So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Nguyen, William; Dans, Madeline G.; Ngo, Anna; Gancheva, Maria R.; Romeo, Ornella; Duffy, Sandra; de Koning-Ward, Tania F.; Lowes, Kym N.; Sabroux, Helene Jousset; Avery, Vicky M.; Wilson, Danny W.; Gilson, Paul R.; Sleebs, Brad E. researched the compound: 4,4-Difluoropiperidine hydrochloride( cas:144230-52-4 ).SDS of cas: 144230-52-4.They published the article 《Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion》 about this compound( cas:144230-52-4 ) in European Journal of Medicinal Chemistry. Keywords: phenyl sulfonyl piperazine preparation antimalarial antitumor lipophilicity SAR; Antimalarial; Erythrocyte invasion; Malaria; Phenylsulfonyl piperazine; Plasmodium. We’ll tell you more about this compound (cas:144230-52-4).
The optimization and further characterization of the phenylsulfonyl piperazine class I [R = 4-Me, 3-t-Bu, 4-Br, etc.; R1 = pyrrolidin-1-yl, piperidin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, etc.; X = -(N(CH2)2N(CH2)2)-CH(CH3), -(NCH(CH3)N(CH2)2)-CH(CH3), -(NC(CH3)2N(CH2)2)-CH(CH3), etc.] was described. During the optimization process the functionality required for P. falciparum asexual stage activity was defined and determined the alpha-carbonyl S-Me isomer was important for antimalarial potency. The optimized compounds I also possessed comparable activity against multidrug resistant strains of P. falciparum and displayed weak activity against sexual stage gametocytes. The optimized compounds I blocked erythrocyte invasion consistent with the asexual activity observed and therefore the phenylsulfonyl piperazine analogs described could serve as useful tools for studying Plasmodium erythrocyte invasion.
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Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem