51034-34-5Relevant articles and documents
Enantioselective synthesis of 3,5-disubstituted thiohydantoins and hydantoins
Chen, Yu,Su, Li,Yang, Xinying,Pan, Wenyan,Fang, Hao
, p. 9234 - 9239 (2015)
A mild method to convert optically pure amino acid thiourea and urea derivatives to thiohydantoins and hydantoins, respectively, is described. It provides an efficient way to realize enantioselective synthesis of thiohydantoins and hydantoins with good to high isolated yields and enantiomeric purities. We found that the enantiomeric purities were highly dependent on the reaction conditions including bases, solvents, and temperature.
An efficient one-pot strategy for the synthesis of 4- methylene-2-thiazolidinethiones in water
Hou, Chang-Long,Wei, Mei-Hong,Chen, Li-Li,Liu, Xiao-Ling,Sheng, Shou-Ri
, p. 1561 - 1566 (2020/04/09)
A simple and efficient, one-pot strategy for the preparation of 4-methylene-2-thiazolidinethiones has been developed. This protocol involved condensation of primary amines with carbon disulfide in water to generate the dithiocarbamate salts in situ, which coupled with 2,3-dibromopropene, followed by intramolecular cyclization to the corresponding heterocycles in moderate to good yields.
Synthesis, in vitro urease inhibitory activity and molecular docking of 3,5-disubstituted thiadiazine-2-thiones
Shah, Muhammad Ishaq Ali,Khan, Rasool,Arfan, Mohammad,Wadood, Abdul,Ghufran, Mehreen
, p. 3073 - 3080 (2019/09/16)
A series of 3,5-disubstituted-tetrahydro-thiadiazine-2-thione (1-16) have been synthesized, characterized by elemental analysis, infrared (IR), UV-visible, 1H NMR, 13C NMR, and MS spectroscopic techniques, and screened against jack bean urease. Among 16 compounds, compounds (1), (2), (3), (4), (6), (7), and (9) demonstrated excellent urease inhibitory activity with IC50 values (9.8?±?0.5, 11.0?±?0.6, 16.0?±?1.5, 17.2?±?0.5, 15.4?±?0.5, 19.7?±?0.4, and 15.8?±?0.2μM), respectively, even better than the standard thiourea (IC50?=?21?±?0.01μM). However, compound (8) shows an almost same level of inhibition (IC50?=?22.9?±?0.3μM), as like standard. In this work, we reported for the first time urease inhibitory activity of thiadiazine thiones and its molecular docking studies.