1.
Bioorg Med Chem Lett
; 22(24): 7672-6, 2012 Dec 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23141913
RESUMO
Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural-activity relationships were developed to yield compounds with good selectivity and excellent in vivo efficacy in rat models.
Assuntos
Descoberta de Drogas , Receptores de Lisoesfingolipídeo/agonistas , Tiadiazóis/farmacologia , Administração Oral , Animais , Cristalografia por Raios X , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Encefalomielite Autoimune Experimental/tratamento farmacológico , Linfopenia/sangue , Modelos Moleculares , Estrutura Molecular , Ratos , Receptores de Esfingosina-1-Fosfato , Relação Estrutura-Atividade , Tiadiazóis/administração & dosagem , Tiadiazóis/síntese química
2.
Org Lett
; 7(19): 4083-6, 2005 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16146357
RESUMO
[reaction: see text] The key fragment (2a or 2b) in a total synthesis of the cytotoxic macrolide (-)-amphidinolide K (1) has been achieved from synthons C9-C14 (3) and C15-C22 (4), which have both been prepared from glutamic acid in good overall yields.