title: Design, synthesis and biological potentials of novel tetrahydroimidazo[1,2-a]pyrimidine derivatives.
abstract: BACKGROUND
  A novel series of 5-(substituted aldehyde)-7-methyl-3-oxo-N-phenyl-2-((3,4,5,6-tetrahydroxytetrahydro-2H-pyran-2-yl)methylene)-1,2,3,5-tetrahydroimidazo[1,2-a]pyrimidine-6-carboxamide analogues (1-24) was synthesized using the Biginelli condensation.
  
  
  CONCLUSIONS
  The synthesized compounds were screened for their in vitro antimicrobial potential against Gram (positive and negative) bacterial and fungal strains by tube dilution technique. In the series, compound15exhibited significant antimicrobial activity againstCandida albicansandAspergillus nigerwith MIC value = 1.04 × 10-2µM/ml and compound2was found to be most active antioxidant agent with IC50value = 46.31 using DPPH assay. Anticancer activity results indicated that compound23displayed better anticancer activity against human breast cancer cell line (MCF-7) with GI50value = 34.78 using SRB assay.
  
  
  CONCLUSIONS
  All synthesized derivatives exhibited good antimicrobial, antioxidant and anticancer activity using specific method and compared with standard drugs, especially compounds2, 15and23displayed more activity than reference drugs. Structure activity relationship demonstrated that presence of electron releasing groups of the synthesized compounds enhanced the antibacterial activity againstEscherichia colias well as antioxidant activity and electron withdrawing groups improved the antimicrobial as well as anticancer activity against human breast (MCF-7) cancer cell line.
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana 124001 India.
authors.forename: Jyoti
authors.initials: J
authors.lastname: Rani
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana 124001 India.
authors.forename: Monika
authors.initials: M
authors.lastname: Saini
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana 124001 India.
authors.forename: Sanjiv
authors.initials: S
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana 124001 India.
authors.forename: Prabhakar Kumar
authors.initials: PK
authors.lastname: Verma
keywords: Antimicrobial; Antioxidant and anticancer activity; Pyrimidine derivatives