- Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis
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Herein, we report the synthesis and anti-tubercular studies of novel molecules based on thiophene scaffold. We identified two novel small molecules 4a and 4b, which demonstrated 2-fold higher in vitro activity (MIC99: 0.195 μM) compared to firs
- Asthana, Shailendra,Kumar, Arun,Kumar, Varun,Mahajan, Dinesh,Meena, Chhuttan L.,Shaliwal, Ravi P.,Singh, Padam,Singh, Ramandeep,Tiwari, Anoop Kumar
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- 1,4-Thienodiazepine-2,5-diones via MCR (I): Synthesis, Virtual Space and p53-Mdm2 Activity
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1,4-Thienodiazepine-2,5-diones have been synthesized via the Ugi-Deprotection-Cyclization (UDC) approach starting from Gewald 2-aminothiophenes in a convergent and versatile manner. The resulting scaffold is unprecedented, cyclic, and peptidomimetic with four points of diversity introduced from readily available starting materials. In addition to eighteen synthesized and characterized compounds, a virtual compound library was generated and evaluated for chemical space distribution and drug-like properties. A small focused compound library of 1,4-thienodiazepine-2,5-diones has been screened for the activity against p53-Mdm2 interaction. Biological evaluations demonstrated that some compounds exhibited promising antagonistic activity.
- Huang, Yijun,Wolf, Siglinde,Bista, Michal,Meireles, Lidio,Camacho, Carlos,Holak, Tad A.,Doemling, Alexander
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p. 116 - 129
(2011/03/20)
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- 1,4-Thienodiazepine-2,5-diones via MCR (II): Scaffold Hopping by Gewald and Ugi-Deprotection-Cyclization Strategy
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A second scaffold of 1,4-thienodiazepine-2,5-diones was discovered and is synthetically accessible from Gewald 2-aminothiophenes via Ugi-Deprotection- Cyclization (UDC) strategy. This approach yielded hybrid peptidomimetic diazepine structures with six po
- Huang, Yijun,Doemling, Alexander
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scheme or table
p. 130 - 141
(2011/03/20)
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- NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome,
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Page/Page column 28
(2009/01/24)
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