Novel orally active inhibitors of passive cutaneous anaphylaxis in rats: N-[2-(4-pyridinyl)-4-pyrimidinyl]ureas and dialkyl [[[2-(4-pyridinyl)-4-pyrimidinyl]amino]methylene]malonates.
4-Chloro-2-(4-pyridinyl)pyrimidines were treated with alkylamines to afford the corresponding N-substituted amino derivatives. 4-Amino-2-(4-pyridinyl)pyrimidines and their N-substituted analogues were converted to amides, carbamates, aminomethylenemalonates, and ureas. Many of these compounds were found to have potential antiallergic activity as indicated by the rat passive cutaneous anaphylaxis screen. The most compounds were found in the last two series.
D000284:Administration, Oral; D000818:Animals; D001491:Basophils / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D006636:Histamine Release / Q000187:drug effects; D007073:Immunoglobulin E / Q000502:physiology; D066298:In Vitro Techniques; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D011725:Pyridines; D011743:Pyrimidines; D007073:Immunoglobulin E