Publications

Fuchs N, Zimmermann R.A, Schwickert M, Gunkel A, Zimmer C, Meta M, Schwickert K, Keiser J, Haeberli C, Kiefer W, Schirmeister T. Dual strategy to design new agents targeting Schistosoma mansoni: advancing phenotypic and SmCB1 inhibitors for improved efficacy. ACS Infect Dis. 2024;10(5):1664-1678. DOI: 10.1021/acsinfecdis.4c00020

Kuevi D.N.O, Keiser J, Häberli C, Owusu-Senyah A.K, Ahiabu M.K. In vitro antischistosomal activity of Bridelia ferruginea, Clausena anisata, Khaya senegalensis, and Vernonia amygdalina. J Trop Med. 2024;2024:8074291. DOI: 10.1155/2024/8074291

Leas D.A, Keiser J, Charman S.A, Shackleford D.M, Jones J.O, Campbell M, Chen G, Katneni K, Patil R, Hu M, Pham T, Häberli C, Schulze T.T, Neville A.J, Wang X, Dong Y, Davis P.H, Vennerstrom J.L. Single-Dose Drug Development Candidate for Schistosomiasis. ACS Infect Dis. 2024(in press). DOI: 10.1021/acsinfecdis.4c00677

Ren R, Leas D.A, Häberli C, Cal M, Chen G, Katneni K, Dong Y, Kaiser M, Keiser J, Charman S.A, Vennerstrom J.L. Medium-ring keto bislactams with antischistosomal activity. J Med Chem. 2024;67(20):18235-18246. DOI: 10.1021/acs.jmedchem.4c01532

Shanley H.T, Taki A.C, Nguyen N, Wang T, Byrne J.J, Ang C.S, Leeming M.G, Nie S, Williamson N, Zheng Y, Young N.D, Korhonen P.K, Hofmann A, Chang B.C.H, Wells T.N.C, Häberli C, Keiser J, Jabbar A, Sleebs B.E, Gasser R.B. Structure-activity relationship and target investigation of 2-aryl quinolines with nematocidal activity. Int J Parasitol Drugs Drug Resist. 2024;24:100522. DOI: 10.1016/j.ijpddr.2024.100522

Biendl S, Häberli C, Chen G, Wang W, Zhong L, Saunders J, Pham T, Wang X, Wu J, Charman S.A, Vennerstrom J.L, Keiser J. In vitro and in vivo antischistosomal activity profiling and pharmacokinetics of ozonide carboxylic acids. ACS Infect Dis. 2023;9(3):643-652. DOI: 10.1021/acsinfecdis.2c00581

D'Abbrunzo I, Bianco E, Gigli L, Demitri N, Birolo R, Chierotti M.R, Škorić I, Keiser J, Häberli C, Voinovich D, Hasa D, Perissutti B. Praziquantel meets Niclosamide: a dual-drug antiparasitic cocrystal. Int J Pharm. 2023;644:123315. DOI: 10.1016/j.ijpharm.2023.123315

Kasago F.M, Häberli C, Keiser J, Masamba W. Design, synthesis and evaluation of praziquantel analogues and new molecular hybrids as potential antimalarial and anti-schistosomal agents. Molecules. 2023;28(13):5184. DOI: 10.3390/molecules28135184

Muya K, Kalonji M, Ilunga N.W, Maseho M, Kitambala M, Kalonda M, Ndoumba K, Byanga K, Wright C.W, Häberli C, Keiser J, Simbi L. Evaluation of 43 species of Congolese medicinal plants used traditionally for the treatment of schistosomiasis leading to the isolation of an anti-schistosomal phaeophytin from Pseudolachnostylis maprouneifolia Pax. J Ethnopharmacol. 2023;315:116688. DOI: 10.1016/j.jep.2023.116688

Noce B, Di Bello E, Zwergel C, Fioravanti R, Valente S, Rotili D, Masotti A, Ansari M.S.Z, Trisciuoglio D, Chakrabarti A, Romier C, Robaa D, Sippl W, Jung M, Häberli C, Keiser J, Mai A. Chemically diverse S. mansoni HDAC8 inhibitors reduced viability in worm larval and adult stages. ChemMedChem. 2023;18(3):e202200510. DOI: 10.1002/cmdc.202200510

Angeli A, Ferraroni M, Carta F, Häberli C, Keiser J, Costantino G, Supuran C.T. Development of praziquantel sulphonamide derivatives as antischistosomal drugs. J Enzyme Inhib Med Chem. 2022;37(1):1479-1494. DOI: 10.1080/14756366.2022.2078970

Biendl S, Häberli C, Keiser J. Discovery of novel antischistosomal scaffolds from the open access Pandemic Response Box. Expert Rev Anti Infect Ther. 2022;20(4):621-629. DOI: 10.1080/14787210.2022.1990042

Cantara A, Luo Y, Dobrovolna M, Bohalova N, Fojta M, Verga D, Guittat L, Cucchiarini A, Savrimoutou S, Häberli C, Guillon J, Keiser J, Brazda V, Mergny J.L. G-quadruplexes in helminth parasites. Nucleic Acids Res. 2022;50(5):2719-2735. DOI: 10.1093/nar/gkac129

Di Bello E, Noce B, Fioravanti R, Zwergel C, Valente S, Rotili D, Fianco G, Trisciuoglio D, Mourão M.M, Sales P. Jr, Lamotte S, Prina E, Späth G.F, Häberli C, Keiser J, Mai A. Effects of structurally different HDAC inhibitors against Trypanosoma cruzi, Leishmania, and Schistosoma mansoni. ACS Infect Dis. 2022;8(7):1356-1366. DOI: 10.1021/acsinfecdis.2c00232

Dube M, Llanes D, Saoud M, Rennert R, Imming P, Häberli C, Keiser J, Arnold N. Albatrellus confluens (Alb. & Schwein.) Kotl. & Pouz.: natural fungal compounds and synthetic derivatives with in vitro anthelmintic activities and antiproliferative effects against two human cancer cell lines. Molecules. 2022;27(9):2950. DOI: 10.3390/molecules27092950

Dube M, Raphane B, Sethebe B, Seputhe N, Tiroyakgosi T, Imming P, Häberli C, Keiser J, Arnold N, Andrae-Marobela K. Medicinal plant preparations administered by Botswana traditional health practitioners for treatment of worm infections show anthelmintic activities. Plants (Basel). 2022;11(21):2945. DOI: 10.3390/plants11212945

Hamway Y, Zimmermann K, Blommers M.J.J, Sousa M, Häberli C, Kulkarni S, Skalicky S, Hackl M, Götte M, Keiser J, da Costa C.P, Spangenberg T, Azzaoui K. Modulation of host-parasite interactions with small molecules targeting Schistosoma mansoni microRNAs. ACS Infect Dis. 2022;8:2028−2034. DOI: 10.1021/acsinfecdis.2c00360

Harrington S, Knox J.J, Burns A.R, Choo K.L, Au A, Kitner M, Häberli C, Pyche J, D'Amata C, Kim Y.H, Volpatti J.R, Guiliani M, Snider J, Wong V, Palmeira B.M, Redman E.M, Vaidya A.S, Gilleard J.S, Stagljar I, Cutler S.R, Kulke D, Dowling J.J, Yip C.M, Keiser J, Zasada I, Lautens M, Roy P.J. Egg-laying and locomotory screens with C. elegans yield a nematode-selective small molecule stimulator of neurotransmitter release. Commun Biol. 2022;5:865. DOI: 10.1038/s42003-022-03819-6

Hassan M.M, Sedighi A, Olaoye O.O, Häberli C, Merz A, Ramos-Morales E, de Araujo E.D, Romier C, Jung M, Keiser J, Gunning P.T. Phenotypic screening of histone deacetylase (HDAC) inhibitors against Schistosoma mansoni. ChemMedChem. 2022:e202100622. DOI: 10.1002/cmdc.202100622

Kersting L, Kuhn L, Anokhin M, Schuster F, Häberli C, Sambyal S, Kumar H.M.S, Keiser J, Alabugin I, Tsogoeva S.B. Visible-light-driven metal-free C-H functionalization: access to new bioactive tetrahydroisoquinoline-butenolide hybrids via domino amine oxidation/vinylogous Mannich reaction. ChemPhotoChem. 2022;6(8):e202200109. DOI: 10.1002/cptc.202200109

Ren R, Wang X, Leas D.A, Häberli C, Cal M, Dong Y, Kaiser M, Keiser J, Vennerstrom J.L. Antischistosomal tetrahydro-γ-carboline sulfonamides. Bioorg Med Chem Lett. 2022;59:128546. DOI: 10.1016/j.bmcl.2022.128546

Schneeberger P.H.H, Gueuning M, Welsche S, Hürlimann E, Dommann J, Häberli C, Frey J.E, Sayasone S, Keiser J. Different gut microbial communities correlate with efficacy of albendazole-ivermectin against soil-transmitted helminthiases. Nat Commun. 2022;13:1063. DOI: 10.1038/s41467-022-28658-1

Taki A.C, Wang T, Nguyen N.N, Ang C.S, Leeming M.G, Nie S, Byrne J.J, Young N.D, Zheng Y, Ma G, Korhonen P.K, Koehler A.V, Williamson N.A, Hofmann A, Chang B.C.H, Häberli C, Keiser J, Jabbar A, Sleebs B.E, Gasser R.B. Thermal proteome profiling reveals Haemonchus orphan protein HCO_011565 as a target of the nematocidal small molecule UMW-868. Front Pharmacol. 2022;13:1014804. DOI: 10.3389/fphar.2022.1014804

Valderas-García E, Häberli C, Álvarez-Bardón M, Escala N, Castilla-Gómez de Agüero V, de la Vega J, Del Olmo E, Balaña-Fouce R, Keiser J, Martínez-Valladares M. Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus. Parasit Vectors. 2022;15:243. DOI: 10.1186/s13071-022-05347-y

Buchter V, Hofmann D, Häberli C, Keiser J. Characterization of moxidectin against Strongyloides ratti: in vitro and in vivo activity and pharmacokinetics in the rat model. ACS Infect Dis. 2021;7(5):1069-1076. DOI: 10.1021/acsinfecdis.0c00435

Debbert S.L, Hintz M.J, Bell C.J, Earl K.R, Forsythe G.E, Häberli C, Keiser J. Activities of quinoxaline, nitroquinoxaline and [1,2,4]triazolo[4,3-a]quinoxaline analogs of MMV007204 against Schistosoma mansoni. Antimicrob Agents Chemother. 2021;65(3):e01370-20. DOI: 10.1128/AAC.01370-20

Dube M, Saoud M, Rennert R, Fotso G.W, Andrae-Marobela K, Imming P, Häberli C, Keiser J, Arnold N. Anthelmintic activity and cytotoxic effects of compounds isolated from the fruits of Ozoroa insignis del. (Anacardiaceae). Biomolecules. 2021;11(12):1893. DOI: 10.3390/biom11121893

Keiser J, Häberli C. Evaluation of commercially available anthelminthics in laboratory models of human intestinal nematode infections. ACS Infect Dis. 2021;7(5):1177-1185. DOI: 10.1021/acsinfecdis.0c00719

Keiser J, Häberli C. Assessment of FDA-approved drugs against Strongyloides ratti in vitro and in vivo to identify potentially active drugs against strongyloidiasis. Parasit Vectors. 2021;14:615. DOI: 10.1186/s13071-021-05117-2

Nguyen W, Lee E.F, Evangelista M, Lee M, Harris T.J, Colman P.M, Smith N.A, Williams L.B, Jarman K.E, Lowes K.N, Häberli C, Keiser J, Smith B.J, Fairlie W.D, Sleebs B.E. Optimization of benzothiazole and thiazole hydrazones as inhibitors of schistosome bcl-2a. ACS Infect Dis. 2021;7(5):1143-1163. DOI: 10.1021/acsinfecdis.0c00700

Partridge F.A, Bataille C.J.R, Forman R, Marriott A.E, Forde-Thomas J, Häberli C, Dinsdale R.L, O'Sullivan J.D.B, Willis N.J, Wynne G.M, Whiteland H, Archer J, Steven A, Keiser J, Turner J.D, Hoffmann K.F, Taylor M.J, Else K.J, Russell A.J, Sattelle D.B. Structural requirements for dihydrobenzoxazepinone anthelmintics: actions against medically important and model parasites: Trichuris muris, Brugia malayi, Heligmosomoides polygyrus, and Schistosoma mansoni. ACS Infect Dis. 2021;7(5):1260-1274. DOI: 10.1021/acsinfecdis.1c00025

Probst A, Chisanga K, Dziwornu G.A, Häberli C, Keiser J, Chibale K. Expanding the activity profile of pyrido[1,2-a]benzimidazoles: synthesis and evaluation of novel n(1)-1-phenylethanamine derivatives against Schistosoma mansoni. ACS Infect Dis. 2021;7(5):1032-1043. DOI: 10.1021/acsinfecdis.0c00278

Probst A, Pujol E, Häberli C, Keiser J, Vázquez S. In vitro, in vivo, and ADME evaluation of SF5-containing N,N'-diarylureas as antischistosomal agents. Antimicrob Agents Chemother. 2021;65(10):e0061521. DOI: 10.1128/aac.00615-21

Sirak B, Asres K, Hailu A, Dube M, Arnold N, Häberli C, Keiser J, Imming P. In vitro antileishmanial and antischistosomal activities of anemonin isolated from the fresh leaves of Ranunculus multifidus forsk. Molecules. 2021;26(24):7473. DOI: 10.3390/molecules26247473

Lin Y, Ong Y.C, Keller S, Karges J, Bouchene R, Manoury E, Blacque O, Müller J, Anghel N, Hemphill A, Häberli C, Taki A.C, Gasser R.B, Cariou K, Keiser J, Gasser G. Synthesis, characterization and antiparasitic activity of organometallic derivatives of the anthelmintic drug albendazole. Dalton Trans. 2020;49(20):6616-6626. DOI: 10.1039/d0dt01107j

Probst A, Häberli C, Siegel D, Huang J, Vigneron S, Ta A.P, Skinner D.E, El-Sakkary N, Momper J.D, Gangoiti J, Dong Y, Vennerstrom J.L, Charman S.A, Caffrey C.R, Keiser J. Efficacy, metabolism and pharmacokinetics of Ro 15-5458, a forgotten schistosomicidal 9-acridanone hydrazone. J Antimicrob Chemother. 2020:dkaa247. DOI: 10.1093/jac/dkaa247

Wu J, Wang X, Chiu F.C.K, Häberli C, Shackleford D.M, Ryan E, Kamaraj S, Bulbule V.J, Wallick A.I, Dong Y, White K.L, Davis P.H, Charman S.A, Keiser J, Vennerstrom J.L. Structure-activity relationship of antischistosomal ozonide carboxylic acids. J Med Chem. 2020;63(7):3723-3736. DOI: 10.1021/acs.jmedchem.0c00069

Karpstein T, Pasche V, Häberli C, Scandale I, Neodo A, Keiser J. Evaluation of emodepside in laboratory models of human intestinal nematode and schistosome infections. Parasit Vectors. 2019;12:226. DOI: 10.1186/s13071-019-3476-x

Mayoka G, Keiser J, Häberli C, Chibale K. Structure–activity relationship and in vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) studies of N-aryl 3-trifluoromethyl pyrido[1,2-a]benzimidazoles that are efficacious in a mouse model of schistos. ACS Infect Dis. 2019;5(3):418-429. DOI: 10.1021/acsinfecdis.8b00313

Wu J, Wang C, Häberli C, White K.L, Shackleford D.M, Chen G, Dong Y, Charman S.A, Keiser J, Vennerstrom J.L. SAR of a new antischistosomal urea carboxylic acid. Bioorg Med Chem Lett. 2018;28(23-24):3648-3651. DOI: 10.1016/j.bmcl.2018.10.039