193955-35-0Relevant academic research and scientific papers
Synthesis, biological evaluation, and qpld studies of piperazine derivatives as potential dpp-iv inhibitors
Al-Qirim, Tariq,Jarad, Haya Abu,Khalaf, Reema Abu,Sabbah, Dima
, p. 937 - 944 (2021/11/30)
Background: Diabetes mellitus is a serious global health issue, currently affecting 425 million people and is set to affect over 690 million people by 2045. It is a chronic disease characterized by hyperglycemia due to relative or absolute insulin hormone deficiency. Dipeptidyl peptidaseIV (DPP-IV) inhibitors are hypoglycemic agents augmenting the action of the incretin hormones that stimulate insulin secretion from the pancreatic beta cells. Objective: In this study, synthesis and biological evaluation of seven piperazine derivatives 3a-g was carried out. Methods: The synthesized molecules were characterized using proton-nuclear magnetic resonance, carbon-nuclear magnetic resonance, infrared spectroscopy and mass spectrometry. Results: In vitro biological evaluation study showed comparable DPP-IV inhibitory activity for the targeted compounds ranging from 19%-30% at 100 μM concentration. Furthermore, the in vivo hypoglycemic activity of 3d was evaluated using streptozotocin-induced diabetic mice. It was found that compound 3d significantly decreased the blood glucose level when the diabetic group treated with 3d was compared to the control diabetic group. Quantum–Polarized Ligand Docking (QPLD) studies demonstrate that 3a-g fit the binding site of DPP-IV enzyme and form H-bonding with the backbones of R125, E205, E206, K554, W629, Y631, Y662, R669, and Y752. Conclusion: Piperazine derivatives were successfully found to be new scaffolds as potential DPP-IV inhibitors.
SUBSTITUTED PIPERIDINYL-PYRIDAZINYL DERIVATIVES USEFUL AS SCD 1 INHIBITORS
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Page/Page column 75, (2013/06/27)
The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
Synthesis and anti-angiogenic activity of 6-(1,2,4-thiadiazol-5-yl)-3-amino pyridazine derivatives
Bongartz, Jean-Pierre,Stokbroekx, Raymond,Van der Aa, Marcel,Luyckx, Marcel,Willems, Marc,Ceusters, Marc,Meerpoel, Lieven,Smets, Gerda,Jansen, Tine,Wouters, Walter,Bowden, Charlie,Valletta, Lisa,Herb, Mark,Tominovich, Rose,Tuman, Robert
, p. 589 - 591 (2007/10/03)
General screening for inhibitors of microvessel growth in vitro in the rat aortic ring assay led to the discovery of a novel series of thiadiazole pyridazine compounds with potential anti-angiogenic activity. Chemical optimization produced orally active compounds with potent in vitro and in vivo anti-angiogenesis and anti-tumor activities.
Angiogenesis inhibiting pyridazinamines
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, (2008/06/13)
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH2 groups of the STR1 moiety which may also contain one double bond, may be substituted with C1-6 alkyl, amino, aminocarbonyl, mono- or di(C1-6 alkyl)amino, C1-6 alkyloxycarbony, C1-6 alkylcarbonylamino, hydroxy or C1-6 alkyloxy; and/or 2 C-atoms of said CH2 groups may be bridged with C2-4 alkanediyl; R1 is hydrogen, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylthio, amino, mono- or di(C1-6 alkyl)amino, Ar, ArNH--, C3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula --CH=CH--CH=CH--; in case X represents CH then L is a radical L1, L2 or L3 ; or in case X represents N then L is a radical L2 or L3 ; L1 is Ar-C1-6 alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar--NR4 --, Ar-Alk-NR4 --, Ar--NR4 -Alk-NR5 -- or Het-NR4 --; L2 is Ar, Ar-carbonyl, Ar--CH=CH--CH2 --, naphtalenyl or Het; L3 is C1-6 alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl;Ar-piperidinyl or Ar--NR4 -Alk-; R4 and R5 are each independently selected from hydrogen or C1-6 alkyl; Alk is C1-6 alkanediyl; their preparation, compositions containing them and their use as a medicine.
Organic Synthesis Using PTC: Part 8 - Synthesis of Macrocylic Systems Containing Nitrogen and/or Oxygen as Heteroatom(s)
Singh, Paramjit,Jain, Anupa
, p. 790 - 792 (2007/10/02)
Reactions of p-toluene/benzenesulphonamides with p-toluenesulphonate ester of diols under liquid-liquid and solid-liquid phase transfer (PT) conditions give cyclic N-p-toluenesulphonyl or N-benzenesulphonyl derivatives with 1:1 and/or 2:2 stoichiometries.Thus, the cyclic system containing N and/or O as heteroatom(s) have been procured usimg this procedure.
