Discovery of an Orally Efficacious Pyrazolo[3,4-d]pyrimidine Benzoxaborole as a Potent Inhibitor of Cryptosporidium.
J Med Chem.
2025 Jan 9;68(1):832-849. doi: 10.1021/acs.jmedchem.4c02805. Epub 2024 Dec 23. PubMed PMID:
39714730.
Analogs of the anti-malaria drug mefloquine have broad-spectrum antifungal activity and are efficacious in a model of disseminated Candida auris infection.
Antimicrob Agents Chemother.
2024 Nov 6;68(11):e0130124. doi: 10.1128/aac.01301-24. Epub 2024 Oct 4. PubMed PMID:
39365066; PubMed Central PMCID:
PMC11539235.
Identification of potent and orally efficacious phosphodiesterase inhibitors in Cryptosporidium parvum-infected immunocompromised male mice.
Nat Commun.
2024 Sep 27;15(1):8272. doi: 10.1038/s41467-024-52658-y. PubMed PMID:
39333545; PubMed Central PMCID:
PMC11436873.
Major open questions in the hepatitis B and D field - Proceedings of the inaugural International emerging hepatitis B and hepatitis D researchers workshop.
Virology.
2024 Jul;595:110089. doi: 10.1016/j.virol.2024.110089. Epub 2024 Apr 16. PubMed PMID:
38640789; PubMed Central PMCID:
PMC11517827.
N-Hydroxypiridinedione: A Privileged Heterocycle for Targeting the HBV RNase H.
Molecules.
2024 Jun 20;29(12). doi: 10.3390/molecules29122942. PubMed PMID:
38931006; PubMed Central PMCID:
PMC11206691.
Synthesis and Antifungal Activity of Stereoisomers of Mefloquine Analogs.
ACS Med Chem Lett.
2024 Jun 13;15(6):822-827. doi: 10.1021/acsmedchemlett.4c00031. eCollection 2024 Jun 13. PubMed PMID:
38894917; PubMed Central PMCID:
PMC11181485.
Targeting CXCR4, VLA-4, and CXCR2 for hematopoietic stem cell mobilization.
Blood Adv.
2024 Mar 26;8(6):1379-1383. doi: 10.1182/bloodadvances.2023011653. PubMed PMID:
38190608; PubMed Central PMCID:
PMC10945136.
Identification and assessment of the 1,6-dihydroxy-pyridin-2-one moiety as privileged scaffold for HBV ribonuclease H inhibition.
Antiviral Res.
2024 Mar;223:105833. doi: 10.1016/j.antiviral.2024.105833. Epub 2024 Feb 5. PubMed PMID:
38325606; PubMed Central PMCID:
PMC11533872.
Comparative chemical genomics in Babesia species identifies the alkaline phosphatase PhoD as a determinant of antiparasitic resistance.
Proc Natl Acad Sci U S A.
2024 Feb 27;121(9):e2312987121. doi: 10.1073/pnas.2312987121. Epub 2024 Feb 20. PubMed PMID:
38377214; PubMed Central PMCID:
PMC10907312.
In Vitro Enzymatic and Cell Culture-Based Assays for Measuring Activity of HBV Ribonuclease H Inhibitors.
Methods Mol Biol.
2024;2837:257-270. doi: 10.1007/978-1-0716-4027-2_22. PubMed PMID:
39044091; PubMed Central PMCID:
PMC11514518.
In vitro evaluation of tropolone absorption, metabolism, and clearance.
Antiviral Res.
2023 Dec;220:105762. doi: 10.1016/j.antiviral.2023.105762. Epub 2023 Nov 22. PubMed PMID:
37996012; PubMed Central PMCID:
PMC10843707.
CWHM-974 is a fluphenazine derivative with improved antifungal activity against Candida albicans due to reduced susceptibility to multidrug transporter-mediated resistance mechanisms.
Antimicrob Agents Chemother.
2023 Oct 18;67(10):e0056723. doi: 10.1128/aac.00567-23. Epub 2023 Sep 13. PubMed PMID:
37702508; PubMed Central PMCID:
PMC10583685.
The anti-cancer efficacy of a novel phenothiazine derivative is independent of dopamine and serotonin receptor inhibition.
Front Oncol.
2023;13:1295185. doi: 10.3389/fonc.2023.1295185. eCollection 2023. PubMed PMID:
37909019; PubMed Central PMCID:
PMC10613967.
Safe and effective treatments are needed for cryptosporidiosis, a truly neglected tropical disease.
BMJ Glob Health.
2023 Aug;8(8). doi: 10.1136/bmjgh-2023-012540. PubMed PMID:
37541693; PubMed Central PMCID:
PMC10407372.
MEPicides: α,β-unsaturated Fosmidomycin N-Acyl Analogs as Efficient Inhibitors of Plasmodium falciparum 1-Deoxy-d-xylulose-5-phosphate reductoisomerase.
ACS Infect Dis.
2023 Jul 14;9(7):1387-1395. doi: 10.1021/acsinfecdis.3c00132. Epub 2023 Jun 13. PubMed PMID:
37310810; PubMed Central PMCID:
PMC10880585.
Structure-Activity Relationship Studies of the Aryl Acetamide Triazolopyridazines against Cryptosporidium Reveals Remarkable Role of Fluorine.
J Med Chem.
2023 Jun 22;66(12):7834-7848. doi: 10.1021/acs.jmedchem.3c00110. Epub 2023 Jun 2. PubMed PMID:
37267631; PubMed Central PMCID:
PMC11103792.
Comparative chemical genomics in Babesia species identifies the alkaline phosphatase phoD as a novel determinant of resistance.
bioRxiv.
2023 Jun 13;. doi: 10.1101/2023.06.13.544849. PubMed PMID:
37398106; PubMed Central PMCID:
PMC10312741.
Structure-Activity relationships of replacements for the triazolopyridazine of Anti-Cryptosporidium lead SLU-2633.
Bioorg Med Chem.
2023 May 15;86:117295. doi: 10.1016/j.bmc.2023.117295. Epub 2023 Apr 28. PubMed PMID:
37148788; PubMed Central PMCID:
PMC10201403.
Design, synthesis, and biological evaluation of novel sulfamoylbenzamide derivatives as HBV capsid assembly modulators.
Bioorg Chem.
2022 Dec;129:106192. doi: 10.1016/j.bioorg.2022.106192. Epub 2022 Oct 13. PubMed PMID:
36265355; PubMed Central PMCID:
PMC10591450.
Predicted structure of the hepatitis B virus polymerase reveals an ancient conserved protein fold.
Protein Sci.
2022 Oct;31(10):e4421. doi: 10.1002/pro.4421. PubMed PMID:
36173165; PubMed Central PMCID:
PMC9601786.
Synthetic derivatives of the antifungal drug ciclopirox are active against herpes simplex virus 2.
Eur J Med Chem.
2022 Aug 5;238:114443. doi: 10.1016/j.ejmech.2022.114443. Epub 2022 May 14. PubMed PMID:
35635945; PubMed Central PMCID:
PMC11103786.
Repurposing and optimization of drugs for discovery of novel antifungals.
Drug Discov Today.
2022 Jul;27(7):2008-2014. doi: 10.1016/j.drudis.2022.04.021. Epub 2022 Apr 27. Review. PubMed PMID:
35489676; PubMed Central PMCID:
PMC11182377.
Phosphoryl Prodrugs: Characteristics to Improve Drug Development.
Med Chem Res.
2022 Feb;31(2):207-216. doi: 10.1007/s00044-021-02766-x. Epub 2021 Jul 23. PubMed PMID:
35492863; PubMed Central PMCID:
PMC9053384.
Correction: Structure-guided microbial targeting of antistaphylococcal prodrugs.
Elife.
2021 Nov 25;10. doi: 10.7554/eLife.75743. PubMed PMID:
34821554; PubMed Central PMCID:
PMC8616559.
Efficient Inhibition of Hepatitis B Virus (HBV) Replication and cccDNA Formation by HBV Ribonuclease H Inhibitors during Infection.
Antimicrob Agents Chemother.
2021 Nov 17;65(12):e0146021. doi: 10.1128/AAC.01460-21. Epub 2021 Sep 13. PubMed PMID:
34516242; PubMed Central PMCID:
PMC8597750.
Mechanism of Action of N-Acyl and N-Alkoxy Fosmidomycin Analogs: Mono- and Bisubstrate Inhibition of IspC from Plasmodium falciparum, a Causative Agent of Malaria.
ACS Omega.
2021 Oct 26;6(42):27630-27639. doi: 10.1021/acsomega.1c01711. eCollection 2021 Oct 26. PubMed PMID:
34722963; PubMed Central PMCID:
PMC8552233.
Optimization of the Urea Linker of Triazolopyridazine MMV665917 Results in a New Anticryptosporidial Lead with Improved Potency and Predicted hERG Safety Margin.
J Med Chem.
2021 Aug 12;64(15):11729-11745. doi: 10.1021/acs.jmedchem.1c01136. Epub 2021 Aug 3. PubMed PMID:
34342443; PubMed Central PMCID:
PMC8792998.
Structure-guided microbial targeting of antistaphylococcal prodrugs.
Elife.
2021 Jul 19;10. doi: 10.7554/eLife.66657. PubMed PMID:
34279224; PubMed Central PMCID:
PMC8318587.
The Clofazimine for Treatment of Cryptosporidiosis in HIV-Infected Adults (CRYPTOFAZ) and Lessons Learned for Anticryptosporidial Drug Development.
Clin Infect Dis.
2021 Jul 15;73(2):192-194. doi: 10.1093/cid/ciaa425. PubMed PMID:
32277815; PubMed Central PMCID:
PMC8427724.
Spontaneous Selection of Cryptosporidium Drug Resistance in a Calf Model of Infection.
Antimicrob Agents Chemother.
2021 May 18;65(6). doi: 10.1128/AAC.00023-21. Print 2021 May 18. PubMed PMID:
33753338; PubMed Central PMCID:
PMC8316126.
Recent Advances in Hepatitis B Treatment.
Pharmaceuticals (Basel).
2021 May 1;14(5). doi: 10.3390/ph14050417. Review. PubMed PMID:
34062711; PubMed Central PMCID:
PMC8147224.
Synthetic Derivatives of Ciclopirox are Effective Inhibitors of Cryptococcus neoformans.
ACS Omega.
2021 Mar 30;6(12):8477-8487. doi: 10.1021/acsomega.1c00273. eCollection 2021 Mar 30. PubMed PMID:
33817509; PubMed Central PMCID:
PMC8015083.
Antimicrobial Prodrug Activation by the Staphylococcal Glyoxalase GloB.
ACS Infect Dis.
2020 Nov 13;6(11):3064-3075. doi: 10.1021/acsinfecdis.0c00582. Epub 2020 Oct 29. PubMed PMID:
33118347; PubMed Central PMCID:
PMC8543975.
Cryptosporidiosis should be designated as a tropical disease by the US Food and Drug Administration.
PLoS Negl Trop Dis.
2020 Jul;14(7):e0008252. doi: 10.1371/journal.pntd.0008252. eCollection 2020 Jul. PubMed PMID:
32614819; PubMed Central PMCID:
PMC7332027.
Potent, specific MEPicides for treatment of zoonotic staphylococci.
PLoS Pathog.
2020 Jun;16(6):e1007806. doi: 10.1371/journal.ppat.1007806. eCollection 2020 Jun. PubMed PMID:
32497104; PubMed Central PMCID:
PMC7297381.
Identification of 4-Amino-Thieno[2,3-d]Pyrimidines as QcrB Inhibitors in Mycobacterium tuberculosis.
mSphere.
2019 Sep 11;4(5). doi: 10.1128/mSphere.00606-19. PubMed PMID:
31511370; PubMed Central PMCID:
PMC6739496.
Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy.
J Pharmacol Exp Ther.
2019 Aug;370(2):219-230. doi: 10.1124/jpet.119.259663. Epub 2019 Jun 12. PubMed PMID:
31189728; PubMed Central PMCID:
PMC6652132.
Phosphonate prodrugs: an overview and recent advances.
Future Med Chem.
2019 Jul;11(13):1625-1643. doi: 10.4155/fmc-2018-0591. Review. PubMed PMID:
31469328; PubMed Central PMCID:
PMC6722485.
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-N-(4-arylpyrrolidin-3-yl)acetamides.
ACS Med Chem Lett.
2019 Jun 13;10(6):966-971. doi: 10.1021/acsmedchemlett.9b00123. eCollection 2019 Jun 13. PubMed PMID:
31223456; PubMed Central PMCID:
PMC6580545.
Targeting VLA4 integrin and CXCR2 mobilizes serially repopulating hematopoietic stem cells.
J Clin Invest.
2019 May 14;129(7):2745-2759. doi: 10.1172/JCI124738. PubMed PMID:
31085833; PubMed Central PMCID:
PMC6597242.
Chemical Approaches to Inhibiting the Hepatitis B Virus Ribonuclease H.
ACS Infect Dis.
2019 May 10;5(5):655-658. doi: 10.1021/acsinfecdis.8b00045. Epub 2018 Mar 22. Review. PubMed PMID:
29565562; PubMed Central PMCID:
PMC7202671.
4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.
J Med Chem.
2019 Apr 11;62(7):3503-3512. doi: 10.1021/acs.jmedchem.8b01972. Epub 2019 Mar 22. PubMed PMID:
30856324; PubMed Central PMCID:
PMC6727846.
Endonuclease Activity Inhibition of the NS1 Protein of Parvovirus B19 as a Novel Target for Antiviral Drug Development.
Antimicrob Agents Chemother.
2019 Mar;63(3). doi: 10.1128/AAC.01879-18. Print 2019 Mar. PubMed PMID:
30530599; PubMed Central PMCID:
PMC6395930.
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
J Med Chem.
2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. PubMed PMID:
30130103.
Synthesis and Evaluation of Troponoids as a New Class of Antibiotics.
ACS Omega.
2018 Nov 30;3(11):15125-15133. doi: 10.1021/acsomega.8b01754. Epub 2018 Nov 8. PubMed PMID:
30533576; PubMed Central PMCID:
PMC6275967.
MEPicides: α,β-Unsaturated Fosmidomycin Analogues as DXR Inhibitors against Malaria.
J Med Chem.
2018 Oct 11;61(19):8847-8858. doi: 10.1021/acs.jmedchem.8b01026. Epub 2018 Sep 24. PubMed PMID:
30192536; PubMed Central PMCID:
PMC6300130.
Antifungal Phenothiazines: Optimization, Characterization of Mechanism, and Modulation of Neuroreceptor Activity.
ACS Infect Dis.
2018 Apr 13;4(4):499-507. doi: 10.1021/acsinfecdis.7b00157. Epub 2017 Nov 2. PubMed PMID:
29058407; PubMed Central PMCID:
PMC8994671.
A Novel Piperazine-Based Drug Lead for Cryptosporidiosis from the Medicines for Malaria Venture Open-Access Malaria Box.
Antimicrob Agents Chemother.
2018 Apr;62(4). doi: 10.1128/AAC.01505-17. Print 2018 Apr. PubMed PMID:
29339392; PubMed Central PMCID:
PMC5913971.
Clinical and microbiologic efficacy of the piperazine-based drug lead MMV665917 in the dairy calf cryptosporidiosis model.
PLoS Negl Trop Dis.
2018 Jan;12(1):e0006183. doi: 10.1371/journal.pntd.0006183. eCollection 2018 Jan. PubMed PMID:
29309415; PubMed Central PMCID:
PMC5774826.
Plasmepsins IX and X are essential and druggable mediators of malaria parasite egress and invasion.
Science.
2017 Oct 27;358(6362):518-522. doi: 10.1126/science.aan1478. PubMed PMID:
29074774; PubMed Central PMCID:
PMC5928414.
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