39575-05-8Relevant academic research and scientific papers
2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L
Garg, Shweta,Raghav, Neera
, p. 64 - 74 (2016/07/06)
High levels of cathepsins indicated in various pathological conditions like arthritis, cancer progressions, and atherosclerosis explains the need to explore potential inhibitors of these proteases which can be of great therapeutic significance. We, in the present work, report the synthesis of some 2,5-diaryloxadiazoles from N-subsitutedbenzylidenebenzohydrazides. The synthesized compounds were screened for their inhibitory potential on cathepsins B, H and L. Structure Activity Relationship studies show that 2,5-diaryloxadiazoles were less inhibitory than their precursors. 1i and 2k have been found to be most inhibitory to cathepsins B and L. Their Ki values have been calculated as 11.38 × 10-8 M and 66.4 × 10-8 M for cathepsin B and 4.2 × 10-9 M and 47.31 × 10-9 M for cathepsin L, respectively. However, cathepsin H activity was maximally inhibited by compounds, 1e and 2c with Ki values of 4.4 × 10-7 M and 5.6 × 10-7 M, respectively. Enzyme kinetic studies suggest that these compounds are competitive inhibitors to the enzymes. The results have been compared with docking results obtained using iGemDock.
Tin Powder-Promoted One-Pot Construction of α-Methylene-γ-lactams and Spirolactams from Aldehydes or Ketones, Acylhydrazines, and 2-(Bromomethyl)acrylate
Xu, Yanli,Huang, Danfeng,Wang, Ke-Hu,Ma, Junyan,Su, Yingpeng,Fu, Ying,Hu, Yulai
, p. 12224 - 12233 (2016/01/09)
A concise and efficient method for the synthesis of α-methylene-γ-lactams is developed from multicomponent one-pot reactions of aldehydes or ketones, hydrazides, and ethyl 2-(bromomethyl)acrylate promoted by tin powder. The reaction proceeds smoothly under mild reaction conditions without using any catalyst to give the corresponding products in high yields. α-Methylene-γ-spirolactams can also be prepared from cyclic ketones.
Nicotinic acid hydrazones: A novel anticonvulsant pharmacophore
Sinha, Reema,Sara, U. V. Singh,Khosa,Stables, James,Jain, Jainendra
experimental part, p. 1499 - 1504 (2012/06/15)
A series of aryl acid hydrazones of substituted aromatic acid hydrazides (D1 to D20) were synthesised and evaluated for anticonvulsant activity. Aryl acid hydrazones of Nicotinic acid hydrazide (D8, D9, and Dsu
Indium-mediated catalytic enantioselective allylation of N -benzoylhydrazones using a protonated chiral amine
Kim, Sung Jun,Jang, Doo Ok
supporting information; experimental part, p. 12168 - 12169 (2010/10/03)
A catalytic enantioselective indium-mediated allylation of N-benzoylhydrazones in conjunction with a protonated chiral amine affording enantioenriched homoallylic amines with an extremely high level of enantioselectivity and chemical yield was developed.
