Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b.

Autor: Awalt JK; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Su W; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Nguyen W; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Loi K; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia., Jarman KE; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Penington JS; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Ramesh S; Research School of Biology, The Australian National University, Canberra, 2600, Australia., Fairhurst KJ; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY, USA; Center for Malaria Therapeutics and Antimicrobial Resistance, Columbia University Irving Medical Center, New York, NY, USA., Yeo T; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY, USA; Center for Malaria Therapeutics and Antimicrobial Resistance, Columbia University Irving Medical Center, New York, NY, USA., Park H; Center for Malaria Therapeutics and Antimicrobial Resistance, Columbia University Irving Medical Center, New York, NY, USA; Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, NY, USA., Uhlemann AC; Center for Malaria Therapeutics and Antimicrobial Resistance, Columbia University Irving Medical Center, New York, NY, USA; Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, NY, USA., Chandra Maity B; TCG Lifesciences, Kolkata, West Bengal, 700091, India., De N; TCG Lifesciences, Kolkata, West Bengal, 700091, India., Mukherjee P; TCG Lifesciences, Kolkata, West Bengal, 700091, India., Chakraborty A; TCG Lifesciences, Kolkata, West Bengal, 700091, India., Churchyard A; Department of Life Sciences, Imperial College London, South Kensington, SW7 2AZ, UK., Famodimu MT; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, UK., Delves MJ; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, UK., Baum J; Department of Life Sciences, Imperial College London, South Kensington, SW7 2AZ, UK; School of Biomedical Sciences, University of New South Wales, Sydney, 2031, Australia., Mittal N; School of Medicine, University of California San Diego, La Jolla, CA, 92093, USA., Winzeler EA; School of Medicine, University of California San Diego, La Jolla, CA, 92093, USA., Papenfuss AT; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Chowdury M; School of Medicine, Deakin University, Waurn Ponds, Victoria, 3216, Australia; Institute for Mental and Physical Health and Clinical Translation, Deakin University, Geelong, Victoria, 3216, Australia., de Koning-Ward TF; School of Medicine, Deakin University, Waurn Ponds, Victoria, 3216, Australia; Institute for Mental and Physical Health and Clinical Translation, Deakin University, Geelong, Victoria, 3216, Australia., Maier AG; Research School of Biology, The Australian National University, Canberra, 2600, Australia., van Dooren GG; Research School of Biology, The Australian National University, Canberra, 2600, Australia., Baud D; Medicines for Malaria Venture, Geneva, 1215, Switzerland., Brand S; Medicines for Malaria Venture, Geneva, 1215, Switzerland., Fidock DA; Department of Microbiology & Immunology, Columbia University Irving Medical Center, New York, NY, USA; Center for Malaria Therapeutics and Antimicrobial Resistance, Columbia University Irving Medical Center, New York, NY, USA; Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, NY, USA., Jackson PF; Global Public Health, Janssen R&D LLC, La Jolla, 92121, USA., Cowman AF; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia., Dans MG; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia. Electronic address: dans.m@wehi.edu.au., Sleebs BE; The Walter and Eliza Hall Institute of Medical Research, Parkville, 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, 3010, Australia. Electronic address: sleebs@wehi.edu.au.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2024 Dec 15; Vol. 280, pp. 116921. Date of Electronic Publication: 2024 Oct 03.

Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4.

Autor: Ashton TD; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Calic PPS; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Dans MG; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Ooi ZK; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia., Zhou Q; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia., Palandri J; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Loi K; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Jarman KE; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Qiu D; Research School of Biology, Australian National University, Canberra 2601, Australia., Lehane AM; Research School of Biology, Australian National University, Canberra 2601, Australia., Maity BC; TCG Lifesciences, Kolkata, West Bengal 700091, India., De N; TCG Lifesciences, Kolkata, West Bengal 700091, India., Giannangelo C; Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia., MacRaild CA; Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia., Creek DJ; Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia., Mao EY; Research Centre for Infectious Diseases, School of Biological Sciences, University of Adelaide, Adelaide 5005, Australia., Gancheva MR; Research Centre for Infectious Diseases, School of Biological Sciences, University of Adelaide, Adelaide 5005, Australia., Wilson DW; Research Centre for Infectious Diseases, School of Biological Sciences, University of Adelaide, Adelaide 5005, Australia., Chowdury M; School of Medicine, Deakin University, Waurn Ponds, Victoria 3216, Australia.; Institute for Mental and Physical Health and Clinical Translation, Deakin University, Geelong, Victoria 3216, Australia., de Koning-Ward TF; School of Medicine, Deakin University, Waurn Ponds, Victoria 3216, Australia.; Institute for Mental and Physical Health and Clinical Translation, Deakin University, Geelong, Victoria 3216, Australia., Famodimu MT; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K., Delves MJ; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K., Pollard H; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K., Sutherland CJ; Department of Infection Biology, London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K., Baud D; MMV Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, Geneva 1215, Switzerland., Brand S; MMV Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, Geneva 1215, Switzerland., Jackson PF; Emerging Science & Innovation, Discovery Sciences, Janssen R&D LLC, La Jolla, California 92121, United States., Cowman AF; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Sleebs BE; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2024 Aug 22; Vol. 67 (16), pp. 14493-14523. Date of Electronic Publication: 2024 Aug 12.

7- N -Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc 1 Complex.

Autor: Nguyen W; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Dans MG; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Currie I; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Awalt JK; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Bailey BL; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Lumb C; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia., Ngo A; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia., Favuzza P; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Palandri J; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Ramesh S; Research School of Biology, The Australian National University, Canberra 2600, Australia., Penington J; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Jarman KE; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Mukherjee P; TCG Lifesciences, Kolkata, West Bengal 700091, India., Chakraborty A; TCG Lifesciences, Kolkata, West Bengal 700091, India., Maier AG; Research School of Biology, The Australian National University, Canberra 2600, Australia., van Dooren GG; Research School of Biology, The Australian National University, Canberra 2600, Australia., Papenfuss T; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Wittlin S; Swiss Tropical and Public Health Institute, Kreuzstrasse 2, 4123 Allschwil, Switzerland.; University of Basel, 4003 Basel, Switzerland., Churchyard A; Department of Life Sciences, Imperial College London, South Kensington, SW7 2AZ U.K., Baum J; Department of Life Sciences, Imperial College London, South Kensington, SW7 2AZ U.K.; School of Biomedical Sciences, University of New South Wales, Sydney 2031, Australia., Winzeler EA; School of Medicine, University of California San Diego, 9500 Gilman Drive 0760, La Jolla, California 92093, United States., Baud D; Medicines for Malaria Venture, Geneva 1215, Switzerland., Brand S; Medicines for Malaria Venture, Geneva 1215, Switzerland., Jackson PF; Global Public Health, Janssen R&D LLC, La Jolla, California 92121, United States., Cowman AF; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia., Sleebs BE; The Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Australia.; Department of Medical Biology, The University of Melbourne, Parkville 3010, Australia.

Publikováno v: ACS infectious diseases [ACS Infect Dis] 2023 Mar 10; Vol. 9 (3), pp. 668-691. Date of Electronic Publication: 2023 Feb 28.

The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.

Autor: de Lera Ruiz M; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Favuzza P; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia.; University of Melbourne, Melbourne, VIC3010, Australia., Guo Z; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Zhao L; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Hu B; WuXi AppTec, 288 Fute Zhong Lu, Shanghai200131, China., Lei Z; WuXi AppTec, 288 Fute Zhong Lu, Shanghai200131, China., Zhan D; WuXi AppTec, 288 Fute Zhong Lu, Shanghai200131, China., Murgolo N; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Boyce CW; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Vavrek M; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Thompson J; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia., Ngo A; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia., Jarman KE; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia., Robbins J; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Boddey J; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia.; University of Melbourne, Melbourne, VIC3010, Australia., Sleebs BE; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia.; University of Melbourne, Melbourne, VIC3010, Australia., Lowes KN; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia.; University of Melbourne, Melbourne, VIC3010, Australia., Cowman AF; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia.; University of Melbourne, Melbourne, VIC3010, Australia., Olsen DB; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., McCauley JA; Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 Oct 12; Vol. 13 (11), pp. 1745-1754. Date of Electronic Publication: 2022 Oct 12 (Print Publication: 2022).

Insights Into Drug Repurposing, as Well as Specificity and Compound Properties of Piperidine-Based SARS-CoV-2 PLpro Inhibitors.

Autor: Calleja DJ; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Kuchel N; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Lu BGC; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Birkinshaw RW; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Klemm T; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Doerflinger M; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Cooney JP; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Mackiewicz L; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Au AE; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Yap YQ; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Blackmore TR; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Katneni K; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia., Crighton E; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia., Newman J; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Biomedical Program, Parkville, VIC, Australia., Jarman KE; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Call MJ; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Lechtenberg BC; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Czabotar PE; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Pellegrini M; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Charman SA; Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia., Lowes KN; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Mitchell JP; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Nachbur U; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia., Lessene G; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia.; Department of Pharmacology and Therapeutics, The University of Melbourne, Melbourne, VIC, Australia., Komander D; Department of Medical Biology, Walter and Eliza Hall Institute, University of Melbourne, Melbourne, VIC, Australia.

Publikováno v: Frontiers in chemistry [Front Chem] 2022 Apr 12; Vol. 10, pp. 861209. Date of Electronic Publication: 2022 Apr 12 (Print Publication: 2022).