- ANTIBIOTIC COMPOSITIONS
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The present disclosure relates to compounds having antimicrobial activity, compositions comprising said compounds in combination with β-lactam antibiotics, and methods of using the compounds and compositions.
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Page/Page column 0139; 0143
(2017/09/02)
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- Structure-Activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating mycobacterium tuberculosis
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Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDRTB) strains. New anti-TB drugs are urgently required to shorten the long 6-12 month treatment regimen and to battle drug-resistant Mtb strains. We have identified several potent quinoline-based anti-TB compounds, bearing an isoxazole containing side-chain. The most potent compounds, 7g and 13, exhibited submicromolar activity against the replicating bacteria (R-TB), with minimum inhibitory concentrations (MICs) of 0.77 and 0.95 μM, respectively. In general, these compounds also had micromolar activity against the nonreplicating persistent bacteria (NRP-TB) and did not show toxicity on Vero cells up to 128 μM concentration. Compounds 7g and 13 were shown to retain their anti-TB activity against rifampin, isoniazid, and streptomycin resistant Mtb strains. The results suggest that quinoline-isoxazole-based anti-TB compounds are promising leads for new TB drug development.
- Lilienkampf, Annamaria,Jialin, Mao,Baojie, Wan,Yuehong, Wang,Franzblau, Scott G.,Kozikowski, Alan P.
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supporting information; experimental part
p. 2109 - 2118
(2009/12/31)
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- Trifluoromethyl substituted analogs of quinine and quinidine
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Trifluoromethyl substituted analogs of quinine and quinidine are prepared by reacting a 4-quinolyllithium compound with a 4,5-erythro-5-ethyl-(or vinyl)-quinuclidine-2 ξ-carboxaldehyde or the corresponding quinuclidine-2 ξ-carboxylic acid alkyl ester. The end products are useful as antimalarial agents.
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