Synthesis, In-Silico Potential Enzymatic Target Predictions, Pharmacokinetics, Toxicity, Anti-Microbial and Anti-Inflammatory Studies of Bis-(2- methylindolyl) Methane Derivatives

Title:Synthesis, In-Silico Potential Enzymatic Target Predictions, Pharmacokinetics, Toxicity, Anti-Microbial and Anti-Inflammatory Studies of Bis-(2- methylindolyl) Methane Derivatives

Volume: 17 Issue: 2

Author(s): Dnyaneshwar T. Nagre, Suraj N. Mali, Bapu R. Thorat*, Swapnali A. Thorat, Atul R. Chopade, Mazhar Farooqui and Brijmohan Agrawal

Affiliation:

• Department of Chemistry, P.G. and Research Centre, Government of Maharashtra’s Ismail Yusuf College, Jogeshwari, Mumbai,India

Keywords: Bis(indolyl)methanes, homogeneous catalysts, heterogeneous catalysts, biological activities, indole-3- carbaldehydes, in silico ADMET.

Abstract:

Background: The bis(indolyl)methanes (BIMs) scaffold is reported for wide varieties of pharmacological profiles, including antibacterial, anti-proliferative, anticancer, cytotoxic, insecticidal, analgesic, antioxidant, and anti-inflammatory agents.

Materials and Methods: A series of bis(indolyl)methanes have been synthesized by a greener and newer approach using the reaction of different substituted aldehydes and indole in the presence of an easily available and biodegradable base such as piperidine in acetic acid at room temperature and characterized with ultraviolet–visible spectrophotometry (UV–Vis or UV/Vis), Fourier-transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy (NMR), etc. The antibacterial and antifungal activities were also carried out against Staphylococcus aureus (RCMB 000106) and Bacillis subtilis (RCMB 000107), as two Gram-positive bacterial strains, and Salmonella typhi and Escherichia coli (RCMB 000103), as two Gram-negative bacterial strains. Fungal species such as Candida Albicans, Penicillium chrysogenum, Aspergillus niger were also used for in vitro antifungal evaluation. All our newly synthesized 14 compounds (4a-4n) were subjected for anti-inflammatory activity in vitro and compared with the known standard drug aceclofenac.

Results: Our newly synthesized compounds showed good to moderate antibacterial agents, in silico ADMET, and anti-inflammatory profiles.

Conclusion: We hope that our current study would aid future developments of bis(indolyl)methanes as antibacterial and anti-inflammatory agents.

Cite this article as:

Nagre T. Dnyaneshwar, Mali N. Suraj , Thorat R. Bapu *, Thorat A. Swapnali , Chopade R. Atul , Farooqui Mazhar and Agrawal Brijmohan , Synthesis, In-Silico Potential Enzymatic Target Predictions, Pharmacokinetics, Toxicity, Anti-Microbial and Anti-Inflammatory Studies of Bis-(2- methylindolyl) Methane Derivatives, Current Enzyme Inhibition 2021; 17 (2) . https://dx.doi.org/10.2174/1573408017666210203203735

DOI https://dx.doi.org/10.2174/1573408017666210203203735	Print ISSN 1573-4080
Publisher Name Bentham Science Publisher	Online ISSN 1875-6662