65840-58-6Relevant academic research and scientific papers
Peroxides as "switches" of dialkyl H-phosphonate: Two mild and metal-free methods for preparation of 2-acylbenzothiazoles and dialkyl benzothiazol-2-ylphosphonates
Chen, Xiao-Lan,Li, Xu,Qu, Ling-Bo,Tang, Yu-Chun,Mai, Wen-Peng,Wei, Dong-Hui,Bi, Wen-Zhu,Duan, Li-Kun,Sun, Kai,Chen, Jian-Yu,Ke, Dian-Dian,Zhao, Yu-Fen
, p. 8407 - 8416 (2015/03/18)
Two mild and metal-free methods for the preparation of two kinds of important benzothiazole derivatives, 2-acylbenzothiazoles and dialkyl benzothiazol-2-ylphosphonates, respectively, were developed. The dialkyl H-phosphonate (RO)2P(O)H exists i
Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors
Banerjee, Abhisek,Narayana, Lakshminarayana,Raje, Firoj A.,Pisal, Dnyandeo V.,Kadam, Pradip A.,Gullapalli, Srinivas,Kumar, Hemant,More, Sandeep V.,Bajpai, Malini,Sangana, Ramachandra Rao,Jadhav, Satyawan,Gudi, Girish S.,Khairatkar-Joshi, Neelima,Merugu, Ravi R.T.,Voleti, Sreedhara R.,Gharat, Laxmikant A.
supporting information, p. 6747 - 6754 (2014/01/06)
The design, synthesis and structure activity relationship studies of a series of compounds from benzo[d]imidazo[5,1-b]thiazole scaffold as phosphodiesterase 10A (PDE10A) inhibitors are discussed. Several potent analogs with heteroaromatic substitutions (9a-d) were identified. The anticipated binding mode of these analogs was confirmed by performing the in silico docking experiments. Later, the heteroaromatics were substituted with saturated heteroalkyl groups which provided a tool compound 9e with excellent PDE10A activity, PDE selectivity, CNS penetrability and with favorable pharmacokinetic profile in rats. Furthermore, the compound 9e was shown to be efficacious in the MK-801 induced psychosis model and in the CAR model of psychosis.
