Back to Search
Start Over
Novel pyrazole-clubbed thiophene derivatives via Gewald synthesis as antibacterial and anti-inflammatory agents.
- Source :
-
Archiv der Pharmazie [Arch Pharm (Weinheim)] 2020 Dec; Vol. 353 (12), pp. e2000103. Date of Electronic Publication: 2020 Sep 07. - Publication Year :
- 2020
-
Abstract
- The aim of this study was to synthesize newer potent Schiff bases by condensing 2-amino-5-(2,4-dichlorophenyl)thiophene-3-carbonitrile and 1,3-disubstituted-1H-pyrazole-4-carbaldehydes, and to investigate their biological activity. The compounds were synthesized via Gewald synthesis and characterized by spectral data and elemental analyses. They were screened for their in vitro antibacterial and anti-inflammatory activities. The synthesized compounds were also evaluated for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Compounds 8b, 8c, 8f, 8g, 8k, 8n, and 8o showed promising antibacterial activity. The interactions between the substituted pyrazoles and bovine protein showed promising anti-inflammatory activity. The experimental results revealed compound 8a as a promising antitubercular agent. Hemolytic assays confirmed that the compounds are nontoxic, with percentage hemolysis ranging from 3.6 to 20.1, at a concentration of 1 mg/ml. The results suggest that the pyrazole ring and the substitution pattern on the heterocyclic moiety have an effect on the bioactivity.<br /> (© 2020 Deutsche Pharmazeutische Gesellschaft.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents toxicity
Anti-Inflammatory Agents chemical synthesis
Anti-Inflammatory Agents toxicity
Antitubercular Agents chemical synthesis
Antitubercular Agents pharmacology
Antitubercular Agents toxicity
Bacteria growth & development
Drug Design
Hemolysis drug effects
Humans
Molecular Structure
Mycobacterium tuberculosis drug effects
Mycobacterium tuberculosis growth & development
Pyrazoles chemical synthesis
Pyrazoles toxicity
Schiff Bases
Structure-Activity Relationship
Thiophenes chemical synthesis
Thiophenes toxicity
Anti-Bacterial Agents pharmacology
Anti-Inflammatory Agents pharmacology
Bacteria drug effects
Pyrazoles pharmacology
Thiophenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1521-4184
- Volume :
- 353
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Archiv der Pharmazie
- Publication Type :
- Academic Journal
- Accession number :
- 32893908
- Full Text :
- https://doi.org/10.1002/ardp.202000103