15823-58-2Relevant academic research and scientific papers
Application of 2-(octylsulphanyl)benzoic acid as Pb2+ selective ionophore in hybrid membrane system
Oberta, Andrzej,Wasilewski, Janusz,Swiatkowski, Marek,Wodzki, Romuald
, p. 26 - 32 (2012)
A solution of 2-(octylsulphanyl)benzoic acid in 1,2-dichloroethane was used as a liquid membrane for selective pertraction of Pb2+ cations. Transport processes were carried out in a multi-membrane hybrid system (MHS) consisting of two cation-ex
Repositioning Salirasib as a new antimalarial agent
Porta, Exequiel O. J.,Bofill Verdaguer, Ignasi,Perez, Consuelo,Banchio, Claudia,Ferreira De Azevedo, Mauro,Katzin, Alejandro M.,Labadie, Guillermo R.
supporting information, p. 1599 - 1605 (2019/09/30)
Malaria is a serious tropical disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with the post-translational modification of Ras. This S-farnesyl thiosalicylate inhibits isoprenylcysteine carboxyl methyltransferase (ICMT), a validated target for cancer drug development. There is a high homology between the human and the parasite enzyme isoforms, in addition to being a druggable target. Looking to repurpose its structure as an antimalarial drug, a collection of S-substituted derivatives of thiosalicylic acid were prepared by introducing 1,2,3-triazole as a diversity entry point or by direct alkylation of the thiol. We further investigated the in vitro toxicity of FTS analogues to Plasmodium falciparum in the asexual stages and in Vero cells. An antiplasmodial activity assay was performed using a simple, high-sensitivity methodology based on nanoluciferase (NLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromolar concentration, including Salirasib. The most potent member of the series has S-farnesyl and the 1,2,3-triazole moiety substituted with phytyl. However, the compound substituted with methyl-naphthyl shows promising physicochemical and activity values. The low cytotoxicity in eukaryotic cells of the most active analogs provided good therapeutic indices, being starting-point candidates for future antimalarial drug development.
Lipase-catalyzed kinetic resolution of a series of esters having a sulfoxide group as the stereogenic centre
Allenmark,Andersson
, p. 2371 - 2376 (2007/10/02)
A series of methyl 2-(alkylsulfinyl)benzoates (alkyl = C1, n-C4, n-C8, n-C12 and n-C16) was investigated with respect to substrate behaviour and enantioselectivity in a lipase (Candida rugosa)-catalyz
