36397-23-6Relevant articles and documents
Compound 48/80. Structure activity relations and poly THIQ, a new, more potent analog
Read,Kiefer,Weber
, p. 1292 - 1295 (1973)
Derivatives of p methoxyphenethylmethylamine were synthesized from which formaldehyde copolymers analogous to compound 48/80 were prepared. Measurement of the hypotensive activity of these analogs revealed that potency was not enhanced by changing the group in the para position, by varying the length of the alkyl group, or by altering the degree of methylation of the amine. However, when the ethylamine side chain was cyclized to form 7 methoxytetrahydroisoquinoline, the copolymer prepared from this derivative (poly THIQ) was seven times more potent than compound 48/80. The hypotensive action of poly THIQ was found to result from the liberation of histamine, as with compound 48/80.
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β2-adrenoceptor agonists
Yi, Ce,Xing, Gang,Wang, Siqi,Li, Xiaoran,Liu, Yichuang,Li, Jinyan,Lin, Bin,Woo, Anthony Yiu-Ho,Zhang, Yuyang,Pan, Li,Cheng, Maosheng
, (2019/11/26)
A series of β2-adrenoceptor agonists with an 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one moiety is presented. The stimulatory effects of the compounds on human β2-adrenoceptor and β1-adrenoceptor were characterized by a cell-based assay. Their smooth muscle relaxant activities were tested on isolated guinea pig trachea. Most of the compounds were found to be potent and selective agonists of the β2-adrenoceptor. One of the compounds, (R)-18c, possessed a strong β2-adrenoceptor agonistic effect with an EC50 value of 24 pM. It produced a full and potent airway smooth muscle relaxant effect same as olodaterol. Its onset of action was 3.5 min and its duration of action was more than 12 h in an in vitro guinea pig trachea model of bronchodilation. These results suggest that (R)-18c is a potential candidate for long-acting β2-AR agonists.
Efficient conversion of primary and secondary alcohols to primary amines
Sun, Weilin,Pelletier, Jeffrey C.
, p. 7745 - 7746 (2008/02/12)
A convenient single-vessel conversion of primary and secondary alcohols to primary amines is reported. Use of this method results in substantially cleaner crude products than similar procedures reported in the literature. A simple work-up also makes this procedure ideal for parallel synthesis.
