59514-89-5Relevant academic research and scientific papers
INHIBITORS OF LOW MOLECULAR WEIGHT PROTEIN TYROSINE PHOSPHATASE (LMPTP) AND USES THEREOF
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, (2018/11/26)
Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.
4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity
Naik, Maruti,Humnabadkar, Vaishali,Tantry, Subramanyam J.,Panda, Manoranjan,Narayan, Ashwini,Guptha, Supreeth,Panduga, Vijender,Manjrekar, Praveena,Jena, Lalit Kumar,Koushik, Krishna,Shanbhag, Gajanan,Jatheendranath, Sandesh,Manjunatha,Gorai, Gopinath,Bathula, Chandramohan,Rudrapatna, Suresh,Achar, Vijayashree,Sharma, Sreevalli,Ambady, Anisha,Hegde, Naina,Mahadevaswamy, Jyothi,Kaur, Parvinder,Sambandamurthy, Vasan K.,Awasthy, Disha,Narayan, Chandan,Ravishankar, Sudha,Madhavapeddi, Prashanti,Reddy, Jitendar,Prabhakar,Saralaya, Ramanatha,Chatterji, Monalisa,Whiteaker, James,McLaughlin, Bob,Chiarelli, Laurent R.,Riccardi, Giovanna,Pasca, Maria Rosalia,Binda, Claudia,Neres, Jo?o,Dhar, Neeraj,Signorino-Gelo, Fran?ois,McKinney, John D.,Ramachandran, Vasanthi,Shandil, Radha,Tommasi, Ruben,Iyer, Pravin S.,Narayanan, Shridhar,Hosagrahara, Vinayak,Kavanagh, Stefan,Dinesh, Neela,Ghorpade, Sandeep R.
supporting information, p. 5419 - 5434 (2014/07/08)
4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ~100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb.
2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
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, (2013/05/08)
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particu
2,4- DIARYL-SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
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, (2012/01/14)
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases playsa role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors
4-thio substituted quinoline and naphthyridine compounds
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Page/Page column 18, (2009/04/24)
The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative.
4-THIO SUBSTITUTED QUINOLINE AND NAPHTHYRIDINE COMPOUNDS
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Page/Page column 43, (2008/06/13)
The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative.
