In 2022,Taft, Benjamin R.; Yokokawa, Fumiaki; Kirrane, Tom; Mata, Anne-Catherine; Huang, Richard; Blaquiere, Nicole; Waldron, Grace; Zou, Bin; Simon, Oliver; Vankadara, Subramanyam; Chan, Wai Ling; Ding, Mei; Sim, Sandra; Straimer, Judith; Guiguemde, Armand; Lakshminarayana, Suresh B.; Jain, Jay Prakash; Bodenreider, Christophe; Thompson, Christopher; Lanshoeft, Christian; Shu, Wei; Fang, Eric; Qumber, Jafri; Chan, Katherine; Pei, Luying; Chen, Yen-Liang; Schulz, Hanna; Lim, Jessie; Abas, Siti Nurdiana; Ang, Xiaoman; Liu, Yugang; Angulo-Barturen, Inigo; Jimenez-Diaz, Maria Belen; Gamo, Francisco Javier; Crespo-Fernandez, Benigno; Rosenthal, Philip J.; Cooper, Roland A.; Tumwebaze, Patrick; Aguiar, Anna Caroline Campos; Campo, Brice; Campbell, Simon; Wagner, Jurgen; Diagana, Thierry T.; Sarko, Christopher published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria》.Application of 3034-22-8 The author mentioned the following in the article:
A series of 5-aryl-2-amino-imidazothiadiazole (ITD) derivatives were identified by a phenotype-based high-throughput screening using a blood stage Plasmodium falciparum (Pf) growth inhibition assay. A lead optimization program focused on improving antiplasmodium potency, selectivity against human kinases, and absorption, distribution, metabolism, excretion, and toxicity properties and extended pharmacol. profiles culminated in the identification of INE963 (1)(I), which demonstrates potent cellular activity against Pf 3D7 (EC50 = 0.006 μM) and achieves “”artemisinin-like”” kill kinetics in vitro with a parasite clearance time of <24 h. A single dose of 30 mg/kg is fully curative in the Pf-humanized severe combined immunodeficient mouse model. INE963 (1) also exhibits a high barrier to resistance in drug selection studies and a long half-life (T1/2) across species. These properties suggest the significant potential for INE963 (1) to provide a curative therapy for uncomplicated malaria with short dosing regimens. For these reasons, INE963 (1) was progressed through GLP toxicol. studies and is now undergoing Ph1 clin. trials. In the experiment, the researchers used 5-Bromothiazol-2-amine(cas: 3034-22-8Application of 3034-22-8)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Application of 3034-22-8
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica