20610-20-2Relevant academic research and scientific papers
INSULIN ANALOGUES WITH GLUCOSE REGULATED CONFORMATIONAL SWITCH
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Page/Page column 24, (2021/02/05)
The present invention relates to glucose-responsive insulin analogues, compositions including the glucose-responsive insulin analogues, and methods of lowering blood sugar of a patient using the insulin analogue or compositions thereof.
Lipodiscamides A-C, new cytotoxic lipopeptides from discodermia kiiensis
Tan, Karen Co,Wakimoto, Toshiyuki,Abe, Ikuro
supporting information, p. 3256 - 3259 (2014/07/08)
Lipodiscamides A-C, three new lipodepsipeptides, were characterized from the marine sponge Discodermia kiiensis. These structurally rare cyclic lipodepsipeptides were found to possess an unprecedented dilactone macrocycle and, thus, represent a new family of lipopeptides. They are the only lipopeptides bearing 4S-hydroxy-trans-2-enoate, and noncanonical amino acids, l-3-ureidoalanine (Uda), E-dehydronorvaline (Denor), and d-citrulline (Cit). MTT assays against P388 and HeLa cells revealed the moderate cytotoxicity of all three compounds.
Calyxamides A and B, cytotoxic cyclic peptides from the marine sponge Discodermia calyx
Kimura, Miki,Wakimoto, Toshiyuki,Egami, Yoko,Tan, Karen Co,Ise, Yuji,Abe, Ikuro
experimental part, p. 290 - 294 (2012/05/05)
Cyclic peptides containing 5-hydroxytryptophan and thiazole moieties were isolated from the marine sponge Discodermia calyx collected near Shikine-jima Island, Japan. The structures of calyxamides A (1) and B (2), including the absolute configurations of all amino acids, were elucidated by spectroscopic analyses and degradation experiments. The structures are similar to keramamides F and G, previously isolated from Theonella sp. The analysis of the 16S rDNA sequences obtained from the metagenomic DNA of D. calyx revealed the presence of Candidatus Entotheonella sp., an unculturable δ-proteobacterium inhabiting the Theonella genus and implicated in the biosynthesis of bioactive peptides.
Discovery of pyrazine carboxamide CB1 antagonists: The introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series
Ellsworth, Bruce A.,Wang, Ying,Zhu, Yeheng,Pendri, Annapurna,Gerritz, Samuel W.,Sun, Chongqing,Carlson, Kenneth E.,Kang, Liya,Baska, Rose A.,Yang, Yifan,Huang, Qi,Burford, Neil T.,Cullen, Mary Jane,Johnghar, Susan,Behnia, Kamelia,Pelleymounter, Mary Ann,Washburn, William N.,Ewing, William R.
, p. 3978 - 3982 (2008/02/07)
Structure-activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose.
Fibrinogen receptor antagonists
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, (2008/06/13)
Fibrinogen receptor antagonists of the formula: STR1 are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
