Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines

Acharya, Badri Narayan; Saraswat, Deepika; Tiwari, Mugdha; Shrivastava, Asish Kumar; Ghorpade, Ramarao; Bapna, Saroj; Kaushik, M. P.

doi:10.1016/j.ejmech.2009.10.023

Cited by 130 publications

(43 citation statements)

References 36 publications

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“…Pyrazolines have received considerable attention in recent years due to their wide range of anticancer [33], antimicrobial [34][35][36], antiviral [37], antioxidant [38], anticonvulsant [39], antiamoebic, cytotoxic [40], antihistaminic [41], antiinflammatory [42], COX-2 inhibitor [43] and antimalarial [44] activities. The current research has focused on the anticancer activity of phthalimides and pyrazolines, combination of the pyrazoline moiety with the phthalimide nucleus may enhance these activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Motaleb

Abdel-Ghaney

Abdel‐Bary

et al. 2015

J Radioanal Nucl Chem

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Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and 1 H NMR spectroscopy. It was radiolabeled with iodine-131 by direct electrophilic substitution reaction and radiochemical yield was determined by using different chromatographic techniques (HPLRC, paper chromatography and paper electrophoresis). 131 I-HPZPHT has high radiolabeling yield (98.00 ± 2.00 %), stability, solid tumor uptake and T/NT ratio (5.17 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.

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Section: Introductionmentioning

confidence: 99%

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Motaleb

Abdel-Ghaney

Abdel‐Bary

et al. 2015

J Radioanal Nucl Chem

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“…Chalcones and pyrazolines are another important class of compounds with wide spread biological applications 18,19 . Growing concern about environmental damage leads to an urgent requirement for the development of efficient and environmentally benign chemical processes for the synthesis of new molecules.…”

Section: Research Articlementioning

confidence: 99%

Thermal solvent-free synthesis of chromonyl chalcones, pyrazolines and their in vitro antibacterial, antifungal activities

Siddiqui

Praveen

Musthafa

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Wanare et al 11 reported pyrazoline derivatives (IV) as growth inhibitors for P. falciparum. Similarly, Acharya et al 12 and Insuasty et al 13 also developed pyrazoline analogues (V-VI) and assessed their antimalarial activity ( Figure 2).…”

Section: Introductionmentioning

confidence: 99%

Novel pyrazole–pyrazoline hybrids endowed with thioamide as antimalarial agents: their synthesis and 3D-QSAR studies

Marella

Shaquiquzzaman

Akhter

et al. 2014

Journal of Enzyme Inhibition and Medicinal Chemistry

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One of the most viable options to tackle the growing resistance to the antimalarial drugs is hybrid molecules. It involves combination of different scaffolds in one frame that may lead to compounds with diverse biological profiles. In this context, new hybrids of three different scaffolds viz pyrazole, pyrazoline and thiosemicarbazone moiety were incorporated into one single compound and evaluated for their in vitro schizontocidal activity against the CQ-sensitive 3D7 strain of Plasmodium falciparum. Compounds with significant in vitro antimalarial activity were further evaluated for cytotoxicity against VERO cell lines. The best active compound 48 exhibited an IC 50 of 1.13 mM. The in vitro results were further validated by quantitative structure-activity relationship (QSAR).

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Synthesis and antimalarial evaluation of 1, 3, 5-trisubstituted pyrazolines

Cited by 130 publications

References 36 publications

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Thermal solvent-free synthesis of chromonyl chalcones, pyrazolines and their in vitro antibacterial, antifungal activities

Novel pyrazole–pyrazoline hybrids endowed with thioamide as antimalarial agents: their synthesis and 3D-QSAR studies

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