42212-19-1

Upstream product

• 372-09-8 cyanoacetic acid 
• 1007-36-9 1-methyl-3-phenylurea 
• 72702-74-0 N-cyanoacetyl-N-methyl-N'-phenyl-urea 
• 15837-45-3 6-amino-1-phenyluracil 
• 77-78-1 dimethyl sulfate 

Downstream Products

• 132373-30-9 3-(6-Amino-3-methyl-2,4-dioxo-1-phenyl-1,2,3,4-tetrahydro-pyrimidin-5-yl)-3-oxo-propionitrile 
• 87166-62-9 6-amino-5-formyl-3-methyl-1-phenyluracil 
• 87166-65-2 3,6-Dimethyl-1,8-diphenyl-1H,8H-1,3,6,8,9-pentaaza-anthracene-2,4,5,7-tetraone 
• 70371-54-9 5-amino-3-methyl-7-methylthio-1-phenylpyrimido<4,5-d>pyrimidine-2,4(1H,3H)-dione 
• 126080-36-2 6-amino-5-(N-methyliminomethyl)uracil 
• 126080-35-1 6-amino-5-iminomethyluracil 
• 111089-73-7 3,7-dimethyl-2,4-dioxo-1-phenyl-1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidine-5-carboxylic acid ethyl ester 
• 53727-29-0 1-phenyl-3-methyl-barbituric acid 
• 50786-93-1 5,6-diamino-3-methyl-1-phenyluracil 

Relevant academic research and scientific papers

Synthesis and biological evaluation of CX-659S and its related compounds for their inhibitory effects on the delayed-type hypersensitivity reaction

In order to find novel nonsteroidal compounds possessing an inhibitory activity against delayed-type hypersensitivity (DTH) reactions, we conducted random screening using a picryl chloride (PC)-induced contact hypersensitivity reaction (CHR) in mice, and found compound 1 as a lead compound. Then we synthesized and evaluated an extensive series of 5-carboxamidouracil derivatives focused on both the uracil and the antioxidative moieties. Among them, we found that the hindered phenol moiety was necessary to exhibit the activities; especially, compounds 28a-28c having the partial structure of vitamin E were found to exert potent activities against the DTH reaction by both oral and topical administration. And compound 28c showed antioxidative activity against lipid peroxidation with an IC50 of 5.9μM. Compound 28c (CX-659S) was chosen as a candidate drug for the treatment of cutaneous disorders such as atopic dermatitis and allergic contact dermatitis. Copyright (C) 2000 Elsevier Science Ltd.

Structure-activity relationships in a series of xanthine derivatives with antibronchoconstrictory and bronchodilatory activities

Thirty-one 1,3,7,8-substituted xanthine derivatives have been synthesized and evaluated for bronchodilator and anti-bronchoconstrictory activities in in vitro tracheal relaxation and in vivo bronchospasm inhibition models. Activity tests have been complemented with phosphodiesterase inhibition and toxicological data. Structure-activity relationships are discussed. Compound 21 (1,3-diisobutyl-8-methylxanthine) has been selected for further pharmacological development because of its good activity profile and favourable therapeutic index, which is 14- and 38-fold greater than that of theophylline and IBMX, respectively.

Xanthine derivatives

Compounds of the formula STR1 or physiologically acceptable salts thereof in which formula R1 is methyl, ethyl or n-propyl, R2 is methyl or n-propyl and R3 is STR2 methods for the preparation thereof; intermediates useful for their preparation; pharmaceutical preparations containing at least one of these compounds; and the use thereof in the treatment of allergy and bronchial asthma.