Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? was written by Terzic, Natasa;Konstantinovic, Jelena;Tot, Miklos;Burojevic, Jovana;Djurkovic-Djakovic, Olgica;Srbljanovic, Jelena;Stajner, Tijana;Verbic, Tatjana;Zlatovic, Mario;Machado, Marta;Albuquerque, Ines S.;Prudencio, Miguel;Sciotti, Richard J.;Pecic, Stevan;D’Alessandro, Sarah;Taramelli, Donatella;Solaja, Bogdan A.. And the article was included in Journal of Medicinal Chemistry in 2016.Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid This article mentions the following:
The syntheses and antiplasmodial activities of various substituted aminoquinolines coupled to an adamantane carrier are described. The compounds exhibited pronounced in vitro and in vivo activity against Plasmodium berghei in the Thompson test. Tethering a fluorine atom to the aminoquinoline C(3) position afforded fluoroaminoquinolines that act as intrahepatocytic parasite inhibitors, with compound 25 having an IC50 = 0.31 μM and reducing the liver load in mice by up to 92% at 80 mg/kg dose. Screening our peroxides as inhibitors of liver stage infection revealed that the tetraoxane pharmacophore itself is also an excellent liver stage P. berghei inhibitor (78: IC50 = 0.33 μM). Up to 91% reduction of the parasite liver load in mice was achieved at 100 mg/kg. Examination of tetraoxane 78 against the transgenic 3D7 strain expressing luciferase under a gametocyte-specific promoter revealed its activity against stage IV-V Plasmodium falciparum gametocytes (IC50 = 1.16 ± 0.37 μM). To the best of our knowledge, compounds 25 and 78 are the first examples of either an 4-aminoquinoline or a tetraoxane liver stage inhibitors. In the experiment, the researchers used many compounds, for example, 5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid).
5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8) belongs to benzothiophene derivatives. Benzothiophene scaffolds are of great importance due to its increased presence in bioactive molecules. It has been used as a raw material for the synthesis of biologically active structures and is found in pharmaceuticals such as leukotriene synthesis inhibitors and antifungals, as well as in many natural products.Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem