title: Novel pyrazole derivatives with oxa/thiadiazolyl, pyrazolyl moieties and pyrazolo[4,3-d]-pyrimidine derivatives as potential antimicrobial and anticancer agents.
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.
authors.affiliation: 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.
authors.forename: Hend N
authors.initials: HN
authors.lastname: Hafez
authors.affiliation: 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.
authors.forename: Abdel-Rhman B A
authors.initials: ABA
authors.lastname: El-Gazzar
authors.affiliation: Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), College of Science, Department of Chemistry, P.O. Box: 90950, Riyadh 11623, Saudi Arabia.
authors.forename: Sami A
authors.initials: SA
authors.lastname: Al-Hussain
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D011720:Pyrazoles
keywords: Anticancer activities; Antimicrobial; Pyrazolo[4,3-d]pyrimidin; Pyrazolotetrazolopyrimidine