Journal ArticleDOI
Synthesis, and antitubercular and antimicrobial activity of 1′-(4-chlorophenyl)pyrazole containing 3,5-disubstituted pyrazoline derivatives
N. Harikrishna,Arun M. Isloor,Arun M. Isloor,K. Ananda,Abdulrahman Obaid,Hoong-Kun Fun,Hoong-Kun Fun +6 more
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TLDR
In this paper, a series of 1′-(4-chlorophenyl)-5-(substituted aryl)-3,4-dihydro-2H,1′H-[3, 4]]-bipyrazolyl derivatives (6a−e, 8a-e, 10a−E, 10e−E) have been synthesized, characterized and screened for antimicrobial and antitubercular activity.Abstract:
A new series of 1′-(4-chlorophenyl)-5-(substituted aryl)-3′-(substituted aryl)-3,4-dihydro-2H,1′H-[3,4′]bipyrazolyl derivatives (6a–e, 8a–e, 10a–e) have been synthesized, characterized and screened for antimicrobial and antitubercular activity. Among the synthesized compounds, the minimum inhibition concentration of 10e was found to be as low as 1.56 μg ml−1 and that of 10c was 6.25 μg ml−1 as compared to the standard anti-tb drugs pyrazinamide and streptomycin.read more
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Recent advancements in the development of bioactive pyrazoline derivatives.
Bhupender Nehra,Sandeep Rulhania,Shalini Jaswal,Bhupinder Kumar,Gurpreet Singh,Vikramdeep Monga +5 more
TL;DR: This review aims to summarizes various recent advancements in the medicinal chemistry of pyrazoline based compounds to afford ideas for the design and development of novel compounds with desired therapeutic implications.
Journal ArticleDOI
Correction: The first computational study for the oxidative aromatization of pyrazolines and 1,4-dihydropyridines using 1,2,4-triazolinediones: an anomeric-based oxidation
TL;DR: The first computational study for the oxidative aromatization of pyrazolines and 1-4-dihydropyridines using 1,2,4-triazolinediones was performed by Mahya Kiafar et al. as discussed by the authors.
Journal ArticleDOI
New chalcone-type compounds and 2-pyrazoline derivatives: synthesis and caspase-dependent anticancer activity.
Mohamed I Chouiter,Houssem Boulebd,David M. Pereira,Patrícia Valentão,Paula B. Andrade,Ali Belfaitah,Artur Silva +6 more
TL;DR: Chalcones 1-3 have been identified as new and promising anticancer agents toward the AGS cell line, and Mechanistic studies showed that these compounds trigger loss of cell viability and mitochondrial membrane potential, while eliciting morphological traits compatible with regulated cell death, which was ultimately shown to derive from caspase activation.
Journal ArticleDOI
Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities
TL;DR: In this article, the synthesis of new compounds with antimicrobial and antiviral properties is a central objective today in the context of the COVID-19 pandemic, and the methods of synthesis of these hybrids, the antimicrobial activities of the compounds, their correlation with various groups present on the molecule, as well as their pharmaceutical properties.
Journal ArticleDOI
Identification and development of pyrazolo[4,3-c]pyridine carboxamides as Mycobacterium tuberculosis pantothenate synthetase inhibitors
Suresh Amaroju,Mahalakshmi Naidu Kalaga,Singireddi Srinivasarao,Agnieszka Napiórkowska,Ewa Augustynowicz-Kopeć,Sankaranarayanan Murugesan,Subhash Chander,Rangan Krishnan,Kondapalli Venkata Gowri Chandra Sekhar +8 more
TL;DR: Among the compounds, 7d was found to be the most active compound with IC50 1.01 ± 0.32 μM against MTB PS; it inhibited MTB with MIC 24.72 μM and it was non-cytotoxic at 50 μM in the RAW 267 cell line.
References
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Journal ArticleDOI
Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-furyl)-pyrazoline derivatives.
TL;DR: Anticonvulsant activities of the compounds were determined by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (metrazol) (scMet.) tests, neurotoxicities was determined by rotarod toxicity test on albino mice.
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Synthesis of novel pyrazole derivatives and evaluation of their antidepressant and anticonvulsant activities
TL;DR: Substituted carboxylic acid hydrazides 1a-d reacted with ethenetetracarbonitril 2 in dimethyl formamide with the formation of diacylhydrazines 4a- d and 5-amino-1-substituting pyrazole-3,3,4-tricarbonitriles 5a-D, and exhibited remarkable protective effect against clonic seizures induced by i.p. injection of PTZ.
Journal ArticleDOI
Synthesis and antidepressant activities of some 3,5-diphenyl-2-pyrazolines.
TL;DR: It was found that 4-methoxy and 4-chloro substituent on the phenyl ring at position 3 of the pyrazoline ring increased the antidepressant activity; the replacement of these groups by bromo and methyl substituents decreased activity in mice.
Journal ArticleDOI
New drug candidates and therapeutic targets for tuberculosis therapy
TL;DR: The increasing emergence of drug resistance and the problem of mycobacterial persistence highlight the need to develop novel TB drugs that are active against drug resistant bacteria but, more importantly, kill persistent bacteria and shorten the length of treatment.
Journal ArticleDOI
Synthesis and anticancer activity of acyl thioureas bearing pyrazole moiety
TL;DR: Results confirm that novel pyrazolyl acyl thioureas derived compounds may be utilized for cancer treatment and have a great potential and significance for further investigations.
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