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The anti‐inflammatory Design, Synthesis and Exploiting Pharmacological Activities of 2,3‐Dihydrofuranocoumarins as Multi‐Therapeutic Agents
Author(s) -
Madar Jyoti M.,
Shastri Lokesh A.,
Shastri Samundeeswari L.,
Holiyachi Megharaja,
Naik Nirmala S.,
Shaikh Farzanabi,
Kumbar Vijay M.,
Bhat Kishor G.,
Joshi Shrinivas D.,
Sungar Vinay A.
Publication year - 2018
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201802196
Subject(s) - antimicrobial , chemistry , anti inflammatory , cytotoxicity , docking (animal) , coumarin , in vitro , pyridinium , biochemistry , combinatorial chemistry , stereochemistry , pharmacology , biology , medicine , nursing , organic chemistry , medicinal chemistry
Abstract Our recent research interest regarding synthesis of bioactive furanocoumarin derivatives, we have developed pyridinium yield assisted synthesis of 2,3‐dihydrofuran coumarin derivatives via, multicomponent one step reaction with excellent yield. All compounds 4(a–p) and 6(a–b) were screened for their in vitro antimicrobial, Anti‐inflammatory and cytotoxicity activity. The activity results demonstrated that, synthesized compounds are selective against both Gram positive bacterial strains B.subtilis , S.aureus and inactive against Gram negative bacterial strains E.coli, P.aeruginosa . Similarly, compounds are highly potent against both fungal strains C.albicans and C.tropicalis over standard drugs Fuconazole. The anti‐inflammatory activity was examined using egg albumin protein denaturation and Human red blood cell membrane stabilization methods; in both methods anti‐inflammatory results are highly promising. Compounds 4 a , 4 b , 4 d and 4 o exhibited potential cytotoxic activity against lung cancer cell lines with IC 50 value ranging from 0.29 to 0.35 μM. Identifying the active antimicrobial and anti‐inflammatory agent is as essential factor for the successful development of lead molecules in drug designing. Molecular docking study was performed for all the compounds and docking result reveals that compounds are possessing drug like property.