329222-94-8Relevant articles and documents
Preparation method and application of tetrahydrobenzothiophene compound and pharmaceutical composition
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Paragraph 0277; 0279; 0286-0288, (2021/10/16)
The invention belongs to the field of medicines, and particularly relates to a tetrahydrobenzothiophene compound as well as a pharmaceutical composition and a preparation method and application thereof. The tetrahydrobenzothiophene compound is a compound I as shown I. In-flight R1 And R2 The C1 -4 is a saturated/unsaturated hydrocarbon group. - OCH3 , OCH2 CH3 Phenyl, substituted phenyl, NO2 One - COR of - OH - F, Cl - Br. I - H R1 AND R2 Or different. R3 It is-F. - Cl, Br, I, OH, Amino, C1 -4 saturated/unsaturated hydrocarbon group, OCH3 , OCH2 CH3 , H, Wherein one of them is, n ≥ 5, n Being an integer. The compound effectively inhibits salmonella by inhibiting the synthesis of ATP-dependent transporter in the lipopolysaccharide synthesis pathway. Aeruginosa, escherichia coli and staphylococcus aureus.
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors
Pinkerton, Anthony B.,Lee, Tom T.,Hoffman, Timothy Z.,Wang, Yan,Kahraman, Mehmet,Cook, Travis G.,Severance, Daniel,Gahman, Timothy C.,Noble, Stewart A.,Shiau, Andrew K.,Davis, Robert L.
, p. 3562 - 3569 (2008/12/23)
We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for o