34576-83-5Relevant articles and documents
Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure-Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents
Pieroni, Marco,Azzali, Elisa,Basilico, Nicoletta,Parapini, Silvia,Zolkiewski, Michal,Beato, Claudia,Annunziato, Giannamaria,Bruno, Agostino,Vacondio, Federica,Costantino, Gabriele
, p. 1959 - 1970 (2017/03/17)
Malaria eradication is a global health priority, but current therapies are not always suitable for providing a radical cure. Artemisinin has paved the way for the current malaria treatment, the so-called Artemisinin-based Combination Therapy (ACT). However, with the detection of resistance to ACT, innovative compounds active against multiple parasite species and at multiple life stages are needed. GlaxoSmithKline has recently disclosed the results of a phenotypic screening of an internal library, publishing a collection of 400 antimalarial chemotypes, termed the “Malaria Box”. After analysis of the data set, we have carried out a medicinal chemistry campaign in order to define the structure-activity relationships for one of the released compounds, which embodies a benzothiophene-2-carboxamide core. Thirty-five compounds were prepared, and a description of the structural features responsible for the in vitro activity against different strains of P. falciparum, the toxicity, and the metabolic stability is herein reported.
Synthesis, characterization and structure activity relationship studies of benzo[b]thiophene derivatives as promising class of antimicrobial agents
Ghodasara,Vaghasiya,Gothaliya,Shah
, p. 349 - 354 (2014/03/21)
Here we employed simple chemistry for the synthesis of a new potent series of benzo[b]thiophene containing 2-carbonylchlorides (1), 2-isopropyl carboxamides (2), 2-(piperidin-1-yl)-methanones (3) by nucleophilic chloro cyclocondensation of substituted-cin
The Synthesis of Difluorobenzothienoquinolines and Their N-Methyl Quaternary Salts
Luo, Jiann-Kuan,Castle, Steven L.,Castle, Raymond N.
, p. 2047 - 2052 (2007/10/02)
A series of difluorobenzothienoquinolines has been prepared by photocyclization of the appropriate carboxamides.The lactams obtained were converted into the corresponding chloro derivatives which were catalytically dechlorinated into the difluorobenzothienoquinolines.The latter compounds were transformed into the N-methyl quaternary salts.