112091-24-4Relevant academic research and scientific papers
Efficient synthesis of new (R)-2-amino-1-butanol derived ureas, thioureas and acylthioureas and in vitro evaluation of their antimycobacterial activity
Dobrikov, Georgi M.,Valcheva, Violeta,Nikolova, Yana,Ugrinova, Iva,Pasheva, Evdokia,Dimitrov, Vladimir
supporting information, p. 468 - 473 (2013/07/25)
The synthesis of 22 structurally diverse urea, thiourea and acylthiourea derivatives containing the (R)-2-amino-1-butanol motif has been performed. The evaluation of their in vitro activity against Mycobacterium tuberculosis (H 37Rv and strain
Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors
Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Sheng-Ju,Lee, Chung-Chi,Lee, Yen-Chun,Wu, Yen-Shian,Hsu, Tsu-An,Yueh, Andrew,Chao, Yu-Sheng,Chern, Jyh-Haur
scheme or table, p. 4134 - 4138 (2010/04/26)
An efficient synthetic methodology to provide indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives is described. These conformationally restricted heterobicyclic scaffolds were evaluated as a novel class of HCV inhibitors. Introduction of an acyl group at the NH2 of the thiourea moiety has been found to enhance inhibitory activity. The chain length and the position of the alkyl group on the indoline aromatic ring markedly influenced anti-HCV activity. The indoline scaffold was more potent than the corresponding indole and tetrahydroquinoline scaffolds and analogue 31 displayed excellent activity (EC50 = 510 nM) against HCV without significant cytotoxicity (CC50 >50 μM).
Efficient approaches to S-alkyl-N-alkylisothioureas: Syntheses of histamine H3 antagonist clobenpropit and its analogues
Yoneyama, Hiroki,Shimoda, Ayako,Araki, Lisa,Hatano, Kouta,Sakamoto, Yasuhiko,Kurihara, Takushi,Yamatodani, Atsushi,Harusawa, Shinya
, p. 2096 - 2104 (2008/09/19)
(Chemical Equation Presented) S-Alkyl-N-alkylisothioureas were efficiently synthesized via synthetic approach (A) using 3-phenylpro-pionyl isothiocyanate (PPI). The utility of the approach was proved by the syntheses of clobenpropit, a potent histamine H3 antagonist, and its analogues. Alternatively, clobenpropit could be prepared via intramolecular amide cleavage (B) with use of 2-nitrophenylacetyl isothiocyanate (NPAI).
