Synthesis and evaluation of 1,2,3-dithiazole inhibitors of the nucleocapsid protein of feline immunodeficiency virus (FIV) as a model for HIV infection.

Animals Antiviral Agents / chemistry Cats HIV Infections / drug therapy Immunodeficiency Virus, Feline Nucleocapsid Proteins / metabolism Structure-Activity Relationship
1,2,3-Dithiazoles Feline Immunodeficiency Virus (FIV) Human Immunodeficiency Virus (HIV) Nucleocapsid protein Zinc ejection

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
15 08 2022
Historique:
received: 29 04 2022
revised: 13 05 2022
accepted: 13 05 2022
pubmed: 3 6 2022
medline: 29 6 2022
entrez: 2 6 2022
Statut: ppublish

Résumé

We disclose a series of potent anti-viral 1,2,3-dithiazoles, accessed through a succinct synthetic approach from 4,5-dichloro-1,2,3-dithiazolium chloride (Appel's salt). A series of small libraries of compounds were screened against feline immunodeficiency virus (FIV) infected cells as a model for HIV. This approach highlighted new structure activity relationship understanding and led to the development of sub-micro molar anti-viral compounds with reduced toxicity. In addition, insight into the mechanistic progress of this system is provided via advanced QM-MM modelling. The 1,2,3-dithiazole represents a versatile scaffold with potential for further development to treat both FIV and HIV.

Identifiants

DOI: 10.1016/j.bmc.2022.116834 PMID: 35653871
pubmed: 35653871
pii: S0968-0896(22)00226-7
doi: 10.1016/j.bmc.2022.116834
pii:
doi:

Substances chimiques

Antiviral Agents 0
Nucleocapsid Proteins 0

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

116834

Commentaires et corrections

Type : ErratumIn

Informations de copyright

Copyright © 2022 The Author(s). Published by Elsevier Ltd.. All rights reserved.

Auteurs

Tuomo Laitinen (T)

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211 Kuopio, Finland.

Theres Meili (T)

Clinical Laboratory, Department of Clinical Diagnostics and Services, and Center for Clinical Studies, Vetsuisse Faculty, University of Zurich, Zurich 8057, Switzerland.

Maria Koyioni (M)

Department of Chemistry, University of Cyprus, P.O. Box 20537, 1678 Nicosia, Cyprus.

Panayiotis A Koutentis (PA)

Department of Chemistry, University of Cyprus, P.O. Box 20537, 1678 Nicosia, Cyprus.

Antti Poso (A)

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211 Kuopio, Finland; Department of Internal Medicine VIII, University Hospital Tübingen, Otfried-Müller-Strasse 14, 72076 Tübingen, Germany.

Regina Hofmann-Lehmann (R)

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211 Kuopio, Finland.

Christopher R M Asquith (CRM)

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, 70211 Kuopio, Finland; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, NC 27599, USA. Electronic address: christopher.asquith@uef.fi.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiviraux › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Feliformia › Felidae › Felis › Chats › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Maladies du système immunitaire › Déficits immunitaires › Infections à VIH › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Virus › Virus à ARN › Retroviridae › Lentivirus › Lentivirus félins › Virus de l'immunodéficience féline › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines virales › Protéines virales structurales › Protéines nucléocapside › Synthesis and evaluation of 1,2,3-dithiazole...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis and evaluation of 1,2,3-dithiazole...