Back to Search
Start Over
Antitubercular Bis-Substituted Cyclam Derivatives: Structure-Activity Relationships and in Vivo Studies.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2018 Apr 26; Vol. 61 (8), pp. 3595-3608. Date of Electronic Publication: 2018 Apr 05. - Publication Year :
- 2018
-
Abstract
- We recently reported the discovery of nontoxic cyclam-derived compounds that are active against drug-resistant Mycobacterium tuberculosis. In this paper we report exploration of the structure-activity relationship for this class of compounds, identifying several simpler compounds with comparable activity. The most promising compound identified, possessing significantly improved water solubility, displayed high levels of bacterial clearance in an in vivo zebrafish embryo model, suggesting this compound series has promise for in vivo treatment of tuberculosis.
- Subjects :
- Animals
Antitubercular Agents chemical synthesis
Antitubercular Agents chemistry
Aza Compounds chemical synthesis
Aza Compounds chemistry
Bacterial Load drug effects
Coordination Complexes chemical synthesis
Coordination Complexes chemistry
Coordination Complexes pharmacology
Drug Resistance, Bacterial
Heterocyclic Compounds, 1-Ring chemical synthesis
Heterocyclic Compounds, 1-Ring chemistry
Macrocyclic Compounds chemical synthesis
Macrocyclic Compounds chemistry
Metals, Heavy chemistry
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium marinum drug effects
Solubility
Structure-Activity Relationship
Tuberculosis drug therapy
Zebrafish
Antitubercular Agents pharmacology
Aza Compounds pharmacology
Heterocyclic Compounds, 1-Ring pharmacology
Macrocyclic Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 61
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29558124
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.7b01569