21331-80-6Relevant academic research and scientific papers
Heterocyclic compound serving as SOS1 inhibitor
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Paragraph 0166-0168, (2021/08/06)
The invention provides a compound serving as an SOS1 inhibitor, and particularly provides a compound with a structure as shown in a formula (I), or an optical isomer, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative, a hydrate and a solvate of the compound. The compound can be used for treating or preventing diseases or symptoms related to the activity or expression quantity of SOS1.
Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT
Deane, Karen J.,Summers, Robert L.,Lehane, Adele M.,Martin, Rowena E.,Barrow, Russell A.
, p. 576 - 581 (2014/06/09)
The emergence and spread of malaria parasites that are resistant to chloroquine (CQ) has been a disaster for world health. The antihistamine chlorpheniramine (CP) partially resensitizes CQ-resistant (CQR) parasites to CQ but possesses little intrinsic antiplasmodial activity. Mutations in the parasite's CQ resistance transporter (PfCRT) confer resistance to CQ by enabling the protein to transport the drug away from its site of action, and it is thought that resistance-reversers such as CP exert their effect by blocking this CQ transport activity. Here, a series of new structural analogues and homologues of CP have been synthesized. We show that these compounds (along with other in vitro CQ resistance-reversers) inhibit the transport of CQ via a resistance-conferring form of PfCRT expressed in Xenopus laevis oocytes. Furthermore, the level of PfCRT-inhibition was found to correlate well with both the restoration of CQ accumulation and the level of CQ resensitization in CQR parasites.
Synthesis of 2-(N-disubstituted amino)ethyltriphenylphosphonium bromides
Rao, G. Venkateswara,Reddy, G. Chandrasekara
, p. 824 - 826 (2008/04/13)
2-(N-Disubstituted amino)ethyltriphenylphosphonium bromides are prepared in quantitative yields with high purity by reacting secondary amines with 2-methoxyethyltriphenylphosphonium bromide under aqueous conditions. The differential reactivity of this reagent offers advantages for the preparation of aminoethyltriphenylphosphonium bromides possessing nucleophiles such as hydroxy groups.
PREPARATION DE SELS D'AMINOALKYLPHOSPHONIUMS
Dantas, T. N. de Castro,Laval, J. P.,Lattes, A.
, p. 97 - 106 (2007/10/02)
Three synthetic methods have been applied to prepare amino phosphonium salts: (C6H5)3P+-(CH2)n-N-.The best ways have been determined for different n values and different substituents on the nitrogen atom.In all cases, yields are better with n=3, but no intramolecular stabilization has been detected.
