New substituted triazolopyrimidines as Anti-malarial agents
A technology of azolopyrimidine and pyrimidine, which is applied in the field of reagents for preparing pharmaceutical preparations and can solve problems such as damage to chemotherapy
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[0036] According to one embodiment, there are provided triazolopyrimidine derivatives of formula (I) and any pharmaceutically acceptable salts, hydrates, solvates, polymorphs, tautomers, geometric isomers thereof or optically active isomers,
[0037]
[0038] where R 1 selected from halogen such as F and H, R 2 from F and C 1 -C 4 Alkyl, such as methyl.
[0039] In a particular embodiment, the present invention provides the triazolopyrimidine derivatives of the present invention, wherein R 1 It is H.
[0040] In a particular embodiment, the present invention provides the triazolopyrimidine derivatives of the present invention, wherein R 1 It is F.
[0041] In a particular embodiment, the present invention provides the triazolopyrimidine derivatives of the present invention, wherein R 2 is CH 3 .
[0042] In a particular embodiment, the present invention provides the triazolopyrimidine derivatives of the present invention, wherein R 2 It is F.
[0043] In a speci...
Embodiment 1
[0096]Example 1: Synthesis of compounds according to the invention
[0097] Triazolopyrimidine Derivatives can be prepared from readily available starting materials using methods and procedures known to those skilled in the art. It should be understood that where typical or preferred experimental conditions (ie, reaction temperatures, times, moles of reagents, solvents, etc.) are given, other experimental conditions can also be used unless otherwise stated. Optimum reaction conditions may vary with the particular reactants or solvent used, but such conditions can be determined by one skilled in the art using routine optimization methods. The title compounds of the present invention were synthesized following the general synthetic route described in Scheme 1 below.
[0098] plan 1
[0099]
[0100] Reagents and conditions: i) a) NaOH, EtOH, room temperature for 3 hours; (or) b) NaOEt, EtOH, reflux for 5 hours, room temperature overnight; ii) a suitable difluoroester, such ...
Embodiment 2
[0137] Example 2: Antimalarial Activity of Compounds of the Invention
[0138] The ability of the triazolopyrimidine derivatives according to the invention to kill and / or inhibit the proliferation of Plasmodium falciparum parasites is determined by their ability to inhibit the growth of Plasmodium falciparum parasites. Growth inhibition was determined as follows: P. falciparum 3D7 cells were grown in Gibco-Invitrogen RPMI-1640 supplemented with 2% (w / v) red blood cells (RBC) and alternatively 20% human type A+ plasma (Desjardins et al. , 1979, Antimicrob Agents Chemother. 16, 710-718) or supplemented with Gibco-Invitrogen 0.5% Albumax I (Coteron et al., 2011, J. Med. Chem., 54, 5540-5561). Serial compound stock dilutions were prepared at 200X final concentrations in 100% DMSO, followed by 20X stocks in culture medium. Cell growth was monitored by the SYBR Green method as described (Deng et al., 2014. J. Med. Chem., 57, 5381-539). Parasites (0.19 ml, 0.5% parasiteemia, 0.5% H...
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