scholarly journals Synthesis and Antibacterial Activity of Novel 3-Hydroxy Benzoic Acid Hybrid Derivative [Part I]

2018 ◽  
pp. 369-374
Author(s):  
Maruti S. Satpute ◽  
Vijay D. Gangan ◽  
Indu Shastri
Keyword(s):  
Antibacterial Activity ◽  
Benzoic Acid ◽  
Direct Action ◽  
Biological Properties ◽  
Chemotherapeutic Agents ◽  
Organic Chemical ◽  
Cell Disease ◽  
Drug Candidates ◽  
Derivatives Of ◽  
Hybrid Derivative

3-hydroxy benzoic acid is an organic chemical which can be obtained naturally as well as synthetically. The literature survey reveals its various biological properties viz. antimicrobial, antialgal, antimutagenic, antiestrogenic, hypoglycemic, anti-inflammatory, anti-platelet aggregating, nematicidal, antiviral, antioxidant etc. It is also reported to be used as preservative in many drugs, cosmetic products, pharmaceuticals, food and beverages. Some derivatives of 3-hydroxybenzoic acid are found to possess direct action on Hbs molecules, inhibit acetic acid induced oedema and used in management of sickle cell disease. It is also has wide applications in perfumery industries. In this paper, novel ester / hybrid derivative of 3- Hydroxy benzoic acid was synthesized and tested for its potential antibacterial activity. This combinatorial synthesis of novel 3-Hydroxy benzoic ester / hybrid derivative can be a useful approach to generate potent chemotherapeutic agents in developing new drug candidates.

scholarly journals Synthesis and Antibacterial Activity of Novel Vanillic Acid Hybrid Derivatives [Part II]

2018 ◽  
pp. 219-223 ◽  
Author(s):  
Maruti S. Satpute ◽  
Vijay D. Gangan ◽  
Indu Shastri
Keyword(s):  
Antibacterial Activity ◽  
Vanillic Acid ◽  
Chemotherapeutic Agents ◽  
Active Pharmaceutical Ingredients ◽  
Dihydroxybenzoic Acid ◽  
Drug Candidates ◽  
Pharmaceutical Ingredients ◽  
Derivatives Of ◽  
Flavoring Agent ◽  
Methoxybenzoic Acid

Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a dihydroxybenzoic acid derivative used as a flavoring agent. It is used in the synthesis of various active pharmaceutical ingredients such as Etamivan, Modecainide, Brovanexine, Vanitiolide, Vanyldisulfamide etc. In this paper, novel ester / hybrid derivatives of vanillic acid were synthesized and tested for potential antibacterial activity. This combinatorial synthesis of novel vanillic ester / hybrid derivatives can be a useful approach to generate potent chemotherapeutic agents in developing new drug candidates.

scholarly journals Methyl Vanillate Ether Derivatives as Future Potential Drug

2019 ◽  
pp. 129-134
Author(s):  
Maruti S. Satpute ◽  
Vijay D. Gangan ◽  
Indu Shastri
Keyword(s):  
Vanillic Acid ◽  
Chemotherapeutic Agents ◽  
Combinatorial Synthesis ◽  
Active Pharmaceutical Ingredients ◽  
Dihydroxybenzoic Acid ◽  
Drug Candidates ◽  
Pharmaceutical Ingredients ◽  
Future Potential ◽  
Derivatives Of ◽  
Methoxybenzoic Acid

Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a dihydroxybenzoic acid derivative used as a flavouring agent. It is used in the synthesis of various active pharmaceutical ingredients such as Etamivan, Modecainide, Brovanexine, Vanitiolide, Vanyldisulfamide etc. In this paper, novel ether derivatives of vanillic acid were synthesized and tested for potential antibacterial activity. This combinatorial synthesis of novel vanillic acid ether derivatives can be a useful approach to generate potent chemotherapeutic agents in developing new drug candidates.

Preparation of esterified derivatives of α-lactalbumin and investigation of their antibacterial activity

2014 ◽  
Vol 1 (1) ◽  
Author(s):  
Negar Ghorbani ◽  
Abdol-Khalegh Bordbar ◽  
Asghar Taheri-Kafrani ◽  
Akbar Vaseghi
Keyword(s):  
Antibacterial Activity ◽  
Derivatives Of

Synthesis and Evaluation of Aromatic Surfactants as Potential Antibacterial and Cytotoxic Agents

2019 ◽  
Vol 16 (6) ◽  
pp. 478-484
Author(s):  
Kenia Barrantes ◽  
Mary Fuentes ◽  
Luz Chacón ◽  
Rosario Achí ◽  
Jorge Granados-Zuñiga ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Hela Cells ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Hydroxybenzoic Acid ◽  
Derivatives Of

Two ether and one ester derivatives of the 4-nitro-3-hydroxybenzoic acid were synthesized and characterized. The in vitro antimicrobial and cytotoxic activities of the three novel compounds were also evaluated. The aromatic derivatives showed antibacterial activity against one of the four microorganisms tested and two compounds (C8 and NOBA) had a lower IC50 in HeLa cells.

The Effect of N-4 Substituent on Antibacterial Activity of Novel Hydroxymethyl/Aminomethyl Derivatives of 1,2,4-Triazole-3-thione

2012 ◽  
Vol 9 (6) ◽  
pp. 633-637 ◽  
Author(s):  
Tomasz Plech ◽  
Monika Wujec ◽  
Urszula Kosikowska ◽  
Anna Malm ◽  
Magdalena Barylka ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Aminomethyl Derivatives ◽  
Derivatives Of

Recent Advances in 1,3,5-Triazine Derivatives as Antibacterial Agents

2020 ◽  
Vol 17 (8) ◽  
pp. 991-1041
Author(s):  
Divya Utreja ◽  
Jagdish Kaur ◽  
Komalpreet Kaur ◽  
Palak Jain
Keyword(s):  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Antibacterial Agents ◽  
Rapid Development ◽  
Pharmacological Action ◽  
Biological Properties ◽  
Vast Array ◽  
Bacterial Diseases ◽  
New Class ◽  
Triazine Derivatives

Triazine, one of the nitrogen containing heterocyclic compounds has attracted the considerable interest of researchers due to the vast array of biological properties such as anti-viral, antitumor, anti-convulsant, analgesic, antioxidant, anti-depressant, herbicidal, insecticidal, fungicidal, antibacterial and anti-inflammatory activities offered by it. Various antibacterial agents have been synthesized by researchers to curb bacterial diseases but due to rapid development in drug resistance, tolerance and side effects, there had always been a need for the synthesis of a new class of antibacterial agents that would exhibit improved pharmacological action. Therefore, this review mainly focuses on the various methods for the synthesis of triazine derivatives and their antibacterial activity.

Structure-Activity Relationship and Antimicrobial Evaluation of N-Phenylpyrazole Curcumin Derivatives

2020 ◽  
Vol 16 (4) ◽  
pp. 481-488
Author(s):  
Heli Sanghvi ◽  
Satyendra Mishra
Keyword(s):  
Antibacterial Activity ◽  
Gram Negative Bacteria ◽  
Pyrazole Derivatives ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Curcumin Derivatives ◽  
Structure Activity ◽  
Electron Donating Groups ◽  
Derivatives Of

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.

scholarly journals Multidisciplinary Studies of Folk Medicine “Five Thieves’ Oil” (Olejek Pięciu Złodziei) Components

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2931
Author(s):  
Przemysław Siejak ◽  
Wojciech Smułek ◽  
Farahnaz Fathordobady ◽  
Anna Grygier ◽  
Hanna Maria Baranowska ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Membrane Permeability ◽  
Significant Contribution ◽  
Spectroscopic Analysis ◽  
Folk Medicine ◽  
Cell Activity ◽  
Biological Properties ◽  
Cell Membrane Permeability ◽  
Comparable Activity ◽  
Terpene Derivatives

To meet the growing interest in natural antibacterial agents, we evaluated the physicochemical and biological properties of the folk medicine known as “five thieves’ oil” (Polish name: olejek pięciu złodziei). Five thieves’ oil consists of a mixture of five oils: rosemary, lemon, clove, eucalyptus, and cinnamon. In this study, we performed gas chromatography, FTIR, and UV–vis spectroscopic analysis, as well as L-a-b color tests, contact angle determination, and surface tension determination. To verify its antibacterial activity, the metabolic activity and changes in cell membrane permeability of bacteria of the genus Pseudomonas were studied. As a result, it was found that among the constituent oils, the oils of clove and cinnamon were the least volatile and, at the same time, had the strongest antibacterial activity. However, a mix of all the oils also showed comparable activity, which was even more pronounced for the oils after 4 weeks of aging. This effect can be linked to the high content of terpene derivatives such as eugenol and cinnamaldehyde, which can cause changes in bacterial membrane permeability, affecting cell activity and survival. This study is the first to characterize the constituents of the popular folk medicine five thieves’ oil, confirming and explaining its strong antibacterial activity, thus constituting a significant contribution to contemporary health education.

scholarly journals Identification of Anti-Severe Acute Respiratory Syndrome-Related Coronavirus 2 (SARS-CoV-2) Oxysterol Derivatives In Vitro

2021 ◽  
Vol 22 (6) ◽  
pp. 3163
Author(s):  
Hirofumi Ohashi ◽  
Feng Wang ◽  
Frank Stappenbeck ◽  
Kana Tsuchimoto ◽  
Chisa Kobayashi ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Viral Replication ◽  
Cultured Cells ◽  
Peak Plasma ◽  
Plasma Concentrations ◽  
Membrane Vesicles ◽  
Drug Candidates ◽  
Increased Risk ◽  
Derivatives Of

The development of effective antiviral drugs targeting the severe acute respiratory syndrome-related coronavirus 2 (SARS-CoV-2) is urgently needed to combat the coronavirus disease 2019 (COVID-19). We have previously studied the use of semi-synthetic derivatives of oxysterols, oxidized derivatives of cholesterol as drug candidates for the inhibition of cancer, fibrosis, and bone regeneration. In this study, we screened a panel of naturally occurring and semi-synthetic oxysterols for anti-SARS-CoV-2 activity using a cell culture infection assay. We show that the natural oxysterols, 7-ketocholesterol, 22(R)-hydroxycholesterol, 24(S)-hydroxycholesterol, and 27-hydroxycholesterol, substantially inhibited SARS-CoV-2 propagation in cultured cells. Among semi-synthetic oxysterols, Oxy210 and Oxy232 displayed more robust anti-SARS-CoV-2 activities, reducing viral replication more than 90% at 10 μM and 99% at 15 μM, respectively. When orally administered in mice, peak plasma concentrations of Oxy210 fell into a therapeutically relevant range (19 μM), based on the dose-dependent curve for antiviral activity in our cell-based assay. Mechanistic studies suggest that Oxy210 reduced replication of SARS-CoV-2 by disrupting the formation of double-membrane vesicles (DMVs); intracellular membrane compartments associated with viral replication. Our study warrants further evaluation of Oxy210 and Oxy232 as a safe and reliable oral medication, which could help protect vulnerable populations with increased risk of developing COVID-19.

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