123193-99-7Relevant articles and documents
Studies on phosphoroheterocycle chemistry II: A simple and new route to 1,3,2-diazaphospholidine-4-thione 2-sulfide derivatives
Deng,Liu
, p. 2445 - 2449 (2001)
A simple and new method for the synthesis of phosphoroheterocycles 1,3,2-diazaphospholidine-4-thione 2-sulfide derivatives by treatment of Lawesson's reagent (LR) with a variety of α-aminonitriles has been developed. The same methodology was also used in the preparation of fused phosphoroheterocycle 6 from 5-amino-4-cyano-3-methylthia-l-phenylpyrazole. The possible mechanism of the reaction involving addition of P-SH to the nitrile and subsequent rearrangement is proposed.
Photoreactive fused aziridinylpiperazines on the background of 4-substituted chalcones and their benzimidazolic analogs
Kotlyar, Volodymyr M.,Kolomoitsev, Oleksii O.,Nikolaievskyi, Dmytro V.,Pedan, Polina I.,Chumak, Andrii Yu,Orlov, Valery D.,Shishkina, Svitlana V.,Doroshenko, Andrey O.
, p. 741 - 746 (2019/01/10)
The reaction of bromo-substituted chalcones with various diamino-compounds leads to the fused heterocyclic products, aziridinylpiperazines, exhibiting photoreactivity in the crystalline state. Crystals of 4-nitrosubstituted compounds of this family change their color from yellowish to deep violet-blue, 4-cyanosubstituted ones – from yellowish to pink at UV irradiation. Discussion on the mechanism of this phototransformation is still in progress, however, several facts points to the free radial nature of the photogenerated colored semi-products stabilized only by crystalline state of the irradiated samples. Formation of a mixture of positional isomers at interaction of bromo-chalcones with asymmetric diamines of aliphatic/alicyclic or aromatic series at synthesis of the title compounds is of significant interest as well.
Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to safinamide with anticonvulsant potential
Aboul-Enein, Mohamed N.,El-Azzouny, Aida A.,Maklad, Yousreya A.,Ismail, Mohamed A.,Ismail, Nasser S. M.,Hassan, Rasha M.
, p. 3767 - 3791 (2015/06/08)
A series of novel safinamide derivatives were synthesized and biologically evaluated for their anticonvulsant activity against maximal electroshock seizure assay and subcutaneous pentylenetetrazole (s.c. PTZ) screening test. Compound 13b is the most active derivative in s.c. PTZ screening test with an ED50 value lower than that of safinamide by about tenfold. A molecular modeling study, including fitting to sodium channel blockers 3D-pharmacophore model and docking into a branched-chain aminotransferase enzyme active site were consistent with the in vivo results.