scholarly journals Synthesis of substituted pyridine based sulphonamides as an antidiabetic agent

2021 ◽  
Vol 12 (3) ◽  
pp. 279-283
Author(s):  
Gautam Sadawarte ◽  
Samadhan Jagatap ◽  
Mukesh Patil ◽  
Vasant Jagrut ◽  
Jamatsing Darbarsing Rajput
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Research Work ◽  
Synthetic Methods ◽  
Alpha Amylase ◽  
Spectroscopic Techniques ◽  
Inhibition Activity ◽  
Antidiabetic Agent ◽  
Biological Functions ◽  
Ir Spectroscopic

This research work describes the synthesis of a new series of heterocyclic compounds, namely sulfonamide derivatives. Sulfonamides are a diverse class of organic compounds having significant and potent biological activities. Diverse synthetic methods have been engaged to build up its various derivatives for different biological functions. In this study, the production of novel pyridine-based heterocyclic compounds having sulfonamide moieties has been elaborated. The obtained sulfonamide-based pyridine scaffold was used to investigate their alpha-amylase inhibition activity. The structures of freshly prepared compounds were described using 1H NMR, 13C NMR, and IR spectroscopic techniques. The molecular docking of sulfonamides performed against porcine pancreatic alpha-amylase using PDB file 1LP was used for generation of grid. All the new synthesized compounds were shown notable anti-diabetic activity.

scholarly journals Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

2021 ◽  
Vol 2 (01) ◽  
pp. 19-27
Author(s):  
Rhambus Rawat ◽  
Prem Shankar Deo ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Heterocyclic Compounds ◽  
Environmental Science ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

Synthetic Methods and Pharmacological Potential of Different Oxazine Analogs

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Organic Chemistry ◽  
Drug Resistance ◽  
Sodium Hydroxide ◽  
Crucial Role ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Wide Range ◽  
Different Types ◽  
Pharmacological Potential

: Oxazine analog is a vital class of heterocyclic compounds and has attracted synthetic interest owing to their wide range of biological activities. Oxazine analogs are valuable in medicinal organic chemistry and exhibited different varieties of biological activities such as antimicrobial, anticancer, antimalarial, antitubercular, sedative, anticonvulsant, analgesic, anti-inflammatory, antipyretic, etc. Oxazine can be derived from benzene by appropriate substitution of carbon atoms of the ring by nitrogen and oxygen atoms. Nowadays, the development of drug resistance is a key problem, and to defeat this problem, it is crucial to synthesize novel compounds. So novel oxazine analogs may play a crucial role to overcome these problems. Oxazine analogs are prepared by reaction of chalcone derivatives with thiourea in the presence of alcohol and sodium hydroxide. The present aims of this review to give an outline of some different synthetic methods and different types of biological activities of oxazine analogs. We hope that this review will be motivating for researchers concerned with oxazine analogs.

Pyrazole Carboxylic Acid and Derivatives: Synthesis and Biological Applications

2020 ◽  
Vol 17 ◽  
Author(s):  
Adnan Cetin
Keyword(s):  
Organic Chemistry ◽  
Biological Activity ◽  
Carboxylic Acid ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Building Blocks ◽  
Literature Survey ◽  
Synthetic Methods ◽  
Biological Applications

: The heterocyclic compounds are the building blocks for synthesis of the different biological active compounds in the organic chemistry. Heterocyclic compounds have versatile synthetic applicability and biological activity. Pyrazole carboxylic acid derivatives are significant scaffold structures in heterocyclic compounds due to biologic activities such as antimicrobial, anticancer, inflammatory, antidepressant, antifungal anti-tubercular and antiviral etc. The aim of this mini-review is an overview synthesis of pyrazole carboxylic acid derivatives and their biologic applications. The summarized literature survey presents in detail biological activities of pyrazole carboxylic acid derivatives and their various synthetic methods. This mini-review can be guide to many scientists in medicinal chemistry.

scholarly journals Biological Aspects of Emerging Benzothiazoles: A Short Review

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Ruhi Ali ◽  
Nadeem Siddiqui
Keyword(s):  
Heterocyclic Compounds ◽  
Scientific Literature ◽  
Biological Activities ◽  
Research Work ◽  
Short Review ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Biological Aspects

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole is a privileged bicyclic ring system with multiple applications. It is known to exhibit a wide range of biological properties including anticancer, antimicrobial, and antidiabetic, anticonvulsant, anti-inflammatory, antiviral, antitubercular activities. A large number of therapeutic agents are synthesized with the help of benzothiazole nucleus. During recent years there have been some interesting developments in the biological activities of benzothiazole derivatives. These compounds have special significance in the field of medicinal chemistry due to their remarkable pharmacological potentialities. This review is mainly an attempt to present the research work reported in the recent scientific literature on different biological activities of benzothiazole compounds.

Recent Advancement of Synthesis of Isatins as a Versatile Pharmacophore: A review

Drug Research ◽  
2020 ◽  
Author(s):  
Gajendra Kumar ◽  
Netra Pal Singh ◽  
Kaushal Kumar
Keyword(s):  
Analgesic Activity ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Antitubercular Activity ◽  
Synthetic Methods ◽  
Active Compounds ◽  
Recent Advancement ◽  
Anti Inflammatory ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds

AbstractIsatin (1 H-indole-2, 3-Dione) and its derivatives are versatile compounds which acts as a precursor for a large number of pharmacologically active compounds. Therefore isatins have a significant importance in the synthesis of different heterocyclic compounds. Isatins show variety of biological activities. In this review we focus on synthetic methods of isatins and their biological activities such as antimicrobial, anticonvulsant, anti-inflammatory and analgesic activity, antitubercular activity.

scholarly journals Synthesis and Chemical Properties of 3-Phosphono-coumarins and 1,2-Benzoxaphosphorins as Precursors for Bioactive Compounds

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2030 ◽  
Author(s):  
Ana I. Koleva ◽  
Nevena I. Petkova-Yankova ◽  
Rositca D. Nikolova
Keyword(s):  
Bioactive Compounds ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Properties ◽  
Conjugate Addition ◽  
Synthetic Methods ◽  
Addition Reactions ◽  
Important Class ◽  
Pharmacological Interest ◽  
And Chemical Properties

Coumarins are an important class of natural heterocyclic compounds that have attracted considerable synthetic and pharmacological interest due to their various biological activities. This review emphasizes on the synthetic methods for the preparation of dialkyl 2-oxo-2H-1-benzo- pyran-3-phosphonates and alkyl 1,2-benzoxaphosphorin-3-carboxylates. Their chemical properties as acceptors in conjugate addition reactions, [2+2] and [3+2] cycloaddition reactions are discussed.

Utility of Certain 2-Furanone Derivatives for Synthesis of Different Heterocyclic Compounds and Testing their Anti-cancer Activity

2021 ◽  
Vol 17 ◽  
Author(s):  
Rania Helmy Abd El-Hameed ◽  
Hend Medhat El-Shanbaky ◽  
Mosaad Sayed Mohamed
Keyword(s):  
Cell Lines ◽  
Heterocyclic Compounds ◽  
Development Process ◽  
Biological Activities ◽  
Biologically Active ◽  
Cytotoxic Agents ◽  
Inhibition Activity ◽  
Small Cell Lung ◽  
Anti Cancer ◽  
Hct 116

Background: 2-Furanones attracted great attention due to their biological activities. They also have the ability to convert to several biologically active heterocyclic and non-heterocyclic compounds, especially as anti-cancer agents. Objectives: This research aims to assist in the development process of novel cytotoxic agents through synthesizing certain 2-furanone derivatives, using them as starting materials for the preparation of novel heterocyclic and non-heterocyclic compounds, and then testing the synthesized derivatives for their anti-cancer activities. Methods: All the newly synthesized compounds were fully characterized by elemental analysis, IR, Mass, and 1H-NMR spectroscopy. 18 synthesized compounds were selected by National Cancer Institute (NCI) for testing against 60 cell lines, and the active compound was tested as MAPK14 and VEGFR2-inhibitor using Staurosporine as standard. Results: Compound 3a showed higher activity against several cell lines, including leukemia (SR), Non-Small Cell Lung Cancer (NCI-H460), colon cancer (HCT-116), ovarian cancer (OVCAR-4), renal cancer (786-0, ACHN and UO-31), and finally breast cancer (T-47D). It also had better inhibition activity against MAPK14 than the used reference. Conclusion: Compound 3a has promising anti-cancer activities compared to the used standards and may need further modifications and investigations.

scholarly journals Antioxidant and Antidiabetic Activities of Biologically Synthesized Silver Nanoparticles using Linumusitatissimum Extract

2021 ◽  
Vol 37 (5) ◽  
pp. Kanmani-R
Author(s):  
Kanmani R ◽  
IrudayaIrin Scleeva P
Keyword(s):  
Silver Nanoparticles ◽  
Research Work ◽  
Radical Scavenging ◽  
Xrd Analysis ◽  
Spectroscopic Studies ◽  
Uv Spectra ◽  
Alpha Amylase ◽  
Ir Spectroscopic ◽  
Flaxseed Extract

This research work was mainly focused to study the anti-oxidant and anti-diabetic activities of biologically synthesis of silver nanoparticles (AgNPs) from the flaxseed extract of Linumusitassimum. Qualitative tests identify the presence of phytochemicals in the flaxseed extract and its results showed the presence of tannins, terpenoids, saponins, flavonoids, steroids, cardiac glycosides, anthraquinones, coumarins, xanthoproteins, alkaloids, emodins, and carbohydrate in it. Preliminarily AgNPs formation is confirmed by the UV spectra and it showed maximum adsorption band at 438nm. FT-IR spectroscopic studies reveal the Phyto-constituents which are involved in the reduction of silver (Ag+1) into silver nanoparticles (Ag0). The spherical shapes of AgNPs are observed with crystalline nature are found in the aid of SEM and XRD analysis. Synthesized AgNPs have the maximum percentage of a silver element which is examined by the EDX analysis. The in-vitro antioxidant and antidiabetic activities of L. usitatissimummediated AgNPs were analyzed by using the DPPH, alpha-amylase, and alpha glycosides assays respectively. The DPPH result shows that the AgNPs possess 59.01% of radical scavenging property and the standard ascorbic acid reveals 48.63% at 100µg/ml concentration. Similarly in anti-diabetic activity, AgNPs shows the maximum inhibition of 79.84% in the alpha-amylase assay, and for alpha-glucosidase, AgNPs showed 58.86% at 100µg/ml concentration.

Recent Progress in the Synthesis of Pyrroles

2020 ◽  
Vol 24 (6) ◽  
pp. 622-657
Author(s):  
Duc Dau Xuan
Keyword(s):  
Biological Activity ◽  
Organic Semiconductors ◽  
Broad Spectrum ◽  
Heterocyclic Compounds ◽  
Recent Progress ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Synthetic Methods ◽  
Pyrrole Derivatives ◽  
Wide Range

: Pyrrole derivatives are nitrogen-containing heterocyclic compounds and widely distributed in a large number of natural and non-natural compounds. These compounds possess a broad spectrum of biological activities such as anti-infammatory, antiviral, antitumor, antifungal, and antibacterial activities. Besides their biological activity, pyrrole derivatives have also been applied in various areas such as dyes, conducting polymers, organic semiconductors. : Due to such a wide range of applicability, access to this class of compounds has attracted intensive research interest. Various established synthetic methods such as Paal-Knorr, Huisgen, and Hantzsch have been modified and improved. In addition, numerous novel methods for pyrrole synthesis have been discovered. This review will focus on considerable studies on the synthesis of pyrroles, which date back from 2014.

Sulfonamides and Sulphonyl Ester of Quinolines as Non-Acidic, Non- Steroidal, Anti-inflammatory Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Bilquees Bano ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
Spectroscopic Techniques ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Hydroxy Quinoline ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background:: Quinolines are important class of heterocyclic compounds possessing wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study. Objective:: In the current study 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their antiinflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood. Methods:: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinoline with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential. Results and Discussion:: Among the synthetic derivatives 1-50, six compounds showed good to moderate anti-inflammatory activity. Compounds 47 (IC50 = 2.9 ± 0.5 μg/mL), 36 (IC50 = 3.2 ± 0.2 μg/mL), and 24 (IC50 = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 μg/mL). Compounds 20 (IC50 = 25.5 ± 0.7 μg/mL), 50 (IC50 = 42.9 ± 5.6 μg/mL), and 8 (IC50 = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive. Conclusion:: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may leads to the discovery of new and potential anti-inflammatory agents.

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