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参考文献:2-Aryl Benzazole Derived New Class Of Anti-Tubercular Compounds: Endowed To Eradicate Mycobacterium Tuberculosis In Replicating And Non-Replicating Forms
标题:2-Aryl Benzazole Derived New Class Of Anti-Tubercular Compounds: Endowed To Eradicate Mycobacterium Tuberculosis In Replicating And Non-Replicating Forms
摘要:The High Mortality Rate And The Increasing Prevalence Of Mtb Resistance Are The Major Concerns For The Tuberculosis (Tb) Treatment In This Century. To Counteract The Prevalence Of Mtb Resistance,We Have Synthesized 2-Aryl Benzazole Based Dual Targeted Molecules. Compound 9M And 9N Were Found To Be Equally Active Against Replicating And Non-Replicating Form Of Mtb (Mic(Maba) 1.98 And 1.66 Mu G/ml; Mic(Lora) 2.06 And 1.59 Mu G/ml Respectively). They Arrested The Cell Division (Replicating Mtb) By Inhibiting The Gtpase Activity Of Ftsz With Ic50 Values 45 And 64 Mu M Respectively. They Were Also Capable Of Kill Mtb In Non-Replicating Form By Inhibiting The Biosynthesis Of Menaquinone Which Was Substantiated By The Meng Inhibition (Ic50 = 11.62 And 7.49 Mu M Respectively) Followed By The Vit-K2 Rescue Study And Atp Production Assay.
Doi:10.1016/j.Bioorg.2020.104170
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专利信息
专利号:US-9217012-B2
优先权日:2009-04-08
标题 :Inhibitors of protein tyrosine phosphatases
发明人:ZHANG ZHONG-YIN; ZHANG SHENG
权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP
摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:US-9700543-B2
优先权日:2011-05-31
标题 :GLP-1 receptor stabilizers and modulators
发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; BRAHMACHARY ENUGURTHI; YEAGER ADAM RICHARD
权利人:CELGENE INT II SÀRL
摘要:Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.