101961-58-4Relevant articles and documents
New sulphonamide pyrolidine carboxamide derivatives: Synthesis, molecular docking, antiplasmodial and antioxidant activities
Onoabedje, Efeturi A.,Ibezim, Akachukwu,Okoro, Uchechukwu C.,Batra, Sanjay
, (2021/03/16)
Carboxamides bearing sulphonamide functionality have been shown to exhibit significant lethal effect on Plasmodium falciparum, the causative agent of human malaria. Here we report the synthesis of thirty-two new drug-like sulphonamide pyrolidine carboxami
Synthetic process of chiral N-aromatic amino acid amide
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Paragraph 0010; 0014, (2016/10/17)
Chiral N-aromatic amino acid amide is a core structure fragment of drugs and an intermediate of the drugs. Only if the chiral structure of the product is not required by special raw materials such aryl halide activated by functional groups of nitryl and t
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design
Meng, Fei,Huang, Manna,Zhu, Xinhai,Wan, Yiqian,Hou, Jing,Shao, Yong-Xian,Cai, Yonghong,Li, Zhe,Xu, Jie,Liu, Peiqing,Luo, Hai-Bin,Ke, Hengming,Wu, Pei-Ying
, p. 8549 - 8558,10 (2020/09/15)
A new series of phosphodiesterase-9 (PDE9) inhibitors that contain a scaffold of 6-amino-pyrazolopyrimidinone have been discovered by a combination of structure-based design and computational docking. This procedure significantly saved the load of chemical synthesis and is an effective method for the discovery of inhibitors. The best compound 28 has an IC50 of 21 nM and 3.3 μM, respectively, for PDE9 and PDE5 and about 3 orders of magnitude of selectivity against other PDE families. The crystal structure of the PDE9 catalytic domain in complex with 28 has been determined and shows a hydrogen bond between 28 and Tyr424. This hydrogen bond may account for the 860-fold selectivity of 28 against PDE1B, in comparison with about 30-fold selectivity of BAY73-6691. Thus, our studies suggest that Tyr424, a unique residue of PDE8 and PDE9, is a potential target for improvement of selectivity of PDE9 inhibitors.
Synthesis of α-amino acid amides: Ruthenium-catalyzed amination of α-hydroxy amides
Zhang, Min,Imm, Sebastian,Baehn, Sebastian,Neumann, Helfried,Beller, Matthias
supporting information; experimental part, p. 11197 - 11201 (2012/02/03)
Give me an N: The catalytic amination of α-hydroxy amides with a variety of amines, including anilines, primary and secondary aliphatic amines, and ammonia, yields a wide range of α-amino amides (see scheme). This atom-efficient amination protocol proceeds efficiently in the presence of a commercially available [Ru3(CO)12]/DCPE catalyst system. Copyright
Nitrosation of α,β-Unsaturated Carboxamide with Nitric Oxide and Triethylsilane Catalyzed by Cobalt(II) Complex
Kato, Koji,Mukaiyama, Teruaki
, p. 1395 - 1398 (2007/10/02)
In the presence of a catalytic amount of N,N'-bis(2-ethoxycarbonyl-3-oxobutylidene)ethylenediaminatocobalt(II), various α,β-unsaturated carboxamides are converted to the corresponding 2-nitrosocarboxamides regioselectively in good yields on treatment with
