50269-95-9Relevant articles and documents
Synthetic (±)-axinellamines deficient in halogen
Ding, Hui,Roberts, Andrew G.,Harran, Patrick G.
, p. 4340 - 4343 (2012)
Hiding in plain sight: Tailored synthetic dimers of the natural product dispacamide exist as a dynamic set of structural isomers. These materials isomerize readily to unveil a spirocyclic glycocyamidine from which ring systems common to complex pyrrole/imidazole alkaloids can be derived. Fully synthetic axinellamine congeners have been prepared in this way (see scheme), wherein a host of unusual and unanticipated reactions are employed. Copyright
Discovery, synthesis and in combo studies of Schiff’s bases as promising dipeptidyl peptidase-IV inhibitors
Abu Khalaf, Reema,Awad, Maha,Al-Essa, Luay,Mefleh, Sara,Sabbah, Dima,Al-Shalabi, Eveen,Shabeeb, Ihsan
, (2021/09/25)
Abstract: Diabetes mellitus is a main global health apprehension. Macrovascular illnesses, neuropathy, retinopathy, and nephropathy are considered some of its severe hitches. Gliptins are a group of hypoglycemic agents that inhibit dipeptidyl peptidase-IV (DPP-IV) enzyme and support blood glucose-lowering effect of incretins. In the current research, synthesis, characterization, docking, and biological evaluation of fourteen Schiff’s bases 5a–f and 9a–h were carried out. Compound 9f revealed the best in vitro anti-DPP-IV activity of 35.7% inhibition at a concentration of 100?μM. Compounds 9c and 9f with the highest in vitro DPP-IV inhibition were subjected to the in vivo glucose-lowering test using vildagliptin as a positive inhibitor. Vildagliptin, 9c, and 9f showed significant reduction in the blood glucose levels of the treated mice after 30?min of glucose administration. Moreover, induced fit docking showed that these derivatives accommodated the enzyme binding site with comparable docking scores. Schiff’s bases can serve as promising lead for the development of new DPP-IV inhibitors. Graphical Abstract: [Figure not available: see fulltext.].
From indole to pyrrole, furan, thiophene and pyridine: Search for novel small molecule inhibitors of bacterial transcription initiation complex formation
Thach, Oscar,Mielczarek, Marcin,Ma, Cong,Kutty, Samuel K.,Yang, Xiao,Black, David StC.,Griffith, Renate,Lewis, Peter J.,Kumar, Naresh
, p. 1171 - 1182 (2016/03/01)
The search for small molecules capable of inhibiting transcription initiation in bacteria has resulted in the synthesis of N,N′-disubstituted hydrazines and imine-carbohydrazides comprised of indole, pyridine, pyrrole, furan and thiophene using the respec
