Antiallergic agents

One area of research is the replacement of sulfur with selenium to enhance the potency of organic compounds in pharmaceutical apphcations. This has seldom been successflil and often the toxicity is increased. There are some exceptions, eg, selenazofurin, phenylaminoethyl selenide, ebselen, and selenotifen (64). Selenazofurin is a cytotoxic compound having antitumor properties, phenyl aminoethyl selenide is used to reduce hypertension, ebselen inhibits a variety of inflammatory and tissue damaging reactions, and selenotifen is an antiallergic agent. 

A number of nitronaphthyridines proved to be valuable intermediates in the synthesis of some antibacterial compounds (80CPB235), new bron-cholitators, antiflammatory and antiallergic agents (91MI2 92JMC4866), and harmyrine (56LA233 60JCS1794). 

Carboxylic acid derivatives of heterocycles have proved a source of compounds that show the same allergic mediator release inhibiting activity as sodium cromoglycate. A number of these agents have been taken to the clinic for trial as antiallergic agents. 

A fused pyrazoloquinolone provides an exception to the rule that antiallergic agents must contain a strongly acidic proton. Entry to the ring system is gained by electrocyclic reaction of diazoindolone 124 (possibly obtained by reaction... 

Marshall GD Jr. Therapeutic options in allergic disease Antihistamines as systemic antiallergic agents. J Allergy Clin Immunol 2000 106 S303-S309. 

Mechanism of Action An antiasthmatic and antiallergic agent that prevents mast cell release of histamine, leukotrienes, and slow-reacting substances of anaphylaxis by inhibiting degranulation after contact with antigens. Therapeutic Effect Helps prevent symptoms of asthma, allergic rhinitis, mastocytosis, and exercise-induced bron-chospasm. 

Mechanism of Action An antiallergic agent that selectively antagonizes H, receptor Therapeutic Effect Blocks histamine-associated symptoms of seasonal allergic conjunctivitis. 

From the variety of experimental studies it becomes obvious that mucosal administration is a powerful tool for modulating immune responses. Apart from the importance to test the effectiveness and the mechanisms of action of any allergen of interest as a potential antiallergic agent or tolerogen in animal models, prophylactic treatment strategies could be of interest in patients with a known risk to develop allergy. 

Wang, N., Yao, X., Ishii, R., and Kitanaka, S. Antiallergic agents from natural sources. 3. Structures and inhibitory effects on nitric oxide production and histamine release of five novel polyacetylene glucosides from Bidens parviflora Willd. Chem Pharm Bull (Tokyo), 49(8), 938-942, 2001. 

The oxazolo[4,5-/z]quinolin-2(3//)-ones (89) and 2,5-disubstituted oxazolo[4,5-/i]quinolines (90) were prepared as new antiallergic agents by oxazole ring annelation conducted by condensing 7-amino-8-hydroxyquinoline intermediates with phosgene, o-ester, or imidate reagents (Scheme 7)... 

Figure 2.9 Already three decades ago, the clinical candidate zaprinast 27 (M B 22, 948) and its sulfonamide analog 28 were synthesized. Whereas 27 is about 40 times more active as an antiallergic agent than the standard compound cromoglycate, 28 has a 1000-fold activity. Sildenafil 29 was originally investigated as an antianginal drug, but turned out to support and maintain penile erections.

The uses of thiocoumarins as pharmaceuticals are numerous and include hemorrhagic agents, anticoagulants, antiallergic agents, and... 

Tranilast is an orally active antiallergic agent. It may have a similar mechanism of action to that of cromoglicate. 

Immunologicals are all medicines which are either allergens defined cis products used to identify or provoke a specific modification to acquire an immunological response to an antiallergic agent, or vaccines, toxins or sera defined as all agents used to provoke an active or passive immunity to diagnose the state of immunity. 

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