33141-10-5Relevant academic research and scientific papers
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors
Feng, Song,Li, Chao,Chen, Dongdong,Zheng, Xiufang,Yun, Hongying,Gao, Lu,Shen, Hong C.
, p. 1147 - 1157 (2017/08/02)
Recently we described a novel class of imidazopyridine compounds that showed exceptional anti-RSV potency in cell culture. However, unfavorable pharmacokinetic (PK) properties and glutathione (GSH) adduct liabilities impeded their further development. In a bid to address the PK and early safety concerns, a small compound library consisting of dozens of scaffold-hopping analogues was designed and synthesized for RSV CPE assay screening, which led to the identification of a new chemical starting point: methylsulfonyl indole compound 8. In this paper, we report the discovery and optimization of a series of methylsulfonyl indazoles as potent RSV fusion inhibitors. In particular, compound 47 was orally efficacious in a RSV mouse model, with 1.6 log unit viral load reduction at 25 mg/kg BID upon oral dosing. The results may have broad implications for the design of new RSV fusion inhibitors, and demonstrate the potential for developing novel therapies for RSV infection.
HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
-
Page/Page column 97, (2010/08/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
The synthesis and some reactions OF 3-(2-aminophenyl)-2-iminothiazolidines. Ring closure of n-(2-thiocyanaoethyl,)-nphenylenediamines; thiazolidine vs. 3,1,6-benzothiadiazocine formation
Hornyak,Bertha,Zauer,Lempert,Feller,Pjeczka
, p. 2009 - 2030 (2007/10/02)
When treated with strong acids, the N-(2-thiocyanatoethyl)-n-phenylenediamines (1g-1y) are cyclized exclusively to 3-(2-aninophen- yl)-2-iminothiazolidines (6) while the related tertiary amines (1a-1f) gave, under the same conditions, benzothiadiazocines
