Abstract
In this study, a series of twenty-five ring-substituted 4-arylamino-7-chloroquinolinium chlorides were prepared and characterized. The compounds were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts and also primary in vitro screening of the synthesized compounds was performed against mycobacterial species. 4-[(2-Bromophenyl)amino]-7-chloroquinolinium chloride showed high biological activity against M. marinum, M. kansasii, M. smegmatis and 7-chloro-4-[(2-methylphenyl)amino]quinolinium chloride demonstrated noteworthy biological activity against M. smegmatis and M. avium subsp. paratuberculosis. The most effective compounds demonstrated quite low toxicity (LD50 > 20 μmol/L) against the human monocytic leukemia THP-1 cell line within preliminary in vitro cytotoxicity screening. The tested compounds were found to inhibit PET in photosystem II. The PET-inhibiting activity expressed by IC50 value of the most active compound 7-chloro-4-[(3-trifluoromethylphenyl)amino]quinolinium chloride was 27 μmol/L and PET-inhibiting activity of ortho-substituted compounds was significantly lower than this of meta- and para-substituted ones. The structure-activity relationships are discussed for all compounds.
Highlights
IntroductionThe increasing incidences of tuberculosis (TB), the number of cases of multi-drug-resistant strains of Mycobacterium tuberculosis (MDR-TB) and infections by non-tuberculous mycobacteria (NTM)
The increasing incidences of tuberculosis (TB), the number of cases of multi-drug-resistant strains of Mycobacterium tuberculosis (MDR-TB) and infections by non-tuberculous mycobacteria (NTM)that are connected with the increase of the number of immunocompromised patients and evolving resistance mycobacterial species to antimycobacterial chemotherapeutics make the discovery of new molecular scaffolds a priority [1,2,3,4].The genus Mycobacterium consists of a closely related group of fast and slow-growing species, some of which are highly pathogenic
Over 50% of commercially available herbicides act by reversible binding to photosystem II (PS II), a membraneprotein complex in the thylakoid membranes, which catalyses the oxidation of water and the reduction of plastoquinone [34] and thereby inhibit photosynthesis [35,36,37]
Summary
The increasing incidences of tuberculosis (TB), the number of cases of multi-drug-resistant strains of Mycobacterium tuberculosis (MDR-TB) and infections by non-tuberculous mycobacteria (NTM). Various studies were published dealing with understanding the systems for Ser/Thr and Tyr protein phosphorylation in M. tuberculosis and it was found that these kinases appear to regulate diverse processes including cell division and molecular transport These facts can result in research of new antimycobacterials [20,21,22,23,24,25,26]. Over 50% of commercially available herbicides act by reversible binding to photosystem II (PS II), a membraneprotein complex in the thylakoid membranes, which catalyses the oxidation of water and the reduction of plastoquinone [34] and thereby inhibit photosynthesis [35,36,37] Both pharmaceuticals and pesticides are designed to target particular biological functions, and in many cases they target similar processes or have similar molecular sites of action. Preliminary in vitro cytotoxicity screening of the most active derivatives was performed using the human monocytic leukemia THP-1 cell line
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