Back to Search
Start Over
Therapeutic effects of isothiocyanate prodrugs on rheumatoid arthritis
- Source :
- Bioorganic & Medicinal Chemistry Letters. 28:737-741
- Publication Year :
- 2018
- Publisher :
- Elsevier BV, 2018.
-
Abstract
- Isothiocyanates 7a and 7b have poor stability and aqueous solubility. To address these problems, prodrugs 8a and 8b were synthesized. Prodrugs 8a and 8b were stable in HEPES buffer at pH 4.4, but released the active compounds 7a and 7b in HEPES buffer at pH 7.4 and in mouse plasma, respectively. Compound 8a and especially compound 8b showed anti-inflammatory effects. Compound 8b demonstrated significant efficacy in animal models of traumatic inflammation, acute inflammation and rheumatoid arthritis. Compound 8b also did not cause appreciable toxicity in mice after 5 weeks at a daily dose of 200 mg/kg.
- Subjects :
- 0301 basic medicine
Neutrophils
Clinical Biochemistry
Pharmaceutical Science
Inflammation
Pharmacology
Biochemistry
Arthritis, Rheumatoid
Rats, Sprague-Dawley
Hepes buffer
Mice
03 medical and health sciences
chemistry.chemical_compound
Isothiocyanates
Drug Discovery
Aqueous solubility
medicine
Animals
Prodrugs
Rats, Wistar
Molecular Biology
Zebrafish
Anti-Inflammatory Agents, Non-Steroidal
Body Weight
Organic Chemistry
Therapeutic effect
Prodrug
medicine.disease
030104 developmental biology
chemistry
Rheumatoid arthritis
Isothiocyanate
Toxicity
Molecular Medicine
medicine.symptom
Half-Life
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 28
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....4e7b70e396cdbcace40824738a323e51