Synthesis, Antitumor and Antimicrobial Activities of Some Novel 1-(Substituted)-3-Methyl-1<i>H</i>-Pyrazol-5(4<i>H</i>)-One

Abstract

Several 1-(substituted)-3-methyl-1H-pyrazol-5(4H)-one as RA1-RA9 were synthesized and compounds were screened for antitumor activity against Ehrlich ascites carcinoma (EAC) cells and antimicrobial activity. Elemental analysis, mass spectral data, 1H-NMR, and IR confirmed the structure of the newly synthesized compounds. Some of the tested compounds showed good antitumor and antimicrobial activity. Compounds RA1, RA4, and RA9 exhibit highest antitumor activity against EAC cells in comparison with 5-flurouracil as standard drug.Keywords: Ehrlich ascites carcinoma; Pyrazolone; Antitumor; N-substitution; Antimicrobial.© 2012 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v4i1.7027 J. Sci. Res. 4 (1), 183-192 (2012)

One-pot synthesis of 4,4ʹ-(arylmethylene)-bis-(3-methyl-1-phenyl-1H-pyrazol-5-ols) catalyzed by Brönsted acidic ionic liquid supported on nanoporous Na+-montmorillonite

“…Pyrazoles are important classes of heterocyclic compounds that occur widely in the pharmaceutical industry. For example, compounds containing 2,4-dihydro-3H-pyrazol-3-one structural motif, including 4,4 -(arylmethylene)-bis-(1H-pyrazol-5-ols), have attracted an interest because they exhibit a wide range of biological activities such as antimalarial [1], antifungal [2], anti-inflammatory [3], antimicrobial [4], antinociceptive [5], analgesic [6], fungicide [7] and antitumor [8] activities. Additionally, they are applied as important intermediates in organic synthesis [9] and as bis-Schiff bases [10].…”

Sulfonated nanohydroxyapatite functionalized with 2-aminoethyl dihydrogen phosphate (HAP@AEPH2-SO3H) as a new recyclable and eco-friendly catalyst for rapid one-pot synthesis of 4,4′-(aryl methylene)bis(3-methyl-1H-pyrazol-5-ol)s

“…4,4 0 -(Aryl methylene)bis(1H-pyrazol-5-ol)s, an important class of heterocyclic compounds, have exhibited a wide range of biological activities such as antimalarial, 1 antifungal, 2 anti-inammatory, 3 antimicrobial, 4 antinociceptive, 5 antiviral, 6 and antitumor 7 activities. Also, they are used as pesticides, 8 fungicides, 9 analgesics, 10 important intermediates in organic synthesis, 11 bis-Schiff bases 12 and ligands.…”