ArticleCurrent medicinal chemistry2026
Side Chain Effects on the Lipophilicity-antimicrobial-toxicity Correlation of Greener 4-Alkoxy/Amino-7-Chloroquinolines.
Article in Current medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- Rational Design of N-2-(7-Chloroquinolin-4-ylamino)ethyl Amides Active Against Chloroquine-Resistant Plasmodium falciparum.Archiv der Pharmazie · 2026Article
- Clean Synthesis of N-4-Alkylamino-7-chloroquinoline Cyclic Imides: Influence of Lipophilicity on Antibacterial and Ecotoxicological Properties.Chemistry & biodiversity · 2026Article
- Effects of 4‑Alkoxy/Amino-7-Chloroquinolines onACS omega · 2025Article
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Authors and funding
9 authors.
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Abstract
backgroundMore robust 4-substituted 7-chloroquinolines have been investigated for their diverse properties. However, there is still no systematic study that correlates the effects of the side chain at the 4-position of chloroquine and hydroxychloroquine derivatives with their lipophilicity, antimicrobial and toxicity properties.
objectiveTo this end, a cleaner and facile approach was planned to obtain nineteen 4- substituted 7-chloroquinolines, whose influence of the substituent group and side chain extension at the 4-position on their properties was studied.
methods4-Alkoxy/amino-7-chloroquinolines were prepared by a nucleophilic aromatic substitution (SNAr) reaction between 4,7-dichloroquinoline and alcohols/amines, evaluated for their
results4-Alkoxy/amino-7-chloroquinolines were obtained in yields ranging from 81 to 100%. The best results showed antimicrobial activity against Pseudomonas aeruginosa for 4-amino-7-chloroquinolines 6-8, with halos greater than 20 mm, and against C. albicans for 4-amino-7-chloroquinolines 1-3, with halos close to 30 mm. A correspondence between Minnow toxicity prediction and
conclusionConsidering the results for compounds 1-3 and 6-8 with greater activity against
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