O-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity was written by Corpas-Lopez, Victoriano;Tabraue-Chavez, Mavys;Sixto-Lopez, Yudibeth;Panadero-Fajardo, Sonia;Alves de Lima Franco, Fernando;Dominguez-Seglar, Jose F.;Morillas-Marquez, Francisco;Franco-Montalban, Francisco;Diaz-Gavilan, Monica;Correa-Basurto, Jose;Lopez-Viota, Julian;Lopez-Viota, Margarita;Perez del Palacio, Jose;de la Cruz, Mercedes;de Pedro, Nuria;Martin-Sanchez, Joaquina;Gomez-Vidal, Jose A.. And the article was included in Journal of Medicinal Chemistry in 2020.SDS of cas: 62473-92-1 This article mentions the following:
Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound PhNHCO(CH2)6CONHOCPh3 (I)showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound I represents a new class of selective ligands with antileishmanial activity. In the experiment, the researchers used many compounds, for example, 6-Bromobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 62473-92-1SDS of cas: 62473-92-1).
6-Bromobenzo[d]isothiazol-3(2H)-one 1,1-dioxide (cas: 62473-92-1) belongs to isothiazole derivatives. The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. In general, isothiazole undergoes nitration in the presence of HNO3, sulfuric acid, and sulfonation by using sulfuric acid under thermal conditions to generate corresponding 4-nitro- and 4-sulfonic acid derivatives, respectively.SDS of cas: 62473-92-1
Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com