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A series of analogs of the non-peptidic benzolactam growth hormone secretagogue L-692,429 was prepared with heteroatom substitutions at the 5-position of the benzolactam ring. Replacement of the 5-position with sulfur or oxygen resulted in secretagogues of approximate equal potency to L-692,429...
The synthesis and the preliminary microbiological activity of some tryciclic β-lactam derivatives designed combining the structural features of the natural carbapenems and the synthetic “ tribactams ” are described.
A range of novel benzimidazole derivatives, some bearing analogy to TIBO, have been synthesized, and evaluated for inhibition of HIV-1 infectivity. The most active and selective compounds are a series of N-alkoxy-2-alkyl-benzimidazoles, several having EC 50 < 10μM (one sub-micromolar at 600nM),...
The chemistry and in vitro pharmacology of novel prostanoid TXA 2 (TP)-receptor antagonists is described. (5Z)-(9R)-12-(4-Chlorobenzenesulfonamido)-9-fluoro-13,14,15,16,17,18,19,20-octanor-5-prostenoic acid was identified as a potent TP-receptor antagonist.
Isolation and sequence determination of a protein exhibiting α-ketoisocaproate dioxygenase activity from rat liver revealed that the protein was identical to the liver-specific rat F antigen which is believed to be a species variant of 4-hydroxyphenylpyruvate dioxygenase. Isolation and sequence...
Diastereoselectively labeled (3S)-(4- 13 C)- l -valine and regioselectively labeled (3- 13 CH 3 )- l -isoleucine hydrochlorides were synthesized in 54% and 62% respective overall yields from l -aspartic acid.
Initial work on a series of quinuclidine based antagonists suggested that only one of the rigns of the benzhydryl was involved in receptor binding. This communication endeavors to test this hypothesis and to identify which of the phenyl rings interacts with Histidine 197.
A diastereoselective version of Katritzky's method for tertiary amine formation provides an efficient route to the highly selective, non-peptidal, delta opioid agonist (+)-4-((αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethylbenzamide ((+)-BW373U86), 1 .
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