ArticleBioorganic & medicinal chemistry letters2012
Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed.
- Molecular pathogenesis of Cryptosporidium and advancements in therapeutic interventions.Parasite (Paris, France) · 2025Review
- An update onJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2022Review
- The Enzymatic Activity of Inosine 5'-Monophosphate Dehydrogenase May Not Be a Vulnerable Target forACS infectious diseases · 2021Article
- Discovery of Novel GMPS Inhibitors ofBiology · 2021Article
- A probable means to an end: exploring P131 pharmacophoric scaffold to identify potential inhibitors of Cryptosporidium parvum inosine monophosphate dehydrogenase.Journal of molecular modeling · 2021Article
- Mycophenolic anilides as broad specificity inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors.Bioorganic & medicinal chemistry letters · 2020Article
- Evaluation of Bronopol and Disulfiram as PotentialMolecules (Basel, Switzerland) · 2020Article
- Targeting Genome Integrity inMolecules (Basel, Switzerland) · 2020Review
- Genetic ablation of purine salvage inProceedings of the National Academy of Sciences of the United States of America · 2019Article
- Inhibitors of inosine 5'-monophosphate dehydrogenase as emerging new generation antimicrobial agents.MedChemComm · 2019Review
- Identification of selective inhibitors of Helicobacter pylori IMPDH as a targeted therapy for the infection.Scientific reports · 2019Article
- Expanding Benzoxazole-Based Inosine 5'-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents.Journal of medicinal chemistry · 2018Article
- Benzoxazoles, Phthalazinones, and Arylurea-Based Compounds with IMP Dehydrogenase-Independent Antibacterial Activity against Francisella tularensis.Antimicrobial agents and chemotherapy · 2017Article
- Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives and Analogs Targeting the NLRP3 Inflammasome.Molecules (Basel, Switzerland) · 2017Article
- Development of Small Molecules with a Noncanonical Binding Mode to HIV-1 Trans Activation Response (TAR) RNA.Journal of medicinal chemistry · 2016Article
- Inhibition of Inosine-5'-monophosphate Dehydrogenase from Bacillus anthracis: Mechanism Revealed by Pre-Steady-State Kinetics.Biochemistry · 2016Article
- A Proposed Target Product Profile and Developmental Cascade for New Cryptosporidiosis Treatments.PLoS neglected tropical diseases · 2015Article
- Structure of Cryptosporidium IMP dehydrogenase bound to an inhibitor with in vivo antiparasitic activity.Acta crystallographica. Section F, Structural biology communications · 2015Article
- A novel cofactor-binding mode in bacterial IMP dehydrogenases explains inhibitor selectivity.The Journal of biological chemistry · 2015Article
- Mycobacterium tuberculosis IMPDH in Complexes with Substrates, Products and Antitubercular Compounds.PloS one · 2015Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5'-monophosphate dehydrogenase (IMPDH). Thus the inhibition of the parasite IMPDH presents a potential strategy for treating Cryptosporidium infections. A selective benzimidazole-based inhibitor of C. parvum IMPDH (CpIMPDH) was previously identified in a high throughput screen. Here we report a structure-activity relationship study of benzimidazole-based compounds that resulted in potent and selective inhibitors of CpIMPDH. Several compounds display potent antiparasitic activity in vitro.
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