Synthesis of lignan conjugates via cyclopropanation: Antimicrobial and antioxidant studies.
Ethyl 2-(4-methoxyphenyl)-3-(thiophene-2-carbonyl)cyclopropanecarboxylates 2(a-f) and ethyl 4-aryl-7-oxo-4,5,6,7-tetrahydrobenzo[b]thiophene-5-carboxylates 4(a-f) were synthesized by simple procedure. The synthesized new compounds were screened in vitro for their antimicrobial and antioxidant activities. The compounds 2b and 4f showed excellent antibacterial activity; while 2b and 4f showed remarkable antifungal properties. The results of antioxidant activity studies revealed that compounds 4b and 4f manifested profound antioxidant potential. The docking studies were done for the final compounds. The ADME result indicates that all these molecules possess pharmaceutical properties in the range of 95% of drugs.
Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore, India.
Kanchipura Ramachandrappa
KR
Raghavendra
Department of Chemistry, Yuvaraja College, University of Mysore, India.
Nagamallu
N
Renuka
Central Research Laboratory, Adichunchanagiri Institute of Medical Sciences, B.G. Nagara, India.
Vivek H
VH
Kameshwar
Center for the Study of Systems Biology, School of Biology, Georgia Institute of Technology, Atlanta, GA 30332, USA.
Bharath
B
Srinivasan
Department of Chemistry, Yuvaraja College, University of Mysore, India. Electronic address: ajaykumar@ycm.uni-mysore.ac.in.
Kariyappa
K
Ajay Kumar
Department of Studies in Chemistry, University of Mysore, Manasagangothri, Mysore, India. Electronic address: padduammu2016@gmail.com.
Sheena
S
Shashikanth
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D003521:Cyclopropanes / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects; D017705:Lignans / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000975:Antioxidants; D003521:Cyclopropanes; D017705:Lignans
Antimicrobial; Antioxidant; Lignans; MIC; Molecular docking