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.

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 A Review of the Pharmacological Characteristics of Vanillic Acid

2021 ◽  
Vol 11 (2-S) ◽  
pp. 200-204
Author(s):  
Ashwini Ingole ◽  
Megha P Kadam ◽  
Aishwarya P. Dalu ◽  
Shital M Kute ◽  
Piyusha R Mange ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Vanillic Acid ◽  
The Other ◽  
Pharmacological Properties ◽  
Dihydroxybenzoic Acid ◽  
Acid Analog ◽  
Effective Antioxidant ◽  
Pharmacological Potential ◽  
Flavoring Agent ◽  
Methoxybenzoic Acid

A dihydroxybenzoic acid analog used as a flavoring agent is vanillic acid (4hydroxy-3-methoxybenzoic acid). It's a form of vanillin that has been oxidized. It's also a step in the process of making vanillin from Ferulic Acid. Vanillic acid has seen a lot of press because of its many uses in the cosmetics, fruit, flavorings, cigarettes,alcohols, drinks, and polymer sectors. It's said to have effective antioxidant, anti-inflammatory, and neuroprotective properties. The pharmacological impact on oxidative stress-induced neuro-degeneration, on the other hand, have not been thoroughly examined. The pharmacological properties of vanillic Acid lead to its possible use in the treatment of various diseases. Keywords: Vanillic acid, Pharmacological Potential, wound healing, Antioxidants

scholarly journals The Lisbon Supramolecular Green Story: Mechanochemistry towards New Forms of Pharmaceuticals

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2705
Author(s):  
João Luís Ferreira da Silva ◽  
M. Fátima Minas da Piedade ◽  
Vânia André ◽  
Sofia Domingos ◽  
Inês C. B. Martins ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Physicochemical Properties ◽  
Mechanochemical Synthesis ◽  
Crystal Engineering ◽  
Short Review ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Polymorphic Forms ◽  
Derivatives Of

This short review presents and highlights the work performed by the Lisbon Group on the mechanochemical synthesis of active pharmaceutical ingredients (APIs) multicomponent compounds. Here, we show some of our most relevant contributions on the synthesis of supramolecular derivatives of well-known commercial used drugs and the corresponding improvement on their physicochemical properties. The study reflects, not only our pursuit of using crystal engineering principles for the search of supramolecular entities, but also our aim to correlate them with the desired properties. The work also covers our results on polymorphic screening and describes our proposed alternatives to induce and maintain specific polymorphic forms, and our approach to avoid polymorphism using APIs as ionic liquids. We want to stress that all the work was performed using mechanochemistry, a green advantageous synthetic technique.

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.

Reversed-Phase High Performance Liquid Chromatographic Analysis of Three First Line Anti-Tuberculosis Drugs

2019 ◽  
Vol 69 (12) ◽  
pp. 3590-3592
Author(s):  
Nela Bibire ◽  
Romeo Iulian Olariu ◽  
Luminita Agoroaei ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Fluids ◽  
Gradient Elution ◽  
High Performance Liquid Chromatographic ◽  
Reversed Phase ◽  
Assay Method ◽  
Active Pharmaceutical Ingredients ◽  
First Line ◽  
Pharmaceutical Ingredients ◽  
Liquid Chromatographic

Active pharmaceutical ingredients such as isoniazid, pyrazinamide and rifampicin are among the most important first-line anti-tuberculosis drugs. A simple, rapid and sensitive reversed phase-high performance liquid chromatographic assay method for the simultaneous determination of isoniazid, pyrazinamide and rifampicin has been developed. Separation of the interest compounds was achieved in a 10 min chromatographic run in gradient elution mode on a Zorbax SB-C18 stainless steel column (150 � 4 mm, 5 mm) using a guard column containing the same stationary phase. The gradient elution was carried out with a mobile phase of 10% CH3CN aqueous solution for channel A and 50% CH3CN in pH = 6.8 phosphate buffer (20 mM), to which 1.5 mL triethylamine were added for channel B. Quantification of the analyzed substances was carried out spectrophotometrically at 269 nm. Detection limits of 0.48 mg/L for isoniazid, 0.52 mg/L for pyrazinamide and 0.48 mg/L for rifampicin were established for the developed assay method. The present work showed that the proposed analysis method was advantageous for simple and rapid analysis of the active pharmaceutical ingredients in pharmaceuticals and biological fluids.

scholarly journals Numaswitch: an efficient high-titer expression platform to produce peptides and small proteins

AMB Express ◽  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Bach-Ngan Nguyen ◽  
Florian Tieves ◽  
Thomas Rohr ◽  
Hilke Wobst ◽  
Felix S. Schöpf ◽  
...  
Keyword(s):  
Fermentation Broth ◽  
High Titer ◽  
New Technology ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Expression Platform ◽  
Small Proteins ◽  
Production Platform ◽  
Β Amyloid ◽  
Cost Efficient

AbstractThe production of peptides as active pharmaceutical ingredients (APIs) by recombinant technologies is of emerging interest. A reliable production platform, however, is still missing due the inherent characteristics of peptides such as proteolytic sensitivity, aggregation and cytotoxicity. We have developed a new technology named Numaswitch solving present limitations. Numaswitch was successfully employed for the production of diverse peptides and small proteins varying in length, physicochemical and functional characteristics, including Teriparatide, Linaclotide, human β-amyloid and Serum amyloid A3. Additionally, the potential of Numaswitch for a cost-efficient commercial production is demonstrated yielding > 2 g Teriparatide per liter fermentation broth in a quality meeting API standard.

scholarly journals Diagnosis of Agglomeration and Crystallinity of Active Pharmaceutical Ingredients in Over the Counter Headache Medication by Electrospray Laser Desorption Ionization Mass Spectrometry Imaging

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 610
Author(s):  
Mariann Inga Van Meter ◽  
Salah M. Khan ◽  
Brynne V. Taulbee-Cotton ◽  
Nathan H. Dimmitt ◽  
Nathan D. Hubbard ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Mass Spectrometry Imaging ◽  
Laser Desorption ◽  
Ionization Mass Spectrometry ◽  
Ionization Mass ◽  
Active Pharmaceutical Ingredients ◽  
Laser Desorption Ionization ◽  
Over The Counter ◽  
Pharmaceutical Ingredients ◽  
Desorption Ionization

Agglomeration of active pharmaceutical ingredients (API) in tablets can lead to decreased bioavailability in some enabling formulations. In a previous study, we determined that crystalline APIs can be detected as agglomeration in tablets formulated with amorphous acetaminophen tablets. Multiple method advancements are presented to better resolve agglomeration caused by crystallinity in standard tablets. In this study, we also evaluate three “budget” over-the-counter headache medications (subsequently labeled as brands A, B, and C) for agglomeration of the three APIs in the formulation: Acetaminophen, aspirin, and caffeine. Electrospray laser desorption ionization mass spectrometry imaging (ELDI-MSI) was used to diagnose agglomeration in the tablets by creating molecular images and observing the spatial distributions of the APIs. Brand A had virtually no agglomeration or clustering of the active ingredients. Brand B had extensive clustering of aspirin and caffeine, but acetaminophen was observed in near equal abundance across the tablet. Brand C also had extensive clustering of aspirin and caffeine, and minor clustering of acetaminophen. These results show that agglomeration with active ingredients in over-the-counter tablets can be simultaneously detected using ELDI-MS imaging.

scholarly journals Sulfanyl Porphyrazines with Morpholinylethyl Periphery—Synthesis, Electrochemistry, and Photocatalytic Studies after Deposition on Titanium(IV) Oxide P25 Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2280
Author(s):  
Tomasz Koczorowski ◽  
Wojciech Szczolko ◽  
Anna Teubert ◽  
Tomasz Goslinski
Keyword(s):  
Diclofenac Sodium ◽  
2D Nmr ◽  
Oxide Nanoparticles ◽  
Electrochemical Studies ◽  
Macrocyclic Compounds ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Vis Spectroscopy ◽  
Singlet Oxygen Quencher ◽  
Nmr Techniques

The syntheses, spectral UV–Vis, NMR, and electrochemical as well as photocatalytic properties of novel magnesium(II) and zinc(II) symmetrical sulfanyl porphyrazines with 2-(morpholin-4-yl)ethylsulfanyl peripheral substituents are presented. Both porphyrazine derivatives were synthesized in cyclotetramerization reactions and subsequently embedded on the surface of commercially available P25 titanium(IV) oxide nanoparticles. The obtained macrocyclic compounds were broadly characterized by ESI MS spectrometry, 1D and 2D NMR techniques, UV–Vis spectroscopy, and subjected to electrochemical studies. Both hybrid materials, consisting of porphyrazine derivatives embedded on the titanium(IV) oxide nanoparticles’ surface, were characterized in terms of particle size and distribution. Next, they were subjected to photocatalytic studies with 1,3-diphenylisobenzofuran, a known singlet oxygen quencher. The applicability of the obtained hybrid material consisting of titanium(IV) oxide P25 nanoparticles and magnesium(II) porphyrazine derivative was assessed in photocatalytic studies with selected active pharmaceutical ingredients, such as diclofenac sodium salt and ibuprofen.

US trade policy is putting at risk the sustainability of the generic/biosimilar industry and the drug supply chain

2021 ◽  
pp. 174113432199431
Author(s):  
María Fabiana Jorge
Keyword(s):  
Supply Chain ◽  
Trade Policy ◽  
Pharmaceutical Products ◽  
Drug Supply ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Us Trade Policy ◽  
Drug Supply Chain ◽  
Security Concern ◽  
The U.S

With the outbreak of the Coronavirus there is a new realization of the vulnerabilities of the U.S. drug supply chain. However, while such concerns may have been amplified by the pandemic, they preceded Covid-19 and were well documented before 2020. Indeed, in past years the U.S. Congress held several hearings addressing potential vulnerabilities in the U.S. drug supply chain, in part due to the increasing dependency on China as a dominant supplier of active pharmaceutical ingredients (APIs) and some finished pharmaceutical products. These vulnerabilities go well beyond health policy and constitute a national security concern. The article addresses how U.S. trade policy plays a significant role in shaping the pharmaceutical industry at home and abroad and is in part responsible for some of the current vulnerabilities of the U.S. drug supply chain.

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