1694-57-1Relevant articles and documents
Kinetic Energy Release and Position of Transition State During the Intramolecular Substitution of Ionized 2-Benzoyl Pyridines
Schubert, Ralf,Gruetzmacher, Hans-Friedrich
, p. 122 - 130 (1980)
The loss of substituents X from molecular ions of ortho substituted 2-benzoyl pyridines has been investigated as a function of the dissociation energy of the C-X bond.Comparison of unimolecular and collisional induced decompositions of the resulting + ions and reference ions arising from 3-hydroxypyridoindole shows that cyclic fragment ions are formed in every case by an intramolecular substitution reaction with the exception of the parent compound (X=H), which gives rise to a mixture of + ions with different structures.The heat of formation of the cyclic ion has been estimated experimentally and by calculation using thermochemical data, and from this value and the appearance energies, the activation energies of the reverse reactions have been evaluated for the different reaction systems.Measurement of the kinetic energy release during the substitution reactions shows that only part of the reverse activation energy is released as kinetic energy.The energy partitioning quotient varies from 0.37 to 0.08 depending on the dissociation energy of the C-X bond or the reaction enthalpy.A sudden change in the energy partitioning quotient is observed with increasing exothermicity of the reaction, paralleling the behaviour of similar reaction systems.These results are interpreted as a demonstration of the influence of the variation of transition state position on the energy partitioning quotient.
Ortho-halogenated phenylpyridine ketone compound and preparation method thereof
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Paragraph 0110-0113, (2019/12/25)
The invention relates to an ortho-halogenated phenylpyridine ketone compound and a preparation method thereof. According to the invention, dibromohydantoin or dichlorohydantoin is taken as a halogenating reagent, and the ortho-halogenation of a diarylketo
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.
supporting information, 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.