Medium-Ring Keto Bislactams with Antischistosomal Activity.

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:
08 Oct 2024
Historique:
medline: 8 10 2024
pubmed: 8 10 2024
entrez: 8 10 2024
Statut: aheadofprint

Résumé

We discovered medium-ring keto bislactams as a new antischistosomal chemotype. The ketone functional group and isoindolinone substructure were required for high antischistosomal activity. Aryl substitution with EWG functional groups decreased the chemical stability. These compounds were relatively polar with the measured LogD

Identifiants

DOI: 10.1021/acs.jmedchem.4c01532 PMID: 39377659
pubmed: 39377659
doi: 10.1021/acs.jmedchem.4c01532
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Auteurs

Rongguo Ren (R)

College of Pharmacy, University of Nebraska Medical Center, Nebraska Medical Center, Omaha, Nebraska 986125, United States.

Derek A Leas (DA)

College of Pharmacy, University of Nebraska Medical Center, Nebraska Medical Center, Omaha, Nebraska 986125, United States.

Cécile Häberli (C)

Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, Basel CH-4002, Switzerland.
University of Basel, Basel CH-4003, Switzerland.

Monica Cal (M)

Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, Basel CH-4002, Switzerland.
University of Basel, Basel CH-4003, Switzerland.

Gong Chen (G)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.

Kasiram Katneni (K)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.

Yuxiang Dong (Y)

College of Pharmacy, University of Nebraska Medical Center, Nebraska Medical Center, Omaha, Nebraska 986125, United States.
ORCID: 0000-0003-1412-3178

Marcel Kaiser (M)

Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, Basel CH-4002, Switzerland.
University of Basel, Basel CH-4003, Switzerland.

Jennifer Keiser (J)

Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, Basel CH-4002, Switzerland.
University of Basel, Basel CH-4003, Switzerland.

Susan A Charman (SA)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
ORCID: 0000-0003-1753-8213

Jonathan L Vennerstrom (JL)

College of Pharmacy, University of Nebraska Medical Center, Nebraska Medical Center, Omaha, Nebraska 986125, United States.
ORCID: 0000-0003-0075-2336

Classifications MeSH