13886-00-5Relevant academic research and scientific papers
Discovery of a potent non-oxime reactivator of nerve agent inhibited human acetylcholinesterase
de Koning, Martijn Constantijn,Horn, Gabriele,Worek, Franz,van Grol, Marco
, p. 151 - 160 (2018/08/10)
Organophosphorous (OP) compounds (such as nerve agents) inhibit the enzyme acetylcholinesterase (AChE) by covalent phosphylation of a key serine residue in the active site of the enzyme resulting in severe symptoms and ultimately death. OP intoxications are currently treated by administration of certain oxime compounds. The presently fielded oximes reactivate OP-inhibited AChE by liberating the phosphylated serine. Recent research towards new reactivators was predominantly devoted to design, synthesis and evaluation of new oxime-based compounds dedicated to overcoming some of the major limitations such as their intrinsic toxicity, their permanent charge which thwarts penetration of brain tissues and their inability to effectively reactivate all types of nerve agent inhibited AChEs. However, in over six decades of research only limited success has been achieved, indicating that there is a need for alternative classes of compounds that could reactivate OP-inhibited AChE. Recently, a number of non-oxime compounds was discovered in which the 4-amino-2-((diethylamino)methyl)phenol (ADOC) motif proved to be able to reactivate OP-inhibited AChE to some extent. In this paper several structural derivatives of ADOC were synthesized and screened for their ability to reactivate human AChE (hAChE) inhibited by the nerve agents VX, sarin, tabun, cyclosarin and paraoxon. We here disclose that one of those compounds showed a remarkable ability to reactivate OP-inhibited hAChE in vitro and that it is the most potent non-oxime reported to date.
Design, synthesis and antimalarial activity of some new 2-hydroxy-1,4-naphthoquinone-4-hydroxyaniline hybrid mannich bases
Sharma, Dipshikha,Chetia, Dipak,Rudrapal, Mithun
, p. 782 - 788 (2016/03/01)
In this study, some novel 2-hydroxy-1,4-naphthoquinone-4-hydroxyaniline hybrid Mannich bases were designed, synthesized and evaluated for in vitro antimalarial activity. The design strategy of novel hybrid molecules involves fusion between the pharmacopho
Synthesis and in vitro and in vivo antimalarial activity of novel 4-anilinoquinoline Mannich base derivatives
Singh, Bhupendra,Chetia, Dipak,Puri,Srivastava, Kumkum,Prakash, Anil
experimental part, p. 1523 - 1529 (2012/06/05)
Development of resistance has severely limited the choice of available antimalarial drugs, which clearly highlights the urgent need of novel chemotherapeutic agents for the treatment of malaria. The purpose of this study was to develop new potential antim
Microwave-induced Mannich reaction - Synthesis of some Mannich derivatives of p-aminophenol
Mahesh,Perumal, R. Venkatesha
, p. 1012 - 1014 (2007/10/03)
Mono and bis substituted dialkylamino alkyl-p-aminophenol 3 are prepared by treating paracetamol 1 with formaldehyde and appropriate secondary amines followed by deacetylation using 6 M HCI in unmodified domestic microwave oven in unsealed borosil vessels
Synthesis of new arylaminoquinoxalines and their antimalarial activity in mice
Rangisetty,Gupta,Prasad,Srinivas,Sridhar,Parimoo,Veeranjaneyulu
, p. 1409 - 1413 (2007/10/03)
2-Arylaminoquinoxalines were prepared by the condensation of 2-chloroquinoxaline with the appropriate Mannich bases in the presence of HCI. To synthesize the Mannich bases, 4-acetamidophenol was reacted with formaldehyde and dialkylamine to yield 3-[(dial
