotoxicity towards human monocytic (THP‐1) macrophages. The compounds show antileishmanial activity by generating mitochondrial superoxide radicals. However, they did not show interference with trypanothione reductase, a redox enzyme of Leishmania. Significant change in the morphology of the L. donovani promastigote by the compounds was observed. The Structure‐activity relationship analysis suggest the pharmacophoric importance of alkylpolyamine and carboxamide motifs. In silico evaluation indicated that the investigated active molecules 9 a and 9 b possess important drug‐likeness, physicochemical and pharmacokinetic‐relevant properties.
Oil fromJ. multifidawas extracted and it was first converted intoN,N-bis(2-hydroxyethyl) Jatropha fatty amide (HEJFA). HEJFA has been synthesized by reaction between Jatropha oil and diethanol amine in presence of zinc oxide as a catalyst. The reaction is relatively rapid and proceeded to high yield at 200±5OC. The resulting HEJFA was used to formulate thermosetting coating compositions. Films were cured at ambient (air drying) and elevated (stove drying) temperatures usingN, N-bis(2-hydroxyethyl) Jatropha fatty amide (HEJFA) as eco-friendly crosslinking agent for acrylic resin. The coating performance of the various compositions was tested by measurement of scratch hardness, impact strength and chemical resistance. The results show better performance of the HEJFA based compositions compared to butylated melamine formaldehyde (MF) based compositions.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.