106412-95-7Relevant academic research and scientific papers
Synthesis of new praziquantel analogues: Potential candidates for the treatment of schistosomiasis
Sadhu, Partha Sarathi,Kumar, Singam Naveen,Chandrasekharam, Malapaka,Pica-Mattoccia, Livia,Cioli, Donato,Rao, Vaidya Jayathirtha
, p. 1103 - 1106 (2012/03/11)
An efficient synthesis of antischistosomal drug praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structure-activity relationship understanding. Total of nineteen PZQ analogues with structural variations at amide, piperazine and aromatic moieties have been synthesized and fully characterized. Among all the new analogues tested for antischistosomal activity, one dimethoxy tetrahydroisoquinoline analogue and two tetrahydro-β-carboline analogues exhibited moderate activity against adult Schistosoma mansoni. Tetrahydro-β-carboline analogues showed moderate activity whereas the presence of p-trifluoromethylbenzoyl and p-toluenesulphonyl moieties resulted in complete suppression of antischistosomal activity.
Efficient and diverse synthesis of indole derivatives
Liu, Haixia,Doemling, Alexander
supporting information; experimental part, p. 6895 - 6898 (2009/12/31)
(Chemical Equation Presented) A convergent 2-step procedure toward an array of indole derivatives involving an Ugi reaction and a Pictet - Spengler reaction is described. The reactions are versatile regarding different starting materials. Hexacyclic 24 can be produced with unprecedented complexity.
PRAZIQUANTEL ANALOGUES. I. NEW AND SHORT SYNTHESIS OF 2-ACYL-4-OXO-1,2,3,4,6,7,12,12b-OCTAHYDROPYRAZINOPYRIDOINDOLES
Valls, Nativitat,Segarra, Victor M.,Bosch, Joan
, p. 943 - 946 (2007/10/02)
A series of potential anthelmintic 2-acyl-4-oxo-1,2,3,4,6,7,12,12b-octahydropyrazinopyridoindoles has been synthesized in high yield by Pictet-Spengler reaction between tryptamine and the appropriate N-acyl-N-(2,2-diethoxyethyl)glycine ethyl ester.
