Expanding Benzoxazole-Based Inosine 5′-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure–Activity As Potential Antituberculosis Agents
نویسندگان
چکیده
منابع مشابه
Inosine 5 0 - Monophosphate Dehydrogenase
I. Overview of IMPDH A. Protein Structures II. Medicinal Applications of IMPDH Inhibitors A. IMP Analogs B. NAD Analogs C. Natural Product Inhibitors D. Novel Synthetic Inhibitors III. Kinetic Mechanism and Substrate Interactions A. Case Studies 1. Tritrichomonas foetus IMPDH 2. Escherichia coli IMPDH 3. Human IMPDH B. Ligand Binding 1. IMP Binding Site 2. NAD Binding Site IV. Chemical Mechanis...
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Cryptosporidium parvum is the common enteric protozoan pathogen causing cryptosporidiosis in human. Available drugs to treat cryptosporidiosis are ineffective and there is yet no vaccine against C. parvum. Therefore, it is of interest to design an improved yet effective drug against C. parvum. Here, we docked benzoxazole derivatives (collected from literature) with inosine 5`- monophosphate deh...
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This study aimed to evaluate the trypanocidal activity of mycophenolic acid (MPA) and its derivatives for Trypanosoma congolense The proliferation of T. congolense was completely inhibited by adding <1 μM MPA and its derivatives. In addition, the IMP dehydrogenase in T. congolense was molecularly characterized as the target of these compounds. The results suggest that MPA and its derivatives ha...
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Inosine-5'-monophosphate dehydrogenase (IMPDH) is an attractive drug target for the control of parasitic infections. The enzyme catalyzes the NAD-dependent oxidation of inosine monophosphate (IMP) to xanthosine monophosphate (XMP), the committed step in guanosine monophosphate (GMP) biosynthesis. We have determined the crystal structures of IMPDH from the protozoan parasite Tritrichomonas foetu...
متن کاملRecent advances on the enantioselective synthesis of C-nucleosides inhibitors of inosine monophosphate dehydrogenase (IMPDH).
This review will describe the recent advances in the synthesis of C-nucleosides with inhibitory activity of inosine monophosphate dehydrogenase (IMPDH), a key enzyme in the biosynthesis of guanine nucleotides. The review will cover synthetic approaches of structural analogues showing modifications in the furanose ring as well as in the heterocyclic base. Heterocyclic sugar nucleoside analogues ...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2018
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.7b01839