2. Academic Validation
  3. Novel pyrazole derivatives with oxa/thiadiazolyl, pyrazolyl moieties and pyrazolo[4,3-d]-pyrimidine derivatives as potential antimicrobial and anticancer agents

Novel pyrazole derivatives with oxa/thiadiazolyl, pyrazolyl moieties and pyrazolo[4,3-d]-pyrimidine derivatives as potential antimicrobial and anticancer agents

  • Bioorg Med Chem Lett. 2016 May 15;26(10):2428-2433. doi: 10.1016/j.bmcl.2016.03.117.
Hend N Hafez 1,  Abdel-Rhman B A El-Gazzar 1,  Sami A Al-Hussain 2
Affiliations

Affiliations

  • 1 Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), College of Science, Department of Chemistry, P.O. Box: 90950, Riyadh 11623, Saudi Arabia; Photochemistry Department (Heterocyclic & Nucleosides Unit), National Research Centre, Dokki, Giza 12622, Egypt.
  • 2 Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), College of Science, Department of Chemistry, P.O. Box: 90950, Riyadh 11623, Saudi Arabia.
PMID: 27080187 DOI: 10.1016/j.bmcl.2016.03.117
Abstract

A series of [4-amino-3-(4-chlorophenyl)-1H-pyrazol-5-yl](3,5-dimethyl-1H-pyrazol-1-yl)-methanone and 6-amino-3-(4-chlorophenyl)-5-methyl-1,6-dihydro-7H-pyrazolo[4,3-d]-pyrimidin-7-one have been synthesized from ethyl 4-amino-3-(4-chlorophenyl)-pyrazol-5-carboxylate. The newly synthesized compounds were characterized by IR, (1)H NMR, (13)CNMR, Mass spectra and Elemental analysis. The compounds were evaluated for their in vitro antimicrobial and Anticancer activity. Among the synthesized compounds, compounds 7a,b and 15 exhibited higher Anticancer activity than the doxorubicin as reference drug. Most of the newly synthesized compounds have good to excellent antimicrobial activity.

Keywords

Anticancer activities; Antimicrobial; Pyrazolo[4,3-d]pyrimidin; Pyrazolotetrazolopyrimidine.

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