Synthesis, Physico-chemical Characterization, Crystal Structure and Influence on Microbial and Tumor Cells of Some Co(II) Complexes with 5,7-Dimethyl-1,2,4-triazolo[1,5-a]pyrimidine.

Luminiţa Măruţescu,Larisa Calu,Constantin-Gabriel Daniliuc,Rodica Olar,Coralia Bleotu,Mihaela Badea,Denisa Fălcescu,Crina Maria Kamerzan,Mariana Carmen Chifiriuc

doi:10.3390/molecules22071233

Luminiţa Măruţescu, Larisa Calu + Show 7 more

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https://doi.org/10.3390/molecules22071233

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Abstract

Three complexes, namely [Co(dmtp)2(OH2)4][CoCl4] (1), [Co(dmtp)2Cl2] (2) and [Co(dmtp)2(OH2)4]Cl2∙2H2O (3) (dmtp: 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine), were synthesized and characterized by spectral (IR, UV-Vis-NIR), and magnetic measurements at room temperature, as well as single crystal X-ray diffraction. Complex (1) crystallizes in monoclinic system (space group C2/c), complex (2) adopts an orthorhombic system (space group Pbca), and complex (3) crystallizes in triclinic system (space group P). Various types of extended hydrogen bonds and π–π interactions provide a supramolecular architecture for all complexes. All species were evaluated for antimicrobial activity towards planktonic and biofilm-embedded microbial cells and influence on HEp-2 cell viability, cellular cycle and gene expression.

Highlights

The rapid selection of resistance after antibiotic and cytostatic drug treatment represents an emerging and acute health problem at a global level
Some triazolopyrimidines linked with a disubstituted pyrazole ring showed promising anti-tuberculostatic activity [7], while derivatives substituted with trifluoromethyl, aryl and aliphatic amines exhibited good activity against chloroquine-resistant
Concerning the antimicrobial activity, the results demonstrated that complex 2 exhibited the most significant antimicrobial activity against planktonic cells and the most intensive anti-biofilm effect, even at subinhibitory concentrations, having potential applications for the development of novel antimicrobial materials or strategies for fighting medical biofilm pathogens frequently implicated in the etiology of chronic infections

Summary

Introduction

The rapid selection of resistance after antibiotic and cytostatic drug treatment represents an emerging and acute health problem at a global level. In order to overcome this challenging problem of increasing antimicrobial resistance, there is an urgent need to design new antimicrobials with better activity profiles and lower toxicity. Derivatives bearing [1,2,4]-triazolo[1,5-a]pyrimidine fused ring systems have been widely investigated for the design of new drugs in view of the similarity of their chemical structure. Molecules 2017, 22, 1233 with that of the purine nucleobases, i.e., adenine and guanine. Such derivatives are interesting from both biological and chemical perspectives. Some triazolopyrimidines linked with a disubstituted pyrazole ring showed promising anti-tuberculostatic activity [7], while derivatives substituted with trifluoromethyl, aryl and aliphatic amines exhibited good activity against chloroquine-resistant

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