10.6084/m9.figshare.5539888.v1
Anda-Mihaela Olaru
Anda-Mihaela
Olaru
Violeta Vasilache
Violeta
Vasilache
Ramona Danac
Ramona
Danac
Ionel I. Mangalagiu
Ionel
I. Mangalagiu
Antimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VII<sup>8–12</sup>
Taylor & Francis Group
2017
Antimycobacterial
indolizine
pyridinium salts
ADMET
2017-10-26 10:49:54
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/Antimycobacterial_activity_of_nitrogen_heterocycles_derivatives_7-_pyridine-4-yl_-indolizine_derivatives_Part_VII_sup_8_12_sup_/5539888
<p>A series of 13 compounds having a monoindolizine mono-salt skeleton was designed and synthesised in order to evaluate their antimycobacterial activity. The synthesis is efficient, involving only three steps: two alkylations and one 3 + 2 dipolar cycloaddition. The antimicrobial activity against <i>Mycobacterium tuberculosis</i> H37Rv grown under aerobic conditions was evaluated, eight compounds showing a very good antimycobacterial activity. SAR correlation reveals a certain influence of the R substituent from the <i>para</i> position of benzoyl moiety at position 3 of indolizine. The most active five compounds passed the second stage of anti-TB testing, the assay demonstrating that they are potent against both replicating and non-replicating <i>Mtb</i>, have a bactericidal mechanism of action, are active against drug-resistant <i>Mtb</i> strains, present a moderate to good activity against nontuberculous mycobacteria, a good intracellular activity, and a moderate to high cytotoxicity. For one compound showing a promising anti-TB profile, a complete ADMET study has been performed.</p>