Quinoline-based drugs

It has been underlined that the antimalarial activity of quinoline-based drugs (quinine, chloroquine, mefloquine) also depend on their interactions with heme, thus preventing aggregation of toxic heme released during proteolysis of hemoglobin by die parasite. In vitro, efficient quinolines block the aggregation... 

Organometallic compounds often show unique catalytic properties that may also allow their use as potential drug candidates. The cyclopentadienyl-ruthenium carbonyl catalyst 75, that bears a quinoline-based bidentate ligand, was found to be a potent inhibitor of certain protein kinases <2006AGE1504>. 

Any perturbation of this heme-detoxification process that is unique to Plasmodium is expected to have drastic consequences for the parasite survival. The inhibition of heme aggregation is the targeted action of conventional quinoline based antimalarial drugs such as quinine, chlmnquine and mefloquine. 

In addition to quinoline-based SARMs, tetrahydroquinoline-derived drug candidates were reported to possess tissue-selective androgen receptor agonist activity. Two representatives are S-40503 and 2-methyl-2-(8-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]chinolin-4-yl)propan-l-ol (Fig. 4.9,12 and 13), and the mass spectrometric behavior was studied for both compounds. The protonated molecule of 13 at m/z 289 dissociates under CID conditions by the loss of a hydroxyl radical (-17 Da) originating from the nitro function. The proton affinity of 1,2,3,4-tetrahydroquinoline was determined as 225 kcal/mol and... 

Walash et al. [10] determined primaquine and other quinoline drugs in bulk and in pharmaceuticals by a titrimetric method. The method is based on reaction with l,3-dibromo-5,5-dimethylhydantoin or TV-bromosuccinimide as the titrant. Primaquine was determined either by usual titration or by potentiometric titration with the brominating agents. The recovery was approximately 100%. The method was simple, precise, and accurate. 

Many drugs based on pyridine derivatives treat symptoms of Parkinson disease. The various pyridine derivatives are bromocriptine 111, an indole-fused quinoline derivative, dexetimide 112, a 4-substituted 1-benzylpiperidine derivative, lisuride 113, an indole-fused quinoline derivative, pergolide 114, another indole-fused quinoline derivative, quinelorane 115, a pyrimidine-fused saturated quinoline derivative, terguride 116, a saturated quinoline derivative, and trihexyphenidyl 117, a 1-substituted piperidine derivative . 

Quinolines represent an important class of heterocycles, and the quinoline skeleton is present in various natural products, especially in alkaloids. Among them quinine is an active ingredient for the treatment of malaria [286]. Despite its relatively low efficacy and tolerability, quinine still plays an important role in the treatment of multiresistant malaria, one of the world s most devastating infectious diseases [287]. Therefore, the design of many drugs and affordable chemotherapies are based upon synthetic quinoline derivatives, such as chloroquine, mefloquine or quinacrine [288-292]. In addition, chimanine alkaloids, are also effective against parasitic diseases such as leishmaniasis and trypanosomiasis [293-295]. Besides,... 

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