947-95-5Relevant articles and documents
Synthesis and biological evaluation of novel triazole substituted pyrazolyl-methylenehydrazinyl-5-arylidene thiazolidinone derivatives as antibacterial and cytotoxic agents
Pogaku, Vinay,Eslavath, Ravi Kumar,Dayakar,Singh, Surya S.,Basavoju, Srinivas
, p. 6079 - 6098 (2017)
Novel triazole substituted pyrazolyl-methylenehydrazinyl-5-arylidene thiazolidinone derivatives 6a–n and 7a–l were synthesized and characterized by Fourier transform infrared, 1H and 13C nuclear magnetic resonance, mass spectrometry and elemental (CHN) analysis. The in vitro antibacterial (6a–n and 7a–l) and cytotoxic (6a–n) activities were evaluated for these compounds. The results revealed that the compounds 6b, 6i, 6k, 7b, 7h displayed good antibacterial activity. The compounds 6c (IC50?=?5.4?μM), 6l (IC50?=?6.3?μM) and 6f (IC50?=?9.85?μM) were effective for inhibition of human breast cancer cell line MCF-7. Similarly, the compounds 6b (IC50?=?8.7?μM) and 6c (IC50?=?9.06?μM) were shown to have effective inhibition on human cervical cancer cell line Hela.
Bipyrazole-based palladium(II) complexes as DNA intercalator and artificial metallonuclease
Thakor, Khyati P.,Lunagariya, Miral V.,Bhatt, Bhupesh S.,Patel, Mohan N.
, p. 233 - 245 (2019)
Abstract: Substituted 3′-methyl-1′,2-diphenyl-3,4-dihydro-1′H,2H-3,4′-bipyrazole and their square planar palladium(II) complexes of type [Pd(4n)Cl2], where 4n = bipyrazole-based ligands, have been synthesized. The compounds have been characterized by various techniques like elemental analysis, mass, absorption, IR, 1H NMR and 13C NMR spectroscopy. The complexes have been further analyzed by thermogravimetric analysis (TGA), conductance measurement and energy-dispersive X-ray spectroscopy (EDX). Interaction between compounds and herring sperm DNA has been studied by absorption titration, viscosity measurement, ethidium bromide displacement titration, and molecular docking study. The binding strength between compounds and DNA has been checked in terms of Kb, Ksv, and Kf values; while spontaneity of interaction has been checked by evaluating thermodynamic parameters like Gibb’s free energy, enthalpy change (?H°) and entropy change (?S°). The plasmid cleavage efficacy of complexes has been evaluated by gel electrophoresis technique. The minimum inhibitory concentration of compounds has been evaluated against pathogens such as Staphylococcus aureus, Escherichia coli, B. subtilis, S. marcescens and Pseudomonas aeruginosa. The in vivo and in vitro cytotoxic activity has been performed using cell viability assay and brine shrimp lethality bioassay. Graphical abstract: [Figure not available: see fulltext.].
Microwave assisted one-pot synthetic route to imidazo[1,2-: A] pyrimidine derivatives of imidazo/triazole clubbed pyrazole and their pharmacological screening
Prasad, Pratibha,Kalola, Anirudhdha G.,Patel, Manish P.
, p. 12666 - 12676 (2018)
An efficient synthesis of imidazo[1,2-a]pyrimidine derivatives of pyrazole in excellent yield over a short reaction time based on a microwave-assisted, one-pot three-component condensation reaction of pyrazole aldehyde clubbed with imidazole 4 and triazole 5 nuclei, (substituted-phenyl/hetero-aryl)ethanones 6(a-g), and 2-amino benzimidazole 7 in the presence of the strong base KOH is described. All the compounds were screened for their preliminary in vitro antimicrobial, antituberculosis and antimalarial activities against a panel of pathogenic strains. The majority of the compounds exhibited excellent inhibitory action against S. typhi, S. pneumoniae, B. subtilis, and C. tetani. Some of the compounds showed good antifungal activity and moderate antituberculosis activity as compared to first line drugs. Two of the compounds 8b and 9b exhibited excellent antimalarial activity against P. falciparum strains.
Design, synthesis, antibacterial evaluation and molecular docking studies of novel pyrazole/1,2,4-oxadiazole conjugate ester derivatives
Depa, Navaneetha,Erothu, Harikrishna
, p. 1087 - 1098 (2021/02/26)
The development of new antimicrobial drugs is most needed due to rapid growth in global antimicrobial resistance. Thus, in this context, a series of novel pyrazole/1,2,4-oxadiazole conjugate ester derivatives (7a–j) was synthesized. All the derivatives we
Design and synthesis of pyrazolone-based compounds as potent blockers of SARS-CoV-2 viral entry into the host cells
Karpoormath, Rajshekhar,Kehinde, Idowu,Kushwaha, Babita,Kushwaha, Narva Deshwar,Mahlalela, Mavela Cleopus,Obakachi, Vincent A.,Shinde, Suraj Raosaheb
, (2021/06/16)
SARS-CoV-2 are enveloped positive-stranded RNA viruses that replicate in the cytoplasm. It relies on the fusion of their envelope with the host cell membrane to deliver their nucleocapsid into the host cell. The spike glycoprotein (S) mediates virus entry into cells via the human Angiotensin-converting enzyme 2 (hACE2) protein located on many cell types and tissues' outer surface. This study, therefore, aimed to design and synthesize novel pyrazolone-based compounds as potential inhibitors that would interrupt the interaction between the viral spike protein and the host cell receptor to prevent SARS-CoV 2 entrance into the cell. A series of pyrazolone compounds as potential SARS-CoV-2 inhibitors were designed and synthesized. Employing computational techniques, the inhibitory potentials of the designed compounds against both spike protein and hACE2 were evaluated. Results of the binding free energy from the in-silico analysis, showed that three compounds (7i, 7k and 8f) and six compounds (7b, 7h, 7k, 8d, 8g, and 8h) showed higher and better binding high affinity to SARS-CoV-2 Sgp and hACE-2, respectively compared to the standard drugs cefoperazone (CFZ) and MLN-4760. Furthermore, the outcome of the structural analysis of the two proteins upon binding of the inhibitors showed that the two proteins (SARS-CoV-2 Sgp and hACE-2) were stable, and the structural integrity of the proteins was not compromised. This study suggests pyrazolone-based compounds might be potent blockers of the viral entry into the host cells.
