11 research outputs found
Affine surfaces with a huge group of automorphisms
We describe a family of rational affine surfaces S with huge groups of automorphisms in the following sense: the normal subgroup of Aut(S) generated by all its algebraic subgroups is not generated by any countable family of such subgroups, and the quotient of Aut(S) by this subgroup contains a free group over an uncountable set of generators
Novel Indole‑<i>N</i>‑glucoside, TA-1887 As a Sodium Glucose Cotransporter 2 Inhibitor for Treatment of Type 2 Diabetes
Inhibition
of the renal sodium glucose cotransporter (SGLT) increases urinary
glucose excretion (UGE) and thus reduces blood glucose levels during
hyperglycemia. To explore the potential of new antihyperglycemic agents,
we synthesized and determined the human SGLT2 (hSGLT2) inhibitory
potential of novel substituted 3-benzylindole-<i>N</i>-glucosides <b>6</b>. Optimization of <b>6</b> resulted in the discovery
of 3-(4-cyclopropylbenzyl)-4-fluoroindole-<i>N</i>-glucoside <b>6a-4</b> (TA-1887), a highly potent and selective hSGLT2 inhibitor,
with pronounced antihyperglycemic effects in high-fat diet-fed KK
(HF-KK) mice. Our results suggest the potential of indole-<i>N</i>-glucosides as novel antihyperglycemic agents through inhibition
of renal SGLT2