Affiliation:
1. SAĞLIK BİLİMLERİ ÜNİVERSİTESİ
2. BIRUNI UNIVERSITY
Abstract
Increasing antibiotic resistance is an important problem for public health therefore new antimicrobial compounds are needed. In this study, the antimicrobial effects of 3-Substituted Indole-2-one and -thione derivatives were investigated. Antimicrobial effects of previously synthesized 18 different 3-substituted indole-2-one and 2-thione derivatives against 5 different microorganisms were investigated and the structure-activity relationships and drug-like properties of compounds were analyzed by molecular docking and in silico prediction studies. The in vitro antimicrobial activities of compounds were tested by microdilution method. The most active compounds were found as 2, 3, 4, 5, 6, 7, 8 at 125 μg/mL of MIC value. Compounds 2 and 3 were found to be active against S. enterica and compounds 4, 5, 6, 7, and 8 were found to be active against methicillin-resistant S. aureus. According to molecular docking studies, all compounds presented weaker binding properties than ciprofloxacin, ampicillin and gentamicin. The predicted values for molecular weight, log P, PSA, crossing the BBB, GI absorption properties and type of CYPP450 inhibition data of compounds were found promising for drug-like properties. 3-Substituted Indole-2-one and -thione derivatives can proivide an important contribution to develop alternative antimicrobial agents.
Publisher
EMU Journal of Pharmaceutical Sciences
Reference27 articles.
1. Banerjee D, Yogeeswari P, Bhat P, Thomas A, Srividya M, Sriram D (2011). Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection. Eur J Med Chem 46(1): 106-121.
2. Bhaskar G, Arun Y, Balachandran C, Saikumar C, Perumal PT (2012). Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity. Eur J Med Chem 51: 79-91.
3. Chodvadiya VD, Pambhar KD, Parmar ND, Dhamsaniya AP, Chhatbar PV, Ram HN, Patel PK (2019). Synthesis and characterization of N-methyl indole derivatives via desulfitative displacement by various amines and Its antimicrobial activity. World Sci. News 120(2): 181-191.
4. Clinical and Laboratory Standards Institute (2018). Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that GrowAerobically, Approved Standard. seventh ed. Wayne: CLSI.
5. Doganay D, Ozcan MS, Senturk MA, Olgen S (2022). Antimicrobial Evaluation, Molecular Docking and ADME Properties of Indole Amide Derivatives. Lett Drug Des Discov 19(5): 387-396.