Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35 was written by Atack, Thomas C.;Raymond, Donald D.;Blomquist, Christa A.;Pasaje, Charisse Flerida;McCarren, Patrick R.;Moroco, Jamie;Befekadu, Henock B.;Robinson, Foxy P.;Pal, Debjani;Esherick, Lisl Y.;Ianari, Alessandra;Niles, Jacquin C.;Sellers, William R.. And the article was included in ACS Medicinal Chemistry Letters in 2020.Quality Control of 4-Iodo-1,2-dimethoxybenzene This article mentions the following:
FK506-binding protein 35, FKBP35, has been implicated as an essential malarial enzyme. Rapamycin and FK506 exhibit antiplasmodium activity in cultured parasites. However, due to the highly conserved nature of the binding pockets of FKBPs and the immunosuppressive properties of these drugs, there is a need for compounds that selectively inhibit FKBP35 and lack the undesired side effects. In contrast to human FKBPs, FKBP35 contains a cysteine, C106, adjacent to the rapamycin binding pocket, providing an opportunity to develop targeted covalent inhibitors of Plasmodium FKBP35. Here, we synthesize inhibitors of FKBP35, show that they directly bind FKBP35 in a model cellular setting, selectively covalently modify C106, and exhibit antiplasmodium activity in blood-stage cultured parasites. In the experiment, the researchers used many compounds, for example, 4-Iodo-1,2-dimethoxybenzene (cas: 5460-32-2Quality Control of 4-Iodo-1,2-dimethoxybenzene).
4-Iodo-1,2-dimethoxybenzene (cas: 5460-32-2) belongs to iodide derivatives. Organoiodine compounds occur widely in organic chemistry, but are relatively rare in nature. Iodo alkanes participate in a variety of organic synthesis reactions, which include the SimmonsSmith reaction (cyclopropanation using iodomethane), Williamson ether synthesis, Wittig reaction, Grignard reaction, alkyl coupling reactions, and Wurtz reaction.Quality Control of 4-Iodo-1,2-dimethoxybenzene
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com