Identification and Repurposing of Trisubstituted Harmine Derivatives as Novel Inhibitors of Mycobacterium tuberculosis Phosphoserine Phosphatase
نویسندگان
چکیده
منابع مشابه
Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors†
Mycobacterium tuberculosis glutamine synthetase (MtGS) is a promising target for antituberculosis drug discovery. In a recent high-throughput screening study we identified several classes of MtGS inhibitors targeting the ATP-binding site. We now explore one of these classes, the 2-tert-butyl-4,5-diarylimidazoles, and present the design, synthesis, and X-ray crystallographic studies leading to t...
متن کاملTrisubstituted Pyrazolopyrimidines as Novel Angiogenesis Inhibitors
Current inhibitors of angiogenesis comprise either therapeutic antibodies (e.g. bevacicumab binding to VEGF-A) or small molecular inhibitors of receptor tyrosin kinases like e.g. sunitinib, which inhibits PDGFR and VEGFR. We have recently identified cyclin-dependent kinase 5 (Cdk5) as novel alternative and pharmacologically accessible target in the context of angiogenesis. In the present work w...
متن کاملSynthesis and Antimicrobial Evaluation of 4H-Pyrans and Schiff Bases Fused 4H-Pyran Derivatives as Inhibitors of Mycobacterium Bovis (BCG)
The focus of our study is the synthesis and biological activity evaluation of a series of 4H-Pyran compounds and schiff bases fused 4H-Pyran derivatives which are known to possess a wide variety of biological activities. In this paper at first a simple and efficient one-pot synthesis of 4H-Pyran s from the three-component reaction between malononitrile, aldehydes, and active methylene compounds...
متن کاملSynthesis and Antimicrobial Evaluation of 4H-Pyrans and Schiff Bases Fused 4H-Pyran Derivatives as Inhibitors of Mycobacterium Bovis (BCG)
The focus of our study is the synthesis and biological activity evaluation of a series of 4H-Pyran compounds and schiff bases fused 4H-Pyran derivatives which are known to possess a wide variety of biological activities. In this paper at first a simple and efficient one-pot synthesis of 4H-Pyran s from the three-component reaction between malononitrile, aldehydes, and active methylene compounds...
متن کاملNovel Group of Imidazole Derivatives as Atypical Selective Cyclooxygenase-2 Inhibitors: Design, Synthesis and Biological Evaluation
In this study, a new series of 5-substituted 1-benzyl-2-(methylsulfonyl)-1-H-imidazolewith atypical structure-activity relationship was designed, synthesized, and biologicalevaluated as selective cyclooxygenase-2 inhibitors. Docking studies revealed that althoughthe pharmacophoric substitute of the compound 5b, methylsulfonyl group, has been directlyattached to the central ring, it is in the sa...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Molecules
سال: 2020
ISSN: 1420-3049
DOI: 10.3390/molecules25020415