In 2022,Cho, Nobuo; Kikuzato, Ko; Futamura, Yushi; Shimizu, Takeshi; Hayase, Hiroki; Kamisaka, Kikuko; Takaya, Daisuke; Yuki, Hitomi; Honma, Teruki; Niikura, Mamoru; Kobayashi, Fumie; Watanabe, Nobumoto; Osada, Hiroyuki; Koyama, Hiroo published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9-tetrahydro-1H-β-carboline derivatives possessing a 2-((coumarin-5-yl)oxy)alkanoyl moiety》.Recommanded Product: 4949-44-4 The author mentioned the following in the article:
The identification, structure-activity relationships (SARs) and biol. effects of new antimalarials I [R = Me, Et, cyclopropylmethyl, etc.; R1 = Me, Et, Pr, etc.; R2 = H; R3 = C(O)OMe, C(O)Me, C(O)NHMe, etc.; R4 = H, Me, morpholin-4-yl] consisting of a 2,3,4,9-tetrahydro-1H-β-carboline core, a coumarin ring and an oxyalkanoyl linker was described. A cell-based phenotypic approach was employed in this search for novel antimalarial drugs with unique modes of action. This screening campaign of the RIKEN compound library succeeded in the identification of the known tetrahydro-β-carboline derivative I [R = n-Bu, R1 = H, R2 = H, R3 = C(O)OMe, R4 = Me] as a hit compound showing significant in vitro activity. SAR studies on this chem. series led to the discovery of compound I [R = n-Bu, R1 = (R)-Me, R2 = H, R3 = (S)-C(O)OMe, R4 = Me] having a (R)-Me group on the oxyacetyl linker with potent inhibition of parasite growth (IC50 = 2.0 nM). Compound I [R = n-Bu, R1 = (R)-Me, R2 = H, R3 = (S)-C(O)OMe, R4 = Me] was also found to exhibit significant in vivo antimalarial effects in mouse models. Furthermore, mol. modeling studies on compounds I [R = n-Bu, R1 = H, (R/S)-Me, R2 = H, R3 = (S)-C(O)OMe, R4 = Me] suggested that the (R)-Me group of 4h forces the preferential adoption of a specific conformer which was considered to be an active conformer. The experimental process involved the reaction of Ethyl 3-oxopentanoate(cas: 4949-44-4Recommanded Product: 4949-44-4)
Ethyl 3-oxopentanoate(cas: 4949-44-4) belongs to ketone compounds. Ketones are highly reactive, although less so than aldehydes, to which they are closely related. Much of their chemical activity results from the nature of the carbonyl group. Ketones readily undergo a wide variety of chemical reactions.Recommanded Product: 4949-44-4
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