192524-14-4Relevant academic research and scientific papers
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring
Guo, Xing-Zhou,Shi, Lin,Wang, Rui,Liu, Xiao-Xiao,Li, Bo-Gang,Lu, Xiao-Xia
experimental part, p. 10301 - 10310 (2009/04/07)
A series of benzimidazole derivatives bearing a heterocyclic ring imidazole (1), 5-chloroimidazole (2), 1,2,4-triazol (3), and imidazoline (4) were synthesized and evaluated for angiotensin II antagonistic activities. The synthetic compounds 1-4 were biologically evaluated in vitro using an AT1 receptor binding assay, where compounds 1 and 3 provided weak binding affinity, compound 2 showed moderate binding affinity, and compound 4 showed good binding affinity. Moreover, compound 4 was found to be almost equipotent with telmisartan in vivo biological evaluation study.
Investigation of bioisosters of the growth hormone secretagogue L-692,429
Ankersen, Michael,Peschke, Bernd,Hansen, Birgit Sehested,Hansen, Thomas Kruse
, p. 1293 - 1298 (2007/10/03)
The synthesis and structure-activity relationships of several analogs of L-692,429 with modifications in the biaryl and tetrazole moieties are described and several derivatives were found to be equipotent or slightly more potent than L-692,429.
Benzo-fused lactams promote release of growth hormone
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, (2008/06/13)
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed. STR1 where L is STR2
Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl group, and the pharmaceutical compositions in which they are present
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, (2008/06/13)
This invention relates to compounds of formula STR1 in which: R1 and R2 are similar or different and are each independently hydrogen or a group selected from CO2 N=C(NH2)2, CONHNHCONH2, CONHNHCSNH2, C(OC2 H5)=NCO2 CH3, COCH2 CO2 H5, N(OH)-CONHCOOC2 NCO2 CH3, COCH2 CO2 H5, N(OH)-CONHCOOC2 H5, C(OC2 H5)=NH or a nitrogen heterocycle; with the proviso that at least one of the substituents R1 or R2 is other than hydrogen; R3 is a hydrogen, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C3 -C7 cycloalkyl, a phenyl, a phenylalkyl, or a phenylalkenyl; R4 and R5 are each independently a C1 -C6 alkyl, a C3 -C7 cycloalkyl, a phenyl or a phenylalkyl; or R4 and R5, bonded together, are either a group of the formula (CH2)n or a group of the formula (CH2)p Y (CH2)q, in which Y is either an oxygen atom, or a sulfur atom, or a substituted carbon atom, or a group N-R6, in which R6 is a hydrogen, a C1 -C4 alkyl, a phenylalkyl, a C1 -C4 alkylcarbonyl, a C1 -C4 halogenoalkylcarbonyl, a C1 -C4 polyhalogenoalkylcarbonyl, a benzolyl, an α-aminoacyl or a N-protecting group, or R4 and R5, together with the carbon atom to which they are bonded, form an indane or an adamantine; p+q=m; n is an integer between 2 and 11; m is an integer between 2 and 5; X is an oxygen or a sulfur atom; and z and t are zero or z+t=1; and its salts.
