15592-29-7Relevant articles and documents
Novel partial agonists for the histamine H3 receptor with high in vitro and in vivo activity
Sasse, Astrid,Stark, Holger,Reidemeister, Sibylle,Hüls, Annette,Elz, Sigurd,Ligneau, Xavier,Ganellin, C. Robin,Schwartz, Jean-Charles,Schunack, Walter
, p. 4269 - 4274 (1999)
Novel branched N-alkylcarbamates and aliphatic ethers derived from 3- (1H-imidazol-4-yl)-propanol were prepared. The compounds were investigated on two functional histamine H3-receptor assays. Some compounds displayed partial agonist activity on synaptosomes of rat brain cortex but behaved as pure competitive antagonists on the guinea pig ileum. Under in vivo conditions after po application to mice, some of the compounds showed partial or full agonist activity. Highest in vivo potency was found for the 3,3- dimethylbutyl ether 10 (ED50 = 0.29 mg/kg, full intrinsic activity). These novel agonists are structurally diverse from classical aminergic histamine H3-receptor agonists (e.g., (R)-α-methylhistamine, imetit) as they lack a basic moiety in the side chain, which is supposed to be important for the activation of the receptor protein. The selectivity for the histamine H3 receptor was proven by determination of H1- and H2-receptor activity on functional assays of the guinea pig.
N-Substituted imido-dicarboxylic acid diaryl ester compounds and herbicide intermediates
-
, (2008/06/13)
Novel N-substituted imido-dicarboxylic acid diaryl ester compounds of the general formula STR1 in which R1 represents an optionally substituted aliphatic, cycloaliphatic, araliphatic, aromatic, heterocyclic radical and R2 and R3 can be identical or different and represent an optionally substituted aryl radical, and a process for their preparation characterized in that a carbamic acid aryl ester of the general formula in which R1 and R2 have the abovementioned meanings, is reacted with a carbonic acid aryl ester halide of the general formula in which R3 has the abovementioned meaning and X represents a halogen atom, optionally in the presence of a diluent, optionally at a temperature between 100° and 300° C. The new compounds (I) can be used as intermediate products for the preparation of known herbicidal active compounds from the 1,3,5-triazine,2,4-(1H,3H)-dione series.