Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite

Animals Anopheles / drug effects Antimalarials / chemical synthesis Female Germ Cells / drug effects High-Throughput Screening Assays Humans Male Mice Microsomes, Liver / metabolism Molecular Structure Parasitic Sensitivity Tests Plasmodium falciparum / drug effects Rats Spiro Compounds / chemical synthesis Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
25 02 2021
Historique:
pubmed: 13 2 2021
medline: 5 5 2021
entrez: 12 2 2021
Statut: ppublish

Résumé

A novel diazaspiro[3.4]octane series was identified from a

Identifiants

DOI: 10.1021/acs.jmedchem.1c00034 PMID: 33573376
pubmed: 33573376
doi: 10.1021/acs.jmedchem.1c00034
doi:

Substances chimiques

Antimalarials 0
Spiro Compounds 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S.

Langues

eng

Sous-ensembles de citation

IM

Pagination

2291-2309

Auteurs

Claire Le Manach (C)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Jean Dam (J)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

John G Woodland (JG)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Gurminder Kaur (G)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Lutete P Khonde (LP)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Christel Brunschwig (C)

Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Mathew Njoroge (M)

Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
ORCID: 0000-0003-1276-2224

Kathryn J Wicht (KJ)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.

André Horatscheck (A)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Tanya Paquet (T)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Grant A Boyle (GA)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Liezl Gibhard (L)

Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Dale Taylor (D)

Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Nina Lawrence (N)

Drug Discovery and Development Center (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.

Tomas Yeo (T)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.

Sachel Mok (S)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
ORCID: 0000-0002-9605-0154

Richard T Eastman (RT)

Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.
ORCID: 0000-0003-3580-380X

Dorjbal Dorjsuren (D)

Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.

Daniel C Talley (DC)

Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.

Hui Guo (H)

Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.

Anton Simeonov (A)

Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States.

Janette Reader (J)

Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.

Mariëtte van der Watt (M)

Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.

Erica Erlank (E)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Nelius Venter (N)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Jacek W Zawada (JW)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Ayesha Aswat (A)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Luisa Nardini (L)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Theresa L Coetzer (TL)

Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.

Sonja B Lauterbach (SB)

Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.

Belinda C Bezuidenhout (BC)

Wits Research Institute for Malaria, School of Pathology, Department of Molecular Medicine and Haematology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.

Anjo Theron (A)

Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa.

Dalu Mancama (D)

Biosciences, Council for Scientific and Industrial Research, P.O. Box 395, Pretoria 0001, South Africa.

Lizette L Koekemoer (LL)

Wits Research Institute for Malaria, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.
Centre for Emerging Zoonotic and Parasitic Diseases, National Institute for Communicable Diseases of the National Health Laboratory Service, Johannesburg 2192, South Africa.

Lyn-Marie Birkholtz (LM)

Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.

Sergio Wittlin (S)

Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
University of Basel, 4003 Basel, Switzerland.

Michael Delves (M)

Imperial College London, South Kensington, London SW7 2AZ, U.K.
London School of Hygiene and Tropical Medicine, London WC1E 7HT, U.K.

Sabine Ottilie (S)

Division of Host-Microbe Systems & Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093-076, United States.
ORCID: 0000-0001-9797-2612

Elizabeth A Winzeler (EA)

Division of Host-Microbe Systems & Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093-076, United States.

Thomas W von Geldern (TW)

Embedded Consulting, P.O. Box 726, Richmond, Illinois 60071, United States.

Dennis Smith (D)

4 The Maltings, Walmer CT14 7AR, U.K.

David A Fidock (DA)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, New York 10032, United States.

Leslie J Street (LJ)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.

Gregory S Basarab (GS)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
ORCID: 0000-0001-5684-6046

James Duffy (J)

Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland.

Kelly Chibale (K)

Drug Discovery and Development Center (H3D), University of Cape Town, Rondebosch 7701, South Africa.
South African Medical Research Council, Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
ORCID: 0000-0002-1327-4727

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female

Evaluation of Low-Value Services Across Major Medicare Advantage Insurers and Traditional Medicare.

Ciara Duggan, Adam L Beckman, Ishani Ganguli et al.
1.00
Humans United States Aged Cross-Sectional Studies Medicare Part C

Effectiveness of Virtual Yoga for Chronic Low Back Pain: A Randomized Clinical Trial.

Hallie Tankha, Devyn Gaskins, Amanda Shallcross et al.
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Identification and Profiling of a Novel...
questionsmedicales.fr › Eucaryotes › Animaux › Invertébrés › Arthropodes › Insectes › Pterygota › Neoptera › Holometabola › Diptera › Nematocera › Culicomorpha › Culicidae › Anopheles › Identification and Profiling of a Novel...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › Antipaludiques › Identification and Profiling of a Novel...
questionsmedicales.fr › Cellules › Cellules germinales › Identification and Profiling of a Novel...
questionsmedicales.fr › Techniques d'investigation › Tests de criblage à haut débit › Identification and Profiling of a Novel...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Identification and Profiling of a Novel...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Identification and Profiling of a Novel...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Identification and Profiling of a Novel...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Identification and Profiling of a Novel...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité parasitaire › Identification and Profiling of a Novel...
questionsmedicales.fr › Eucaryotes › Alveolata › Apicomplexa › Haemosporida › Plasmodium › Plasmodium falciparum › Identification and Profiling of a Novel...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Identification and Profiling of a Novel...
questionsmedicales.fr › Composés polycycliques › Spiranes › Identification and Profiling of a Novel...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Identification and Profiling of a Novel...