10527-64-7Relevant articles and documents
Preparation method of manidipine hydrochloride
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Paragraph 0037; 0038; 0046; 0056; 0066, (2017/12/06)
The invention discloses a preparation method of manidipine hydrochloride and belongs to the technical field of medicine preparation. Piperazine serving as a starting raw material is used for synthesis of N-(2-hydroxyethyl)piperazine, then 1-diphenylmethyl-4-(2-hydroxyethyl)piperazine is synthesized, and 2-(4-diphenylmethyl-1-piperazinyl)ethyl acetoacetic ester is synthesized; 2-(4-diphenylmethyl-1-piperazinyl)ethyl acetoacetic ester, m-nitrobenzaldehyde and methyl 3-aminocrotonate are dissolved in isopropanol, the mixture is subjected to heating reflux, a solvent is removed through steaming, residues are dissolved in trichloromethane, the mixture is dried with anhydrous sodium sulfate and filtered, a solvent of the filtrate is recovered under reduced pressure, residues are mixed with methanol to be completely dissolved, hydrogen chloride is introduced in an ice bath, the solvent is removed through steaming, residues are mixed with methanol, activated carbon is added for decoloration, filtering is performed, filtrate is cooled, and manidipine hydrochloride is obtained. The preparation method of manidipine hydrochloride is simple in process, the yield is high, the cost is low, and the product purity is high.
Polymorphic Forms of Manidipine
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Page/Page column 5, (2012/09/22)
The invention relates to various new polymorphic forms of manidipine and pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparation of the polymorphic forms of manidipine and pharmaceutically acceptable salts thereof.
Synthesis, Structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds
Burgess, Steven J.,Kelly, Jane X.,Shomloo, Shawheen,Wittlin, Sergio,Brun, Reto,Liebmann, Katherine,Peyton, David H.
experimental part, p. 6477 - 6489 (2010/11/05)
We have previously shown that a "reversed chloroquine (RCQ)" molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum (Burgess, S. J.; Selzer, A.; Kelly, J. X.; Smilkstein, M. J.; Riscoe, M. K.; Peyton, D. H. J. Med. Chem. 2006, 49, 5623. Andrews, S.; Burgess, S. J.; Skaalrud, D.; Kelly, J. X.; Peyton, D. H. J. Med. Chem. 2010, 53, 916). Here, we present an investigation into the Structure-activity relationship of the RCQ structures, resulting in an orally active molecule with good in vitro and in vivo antimalarial activity. We also present evidence of the mode of action, indicating that the RCQ molecules inhibit hemozoin formation in the parasite's digestive vacuole in a manner similar to that of chloroquine.