| Literature DB >> 18835161 |
Manisha Moorjani1, Zhiyong Luo, Emily Lin, Binh G Vong, Yongsheng Chen, Xiaohu Zhang, Jaimie K Rueter, Raymond S Gross, Marion C Lanier, John E Tellew, John P Williams, Sandra M Lechner, Siobhan Malany, Mark Santos, María I Crespo, José-Luis Díaz, John Saunders, Deborah H Slee.
Abstract
In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In addition, compound 35 had good metabolic stability with a scaled intrinsic clearance of 3 mL/min/kg (HLM) and demonstrated efficacy in the haloperidol induced catalepsy model.Entities:
Mesh：
Substances：
Year: 2008 PMID： 18835161 DOI： 10.1016/j.bmcl.2008.09.048
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823