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3H-Pyrazole

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Nilo Zanatta – One of the best experts on this subject based on the ideXlab platform.

  • antimalarial activity of 4 5 trifluoromethyl 1h pyrazol 1 yl chloroquine analogues
    Bioorganic & Medicinal Chemistry Letters, 2006
    Co-Authors: Wilson Cunico, Nilo Zanatta, Cleber A Cechinel, Helio G Bonacorso, Marcos A P Martins
    Abstract:

    Abstract The antimalarial activity of chloroquine-pyrazole analogues, synthesized from the reaction of 1,1,1-trifluoro-4-methoxy-3-alken-2-ones with 4-hydrazino-7-chloroquinoline, has been evaluated in vitro against a chloroquine resistant Plasmodium falciparum clone. Parasite growth in the presence of the test drugs was measured by incorporation of [3H]hypoxanthine in comparison to controls with no drugs. All but one of the eight (4,5-dihydropyrazol-1-yl) chloroquine 2 derivatives tested showed a significant activity in vitro, thus, are a promising new class of antimalarials. The three most active ones were also tested in vivo against Plasmodium berghei in mice. However, the (pyrazol-1-yl) chloroquine 3 derivatives were mostly inactive, suggesting that the aromatic functionality of the pyrazole ring was critical.

Wilson Cunico – One of the best experts on this subject based on the ideXlab platform.

  • antimalarial activity of 4 5 trifluoromethyl 1h pyrazol 1 yl chloroquine analogues
    Bioorganic & Medicinal Chemistry Letters, 2006
    Co-Authors: Wilson Cunico, Nilo Zanatta, Cleber A Cechinel, Helio G Bonacorso, Marcos A P Martins
    Abstract:

    Abstract The antimalarial activity of chloroquine-pyrazole analogues, synthesized from the reaction of 1,1,1-trifluoro-4-methoxy-3-alken-2-ones with 4-hydrazino-7-chloroquinoline, has been evaluated in vitro against a chloroquine resistant Plasmodium falciparum clone. Parasite growth in the presence of the test drugs was measured by incorporation of [3H]hypoxanthine in comparison to controls with no drugs. All but one of the eight (4,5-dihydropyrazol-1-yl) chloroquine 2 derivatives tested showed a significant activity in vitro, thus, are a promising new class of antimalarials. The three most active ones were also tested in vivo against Plasmodium berghei in mice. However, the (pyrazol-1-yl) chloroquine 3 derivatives were mostly inactive, suggesting that the aromatic functionality of the pyrazole ring was critical.

Junying Miao – One of the best experts on this subject based on the ideXlab platform.

  • synthesis crystal structure and biological evaluation of novel 2 5 hydroxymethyl 3 phenyl 1h pyrazol 1 yl 1 phenylethanol derivatives
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Liangwen Zheng, Baoxiang Zhao, Yaohui Huang, Jun Ding, Junying Miao
    Abstract:

    Abstract A series of novel 2-(5-(hydroxymethyl)-3-phenyl-1H-pyrazol-1-yl)-1-phenylethanol derivatives (4) was synthesized from ethyl 1-(2-oxo-2-phenylethyl)-3-phenyl-1H-pyrazole-5-carboxylate derivatives (3) and characterized by means of IR, 1H NMR, HRMS and X-ray crystal diffraction. Structures of 4a, 4d, 4e and 4f were also determined by 13C NMR. Isomeric intermediates, 3a and 5a, were unambiguously confirmed by X-ray crystal structure analysis and successfully differentiated with 1H NMR chemical shifts of methylene bonded to pyrazole ring. Preliminary biological evaluation showed that compounds 4d and 4e could suppress A549 lung cancer cell growth through cell cycle arrest and autophagy.