Syntheses of Analogues of Propofol: A Review

Synthesis ◽  
2020 ◽  
Vol 52 (24) ◽  
pp. 3693-3713 ◽  
Author(s):  
Ivaylo V. Dimitrov ◽  
Elina E. K. Suonio
Keyword(s):  
Antioxidant Activity ◽  
Soybean Oil ◽  
Mechanism Of Action ◽  
Critically Ill Patients ◽  
Lipid Emulsion ◽  
Water Solubility ◽  
Rapid Onset ◽  
Clinical Use ◽  
Structure Activity ◽  
Hypnotic Agent

AbstractPropofol (2,6-diisopropylphenol) is an intravenous sedative/hypnotic agent that is used extensively for introduction and maintenance of general anaesthesia, sedation of critically ill patients and procedural sedation (e.g., endoscopy). Propofol has a rapid onset and offset of action and shows only minimal accumulation upon prolonged use. Propofol is only sparingly soluble in water and is currently marketed in 10% soybean oil-based lipid emulsion. Propofol’s anaesthetic properties were discovered over forty years ago, and it has been in clinical use for over thirty years. The main use of propofol remains as an anaesthetic but, over the years, analogues have been developed with varying properties from anticancer, anticonvulsant and antioxidant. In addition, large synthetic efforts have been made towards improving propofol’s water-solubility, its activity, and elucidating its structure–activity­ relationship and exact mechanism of action have been made. This review provides an overview of the research pertaining to propofol-like molecules and covers the efforts of synthetic chemists towards propofol analogues over the last 40 years.1 Introduction2 History3 Early Work4 Improving Water Solubility5 The Importance of the Phenol6 Exploring the Structure–Activity Relationship and Attempts to Improve Activity7 Anticancer Activity8 Anticonvulsant Properties9 Antioxidant Activity10 Photoactive Labelling to Elucidate Mechanism of Action11 Photoregulation12 Conclusion

scholarly journals An Overview of Bioactive Alkaloid, Semi-Synthetic Analogs, Mechanism of Action and Structure-Activity Relationship of Piperine as Antioxidant

2021 ◽  
Vol 33 (9) ◽  
pp. 2244-2250
Author(s):  
Sagar Joshi ◽  
Salahuddin ◽  
Rajnish Kumar ◽  
Divya Sharma
Keyword(s):  
Antioxidant Activity ◽  
Mechanism Of Action ◽  
Structure Activity Relationship ◽  
Black Pepper ◽  
Activity Relationship ◽  
Pharmacological Activities ◽  
Structure Activity ◽  
Natural Alkaloid ◽  
Relationship Of ◽  
Derivatives Of

Piperine, a natural alkaloid obtained from black pepper exhibit a variety of pharmacological activities like antioxidant activity and in this article, the mechanism of the antioxidant, structure-activity relationship of piperine as an antioxidant and various schemes of derivatives of piperine as antioxidants were discussed.

scholarly journals Design and Antiproliferative and Antioxidant Activities of Furan-Based Thiosemicarbazides and 1,2,4-Triazoles: Their Structure-Activity Relationship and SwissADME Predictions

2021 ◽  
Author(s):  
Yusuf SICAK
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Antioxidant Activities ◽  
Cancer Cell Line ◽  
Clinical Use ◽  
Biological Applications ◽  
Triazole Derivatives ◽  
Structure Activity ◽  
Pharmacokinetic Properties ◽  
Drug Similarity

Abstract Due to the limited number of drugs in current clinical use, the diverse biological applications of furan have encouraged the preparation of a wide variety of thiosemicarbazide and triazole derivatives for the purpose of developing new drug agents. In this study aimed to investigate the antiproliferative and antioxidant activities of some thiosemicarbazides (1-12) and 1,2,4-triazoles (13-24). Compound 15 (IC50: 8.81±0.28 µM) showed the highest antiproliferative activity against the cervical (HeLa) cancer cell line among the compounds. Compounds 15, 20, 21, and 22 of the 1,2,4-triazole derivatives (13-24) exhibited excellent antioxidant activity. Moreover, the physicochemical properties, pharmacokinetic properties, drug similarity, and medicinal chemistry properties of all synthesized products were calculated using SwissADME. In addition, the effect of the structure–activity relationships of the 1,2,4-triazole derivatives (13-24) on the results of antiproliferative and antioxidant activity assays was evaluated.

Phenolic Imidazole Derivatives with Dual Antioxidant/Antifungal Activity: Synthesis and Structure-Activity Relationship

2019 ◽  
Vol 15 (4) ◽  
pp. 341-351 ◽  
Author(s):  
Ana P. Bettencourt ◽  
Marián Castro ◽  
João P. Silva ◽  
Francisco Fernandes ◽  
Olga P. Coutinho ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antifungal Activity ◽  
Organic Molecules ◽  
Inhibitory Concentration ◽  
Yeast Species ◽  
Dpph Radical ◽  
Dpph Assay ◽  
Gram Negative ◽  
Structure Activity ◽  
Deoxyribose Degradation

Background: Previous publications show that the addition of a phenolic antioxidant to an antifungal agent, considerably enhances the antifungal activity. Objective: Synthesis of novel compounds combining phenolic units with linear or cyclic nitrogencontaining organic molecules with antioxidant/antifungal activity using methodologies previously developed in the group. Methods: Several N- [1,2-dicyano-2- (arylidenamino) vinyl]-O-alkylformamidoximes 3 were synthesized and cyclized to 4,5-dicyano-N- (N´-alcoxyformimidoyl)-2-arylimidazoles 4 upon reflux in DMF, in the presence of manganese dioxide or to 6-cyano-8-arylpurines 5 when the reagent was refluxed in acetonitrile with an excess of triethylamine. These compounds were tested for their antioxidant activity by cyclic voltammetry, DPPH radical (DPPH•) assay and deoxyribose degradation assay. The minimum inhibitory concentration (MIC) of all compounds was evaluated against two yeast species, Saccharomyces cerevisiae and Candida albicans, and against bacteria Bacillus subtilis (Gram-positive) and Escherichia coli (Gram negative). Their cytotoxicity was evaluated in fibroblasts. Results: Among the synthetised compounds, five presented higher antioxidant activity than reference antioxidant Trolox and from these compounds, four presented antifungal activity without toxic effects in fibroblasts and bacteria. Conclusion: Four novel compounds presented dual antioxidant/antifungal activity at concentrations that are not toxic to bacteria and fibroblasts. The active molecules can be used as an inspiration for further studies in this area.

scholarly journals Impact of Propofol Sedation upon Caloric Overfeeding and Protein Inadequacy in Critically Ill Patients Receiving Nutrition Support

Pharmacy ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 121
Author(s):  
Roland N. Dickerson ◽  
Christopher T. Buckley
Keyword(s):  
Intensive Care Unit ◽  
Intensive Care ◽  
Enteral Nutrition ◽  
Parenteral Nutrition ◽  
Critically Ill Patients ◽  
Protein Intake ◽  
Lipid Emulsion ◽  
Caloric Intake ◽  
Nutrition Therapy ◽  
Nutrition Support

Propofol, a commonly used sedative in the intensive care unit, is formulated in a 10% lipid emulsion that contributes 1.1 kcals per mL. As a result, propofol can significantly contribute to caloric intake and can potentially result in complications of overfeeding for patients who receive concurrent enteral or parenteral nutrition therapy. In order to avoid potential overfeeding, some clinicians have empirically decreased the infusion rate of the nutrition therapy, which also may have detrimental effects since protein intake may be inadequate. The purpose of this review is to examine the current literature regarding these issues and provide some practical suggestions on how to restrict caloric intake to avoid overfeeding and simultaneously enhance protein intake for patients who receive either parenteral or enteral nutrition for those patients receiving concurrent propofol therapy.

Application of Cis-Diamminedichloro-Platinum in Combination Antineoplastic Therapy of Testicular Cancer

1978 ◽  
Vol 12 (4) ◽  
pp. 226-229 ◽  
Author(s):  
Janice M. Williams ◽  
Nicholas G. Popovich
Keyword(s):  
Adverse Effects ◽  
Testicular Cancer ◽  
Antineoplastic Therapy ◽  
Mechanism Of Action ◽  
Combination Chemotherapy ◽  
Clinical Use ◽  
Adult Males ◽  
Testicular Carcinoma ◽  
Dosage Administration

Testicular carcinoma is a leading cause of cancer-related deaths in adult males between the ages of 20 and 35. Cis-Diamminedichloroplatinum (II) (i.e., CDDP) is currently being used investigatively in combination chemotherapy for the treatment of this disease. This article reviews the literature to date on CDDP and its application in testicular cancer. Individual CDDP parameters (e.g., chemistry, mechanism of action, effectiveness and clinical use, adverse effects, dosage, administration and distribution) are discussed.

scholarly journals Antioxidant activity of Spathodea campanulata (Bignoneaceae) extracts

2012 ◽  
Vol 14 (2) ◽  
pp. 287-292 ◽  
Author(s):  
S.C Heim ◽  
F.A Guarnier ◽  
D.T Ferreira ◽  
R Braz-Filho ◽  
R Cecchini ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Complex Formation ◽  
Mechanism Of Action ◽  
Iron Complex ◽  
Bark Extract ◽  
Flower Extract ◽  
Antioxidant Mechanism ◽  
Activity Loss ◽  
Ethanol Extracts ◽  
Antioxidant Mechanisms

Spathodea campanulata is used in traditional medicine in Africa as diuretic and anti-inflammatory. Although few studies have reported the mechanism of antioxidant action, this study evidenced the antioxidant activity of S. campanulata bark and flower extracts and their possible mechanism of action. Ethanol extracts of S. campanulata bark and flowers showed antioxidant activity on lipid peroxidation of liver microsome induced by Fe3+-ascorbic acid. Bark extract was 5 times more efficient than flower extract. The antioxidant activity of flower extract, previously complexed with increasing concentrations of Fe3+ (20 - 100 μM) which resulted in antioxidant activity loss, was shown to be related to iron complex formation. In contrast, the antioxidant activity of bark extract was not inhibited by the previous incubation with Fe3+, although complexation was demonstrated by spectral analysis of the solution. These results suggest an antioxidant mechanism other than Fe3+ complex formation. Therefore, the antioxidant mechanisms of S. campanulata flower and bark extracts are distinct from each other, reflecting the extract heterogeneous composition and the mechanism of action.

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