EVALUATION OF A GROUP OF PYRROLE DERIVATIVES AS TUBERCULOSTATIC AGENTS

Maya Georgieva; Diana Tzankova; Stanislava Vladimirova; Atanas Bijev

doi:10.12955/cbup.v5.1075

Maya Georgieva Medical University, Faculty of Pharmacy, Sofia, Bulgaria
Diana Tzankova Medical University, Faculty of Pharmacy, Sofia, Bulgaria
Stanislava Vladimirova University of Chemical Technology and Metallurgy, Sofia, Bulgaria
Atanas Bijev University of Chemical Technology and Metallurgy, Sofia, Bulgaria

DOI: https://doi.org/10.12955/cbup.v5.1075

Keywords: pyrrole-derivatives, pharmacophore, drug-likeness, tuberculostatic

Abstract

: This research aims to contribute to the global search for more effective tuberculostatics that has been triggered by recent outbreaks of tuberculosis. A group of pyrrole-containing derivatives are designed and theoretically elucidated. The identification of the pharmacophore group using the PharmaGist webserver is attempted. Also, the corresponding drug-like properties of the tested compounds are evaluated, together with their possible toxicity risks. The pharmacokinetic behavior of the structures is predicted, based on the Lipinski’s Rule of Five. The effects of some structural parameters are tested. In addition, in vitro evaluations of the anti-tubercular activity against Mycobacterium tuberculosis H₃₇Rv are performed, with compound GA-9 registering the highest activity.

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