ArticleACS infectious diseases2025
Identification of Substituted 4-Aminocinnolines as Broad-Spectrum Antiparasitic Agents.
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Article in ACS infectious diseases, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
32 authors.
Andrew SpauldingDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Amrita SharmaDepartment of Molecular and Cellular Biology, Kennesaw State University, Science Building MailDrop1201, 370 Paulding Avenue, Kennesaw, Georgia 30144, United States.
Miriam A GiardiniCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-6510-2409
Benjamin HoffmanDepartment of Molecular and Cellular Biology, Kennesaw State University, Science Building MailDrop1201, 370 Paulding Avenue, Kennesaw, Georgia 30144, United States.
Jean A BernatchezCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-8309-1627
Laura-Isobel McCallCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Claudia M CalvetCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Jasmin AckermannCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Julia M SouzaCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Diane ThomasCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Caroline C MillardDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
William G DevineDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.
Baljinder SinghDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0003-2828-5768
Everton M SilvaCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.ORCID 0000-0003-3993-4954
Susan E LeedExperimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.
Norma E RoncalExperimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.
Erica C PennExperimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.
Jessey ErathDepartment of Microbiology, New York University School of Medicine, 430 E. 29th Street, New York, New York 10010, United States.
Gaurav KumarDepartment of Molecular and Cellular Biology, Kennesaw State University, Science Building MailDrop1201, 370 Paulding Avenue, Kennesaw, Georgia 30144, United States.
Yadira SepulvedaCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Arnold GarciaCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Ana RodriguezDepartment of Microbiology, New York University School of Medicine, 430 E. 29th Street, New York, New York 10010, United States.
Nelly El-SakkaryCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Richard J SciottiExperimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.ORCID 0000-0002-3069-3122
Robert F CampbellExperimental Therapeutics, Walter Reed Army Institute of Research, 503 Robert Grant Avenue, Silver Spring, Maryland 20910, United States.
Jeremiah D MomperCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
James H McKerrowCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-5152-4627
Conor R CaffreyCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Jair L Siqueira-NetoCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, California 92093, United States.
Michael P PollastriDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0001-9943-7197
Kojo Mensa-WilmotDepartment of Molecular and Cellular Biology, Kennesaw State University, Science Building MailDrop1201, 370 Paulding Avenue, Kennesaw, Georgia 30144, United States.
Lori FerrinsDepartment of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0001-8992-0919
Funding
Optimization and Modes of Action of NEU-4438, a New Anti-trypanosome Lead DrugR01AI124046 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI, MENSA-WILMOT, KOJO A. · 2016 to 2025
$6.0MRepurposing human kinase inhibitor chemotypes for Neglected Tropical DiseasesR01AI114685 · NIAID · NORTHEASTERN UNIVERSITY · PI FERRINS, LORI · 2015 to 2025
$4.6MTargeting the Genus Leishmania with Small MoleculesR01AI151639 · NIAID · BOSTON UNIVERSITY (CHARLES RIVER CAMPUS) · PI BROWN, LAUREN ELAINE, SCHAUS, SCOTT EDWARD · 2021 to 2025
$3.8MCuraxin-137, A New Lead for Anti-Trypanosome Drug Discovery - Resubmission - 1R01AI126311 · NIAID · UNIVERSITY OF GEORGIA · PI HAJDUK, STEPHEN L, POLLASTRI, MICHAEL P · 2017 to 2020
$2.7MValidation and development of trypanosomal phosphodiesterase inhibitors for treatR01AI082577 · NIAID · NORTHEASTERN UNIVERSITY · PI CAMPBELL, ROBERT KIRWAN, POLLASTRI, MICHAEL P · 2009 to 2013
$2.6MUC San Diego RAPID Faculty Development Program in Infectious DiseasesR25AI147376 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI ADRIANA H TREMOULET, Joann Trejo · 2020 to 2026
$2.5MLead Optimization of Lapatinib Analogs for Human African TrypanosomiasisR56AI099476 · NIAID · UNIVERSITY OF GEORGIA · PI MENSA-WILMOT, KOJO A., POLLASTRI, MICHAEL P · 2014 to 2014
$672kLead optimization of agents targeting multiple kinetoplastid parasitesR21AI127594 · NIAID · NORTHEASTERN UNIVERSITY · PI POLLASTRI, MICHAEL P · 2017 to 2018
$427kDefining the death transcriptome of Schistosoma mansoni to construct a molecular drug screenR21AI126296 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAFFREY, CONOR · 2017 to 2018
$415kNIAID NIH HHS HHSN272201700014CNIAID NIH HHS R01 AI082577NIAID NIH HHS R01 AI114685NIAID NIH HHS R01 AI124046NIAID NIH HHS R01 AI126311NIAID NIH HHS R01 AI151639NIAID NIH HHS R21 AI126296NIAID NIH HHS R21 AI127594NIAID NIH HHS R25 AI147376NIAID NIH HHS R56 AI099476
Abstract
Neglected tropical diseases such as Chagas disease, human African trypanosomiasis, leishmaniasis, and schistosomiasis have a significant global health impact in predominantly developing countries, although these diseases are spreading due to increased international travel and population migration. Drug repurposing with a focus on increasing antiparasitic potency and drug-like properties is a cost-effective and efficient route to the development of new therapies. Here we identify compounds that have potent activity against
Indexed as
Antiparasitic AgentsChagas DiseaseLeishmania donovaniTrypanosoma cruziAnimalsDisease Models, AnimalFemaleHumansLeishmaniasis, VisceralMiceParasitic Sensitivity TestsStructure-Activity RelationshipAntiparasitic AgentsChagas diseasedrug repurposinghuman African trypanosomiasisleishmaniasisneglected tropical diseasesschistosomiasis
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LicenceCC BY-NC-ND
Read underepoch 390
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.