Indole derivatives drugs derived from

Longeon, A., Copp, B. R., Quevrain, E., Roue, M., Kientz, B., Cresteil, T., Petek, S., Debitus, G, and Kondracki, M. L. B. (2011). Bioactive indole derivatives from the south pacific marine sponges. Mar. Drugs 9, 879-888. 

Discriminative stimulus effect. Rhesus monkeys, trained to discriminate A-9-THC from vehicle in a two-lever drug discrimination procedure, were tested with a variety of psychoactive drugs, including cannabinoids or drugs from other classes. The results indicated that A-9-THC discrimination showed pharmacological specificity, in that none of the noncannabinoid drugs fully substituted for A-9-THC. The classical cannabinoids, A-9-THC and A-8-THC, and the novel cannabinoids, WIN and l-butyl-2-methyl-3-(l-naphthoyl)indole, produced full dose-dependent substitution for A-9-THC in all monkeys. A heptyl indole derivative failed to substitute for A-9-THC, but it also did not displace pH] CP-55,940 from its binding site . ... 

Apart from academic interest in its synthesis and properties, most of the work on indolizine has been concerned with the search for drugs (e.g., synthesis of indolizine analogs of indole derivatives which are widely distributed in nature), for dyestuffs, and for light-screening agents in photographic emulsions. 

Sertindole. This is structurally unique among the atypical neuroleptics in that it is an indole derivative with a high affinity for 5-HT2A, D2-like (Dj, D3, D4) and also alpha-1 receptors. The antagonistic action on the 5-HT2 receptors probably accounts for its beneficial effects on negative symptoms. Sertindole was suspended from marketing a few years ago because of the rare occurrence of cardiac conduction defects. As the causal relationship of this adverse effect to the drug was never firmly established it is likely to be relaunched in the near future. 

The biosynthetic pathway for ajmaline in R. serpentina is one of the best-characterized terpenoid indole alkaloid pathways. Much of this progress has been detailed in a recent extensive review (78). Like all other terpenoid indole alkaloids, ajmaline, an antiarrhythmic drug with potent sodium channel-blocking properties (79), is derived from deglycosylated strictosidine (Fig. 2c). 

CAS 520-53-6. C8H5N(OH)C2H4N(CH3)2. An indole derivative. An alkaloid from certain mushrooms a hallucinogenic drug. 

One of the most fascinating products containing multiple components is a combination of the natural product reserpine, hydralazine hydrochloride, and hydrochlorothiazide. This drug product is available in tablet form and contains 0.1 mg of reserpine USP, 25 mg of hydralazine hydrochloride, and 15 mg of hydrochlorothiazide (Fig. 6). Reserpine is an indole alkaloid derived from the dried root of Rauwolfia serpentina and is well known for its complex molecular architecture, the challenges faced during its total synthesis, and its profound effect on the central nervous system as an antihypertensive. Hydralazine is also an antihypertensive and hydrochlorothiazide has diuretic properties. The combination of these three very different molecular structures brings diversity to the analytical testing required. 

Indoles are an important class of fine chemicals derivatives find application as fragrance chemicals. The indole nucleus is present in many biologically active molecules including plant-growth regulators, proteins and pharmaceuticals. The selective synthesis of indole derivatives constitutes an important area of drug research. The well-known Fischer indole synthesis provides a versatile method for synthesizing substituted indoles from the arylhydrazones of aldehydes or ketones... 

Statins can be classified as natural statins and synthetic statins. Lavastatin, simvastatin, and pravastatin are the first three natural statins to reach the market. Lavastatin and pravastatin are natural products isolated from fermentation broths, while simvastatin is a semisynthetic statin derived from lavastatin. Fluvastin was the first truly synthetic statin brought to the market by Sandoz pharmaceutical company (now part of Novartis), and it was obtained by replacing the hexahydro-naphthalene core stiucture of the natural statins with the indole nucleus [5]. It was the discovery of fluvastin that opened up the opportunity of more potent synthetic statins including atorvastatin, the most prescribed drug in the world. 

Cmchona alkaloids. Indole alkaloids (cinchonamine group) and quinoline alkaloids (cinchonine group), only the latter group is of therapeutic significance. C. a. are isolated from Cinchona bark (Jesuit s bark Cin-chonae cortex). The name is derived from the Indian word quina (bark). The drug consists of the dried tube... 

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