1.
Bioorg Med Chem Lett
; 28(11): 2000-2002, 2018 06 15.
Article
in English
| MEDLINE
| ID: mdl-29752183
ABSTRACT
We identified novel (3R, 5S)-3-aminomethyl-5-methanesulfanyl hexanoic acid (5a: DS75091588) and (3R, 5S)-3-aminomethyl-5-ethanesulfanyl hexanoic acid (6a: DS18430756) as sulfur-containing γ-amino acid derivatives that were useful for the treatment of neuropathic pain. These two compounds exhibited a potent analgesic effect in animal models of both type I diabetes and type II diabetes, and good pharmacokinetics.
Subject(s)
Calcium Channels/metabolism , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Type 1/drug therapy , Diabetes Mellitus, Type 2/drug therapy , Neuralgia/drug therapy , Sulfhydryl Compounds/pharmacology , Animals , Caproates/chemistry , Caproates/pharmacology , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Type 1/metabolism , Diabetes Mellitus, Type 2/metabolism , Disease Models, Animal , Ligands , Mice , Molecular Structure , Neuralgia/metabolism , Sulfhydryl Compounds/chemistry
2.
Angew Chem Int Ed Engl
; 52(44): 11607-11, 2013 Oct 25.
Article
in English
| MEDLINE
| ID: mdl-24014169
ABSTRACT
Rise and shine: Using a gene-targeting approach aimed at identifying potential L-threonine:uridine-5'-transaldolases that catalyze the formation of (5'S,6'S)-C-glycyluridine, a new bacterial translocaseâ I inhibitor was discovered from an actinomycete following fermentation optimization.