Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening

Karad, Sharad C.; Purohit, Vishal B.; Raval, Dipak K.

doi:10.1016/j.ejmech.2014.07.008

Cited by 37 publications

(13 citation statements)

References 36 publications

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“…Karad et al reported the synthesized and anti-tuberculosis activity against M. tuberculosis H37Rv of a novel series of fluoro-substituted pyrazolylpyrazolines. Good anti-tubercular activity was exhibited by compound 362 (96% at 250 mg/mL) [ 262 ]. Mehta et al synthesized a new series of quinazolin-4(3 H )-one derivatives containing a (1,3-diphenyl-1 H -pyrazol-4-yl) core and screened for their anti-tubercular activities.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

“…A novel series of fluoro-substituted pyrazolylpyrazolines were synthesized and screened for their antimalarial activity against Plasmodium falciparum . Compound 483 displayed excellent activity with an IC 50 value of 0.022 µg/mL against P. falciparum stain as compared to quinine IC 50 = 0.268 µg/mL [ 262 ]. A new series of pyrazole derivatives were synthesized and evaluated for their in vivo antimalarial activity against Plasmodium berghei -infected mice and the most active derivatives were further examined for their in vitro antimalarial activity against chloroquine resistant (RKL9) strain of Plasmodium falciparum .…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

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Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…SAR study reveals, the presence of electron withdrawing group (4‐F, 4‐Br) at R 1 position and –CF 3 group at meta position of aryloxy ring illustrated anti‐TB activity. The presence of bromo group at R 1 position and fluoro group at ortho , meta , and para positions of aryloxy ring showed enhanced anti‐TB activity (Fig. ).…”

Section: Pyrazole Derivatives For Treatment Of Tuberculosismentioning

confidence: 95%

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

Keri

Chand

Ramakrishnappa

et al. 2015

Archiv der Pharmazie

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New and reemerging infectious diseases will continue to pose serious global health threats well into the 21st century and according to the World Health Organization report, these are still the leading cause of death among humans worldwide. Among infectious diseases, tuberculosis claims approximately 2 million deaths per year worldwide. Also, agents that reduce the duration and complexity of the current therapy would have a major impact on the overall cure rate. Due to the development of resistance to conventional antibiotics there is a need for new therapeutic strategies to combat Mycobacterium tuberculosis. Subsequently, there is an urgent need for the development of new drug candidates with newer targets and alternative mechanism of action. In this perspective, pyrazole, one of the most important classes of heterocycles, has been the topic of research for thousands of researchers all over the world because of its wide spectrum of biological activities. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we have collated published reports on the pyrazole core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. In this article, the possible structure-activity relationship of pyrazole analogs for designing better antituberculosis (anti-TB) agents has been discussed and is also helpful for new thoughts in the quest for rational designs of more active and less toxic pyrazole-based anti-TB drugs.

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“…In continuation of our efforts to synthesize some novel heterocyclic motifs with biological interest [27][28][29][30][31][32][33][34][35][36][37][38][39][40], herein we report the design, synthesis, antimicrobial evaluation, cytotoxicity and genotoxicity of quinoline based 1,2,4-oxadiazole scaffold. Potent 1,2,4-oxadiazole moiety is linked to quinoline moiety at C-3 position to observe the synergistic effect of these rings towards antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%