Anti-Parkinsonian agents

Heterocyclic amines have also been used for aminolysis. Subsequent cyclization of the acylamino amides leads to imidazolones that show a diverse range of biological activities as antibacterial, antifungal, antiviral, antihelmintic, and anti-Parkinsonian agents, as well as central nervous systems (CNS) stimulants. 

Asymmetric hydrogenation of racemic 2-substituted (3-keto esters to produce 2-substituted (3-hydroxy esters with two new chiral centers is a powerful method, and it is useful in the production of other pharmaceutical intermediates. The methodology can be used in the preparation of protected threonine derivatives 34, where 34d and 34e are key intermediates for the anti-Parkinsonian agent, L-Dops (35). 

Hydrogenation of certain racemic 2-substituted 3-oxocarboxylates occurs with high diastereo- and enantioselectivity via dynamic kinetic resolution involving in situ racemization of the substrates. The (R)-BINAP-Ru-catalyzed reaction of 2-acylamino-3-oxocarboxylates in dichloromethane allows preparation of threonine and DOPS (anti-Parkinsonian agent)... 

Anti-parkinsonian agents Beta-sheet breakers peptides... 

As a class, anticholinergics include the antihistamines, atropine and homatropine anti-Parkinsonian agents like benzotropine, procyclidine, and trihexyphenidyl the antimuscarinics of which atropine is the prototype and antispasmodics like dicyclomine and oxybutymin. Most antimuscarinics are amino-alcohols or their derivatives (usually esters or ethers), aminoamides, or other amines. Antimuscarinics can be divided into two groups. These are the naturally occurring alkaloids and their semisynthetic derivatives like atropine, homatropine, scopolamine, and hyoscyamine and the synthetic amine compounds such as anisotropine, dicyclomine, and ipratropium. 

Ethynylnicotine (70) was designed as a potential anti-Parkinsonian agent (9). 

Olney JA, Price MT, Labruyere J et al. (1987). Anti-Parkinsonian agents are phencyclidine agonists and /V-mclLy 1-aspartate antagonists. Eur J Pharmacol, 142, 319-320. 

Tubuloside B (19) significantly attenuated MPP+-induced cytotoxicity, DNA fragmentation and intracellular accumulation of reactive oxygen species (ROS). These results indicated that tubuloside B (19) prevent MPP+-induced apoptosis and oxidative stress and may be applied as an anti-Parkinsonian agent [59]. 

Adamantylamine hydrochloride (Amantadine hydrochloride, Amazolone, Mantadan, Mantadix, Virofral) [665-66-7] M 187.7, m >360° (dec), pK s 10.58. Dissolve the salt in dry EtOH, add a few drops of dry EtOH saturated with HCl gas, followed by dry Et20 to crystallise the hydrochloride out. Dry the salt in a vacuum. Its solubility in H2O is >5 /o and it is solnble in EtOH but insoluble Et20. [Stetter et al. Chem Ber 93 226 19601] It is antiviral and anti-Parkinsonian agent [Komhuber et al.JNeural Transm 46 (Snppl) 399 7995]. 

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