7- pyrimidine, anticonvulsant

Many patents have been issued on the use of pyrogaUol derivatives as pharmaceuticals. PyrogaUol has been used extemaUy in the form of an ointment or a solution in the treatment of skin diseases, eg, psoriasis, ringworm, and lupus erythematosus. GaUamine triethiodide (16) is an important muscle relaxant in surgery it also is used in convulsive-shock therapy. Trimethoprim (2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine) is an antimicrobial and is a component of Bactrin and Septra. Trimetazidine (l(2,3,4-trimethoxybenzyl)piperazine (Vastarel, Yosimilon) is used as a coronary vasodilator. l,2,3,4-Tetrahydro-6-methoxy-l-(3,4,5-trimethoxyphenyl)-9JT-pyrido[3,4- ]indole hydrochloride is useful as a tranquilizer (52) (see Hypnotics, sedatives, ANTICONVULSANTS, AND ANXIOLYTICS). Substituted indanones made from pyrogaUol trimethyl ether depress the central nervous system (CNS) (53). Tyrosine-and glycine(2,3,4-trihydroxybenzyl)hydrazides are characterized by antidepressant and anti-Parkinson activity (54). 

Methanol, l-isoquinolyl(phenyl)-confonnation, 2, 110 Methanol, pyrimidinyl-synthesis, 3, 113 Methanol, tetrahydropyran-2-yl-microwave spectra, 3, 625 Methantheline as neurotransmitter, 1, 175 therapeutic properties, 3, 882 Methaphenilene biological activity, 4, 911 Methapyrilene biological activity, 4, 911 toxicity, 4, 912 Methaqualone, 3, 150 as anticonvulsant, 1, 166 pyrido[2,3-d]pyrimidine analogues metabolism, 3, 205 as sedative, 1, 166 Metharbitone as anticonvulsant, 1, 166 Methazolamide... 

Adenosine and inosine can be transported across cell membranes in either direction, facilitated by a membrane-associated nucleoside transport protein. Concentrative transporters have also been identified. Messenger RNA for a pyrimidine-selective Na+-nucleoside cotransporter (rCNTl) and a purine-selective Na+-nucleoside cotransporter (rCNT2) are found throughout the rat brain. Most degradation of adenosine is intracellular, as evidenced by the fact that inhibitors of adenosine transport, such as dipyridamole, increase interstitial levels of adenosine. Dipyridamole is used clinically to elevate adenosine in coronary arteries and produce coronary vasodilation. In high doses, dipyridamole can accentuate adenosine-receptor-mediated actions in the CNS, resulting in sedation and sleep, anticonvulsant effects, decreased locomotor activity and decreased neuronal activity. 

A very easy cyclodehydration of the pyrimidine (39) using silicon tetrachloride and base yields the tricyclic adenine derivative (40), a conformationally strained analogue of the anticonvulsant compound BWA78U [95TL4249],... 

Pentobarbital] (pyrimidine trione barbiturate) Synthetic GABAA-R agonist [anaesthetic, anticonvulsant used for euthanasia]... 

Pyrido[2,3-highly active compounds possessing antitumor, antibacterial, and anticonvulsive activities (80CPB761, 80JMC327, 80PHA253). 

SOME PYRIMIDINES OF BIOLOGICAL AND MEDICINAL INTEREST—PART III longer than that of (XXXII) or of carisoprodol. The toxicology is similar to that of (XXXII), with a wide safety margin. Anticonvulsive properties are similar to those of methyl phenobarbital. The substance has depressant... 

Pyrimidine is an important heterocycle with a variety of biological activities. They are closely related to nucleic acids since they are very mueh alike in stmeture to the pyrimidine bases [93]. Perhaps, because of this straetural similarity, eompounds with such heterocycles in their molecular structure were reported as antitumor, interferon inducer, antiviral, antihypertensive, hypoglyeemie, anticonvulsant, antinociceptive, and anti-inflammatoiy agents [94]. 

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