Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling

Author:

Rep Valentina1ORCID,Štulić Rebeka1,Koštrun Sanja2,Kuridža Bojan3,Crnolatac Ivo3,Radić Stojković Marijana3ORCID,Paljetak Hana Čipčić4,Perić Mihaela4,Matijašić Mario4,Raić-Malić Silvana1ORCID

Affiliation:

1. Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Marulićev trg 19, 10000 Zagreb, Croatia

2. Selvita d.o.o, Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia

3. Ruđer Bošković Institute, Division of Organic Chemistry and Biochemistry, Bijenička cesta 54, 10000 Zagreb, Croatia

4. Department for Intercellular Communication, Center for Translational and Clinical Research, University of Zagreb School of Medicine, Šalata 2, 10000 Zagreb, Croatia

Abstract

The most active benzimidazole 15a against E. coli, M. catarrhalis and both sensitive and resistant strains of S. pyogenes showed preference toward AT-rich sites and minor groove binding mode, which was in line with docking studies.

Funder

Hrvatska Zaklada za Znanost

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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