http://www.chtf.stuba.sk/~szolcsanyi/education/files/Chemia%20heterocyklickych%20zlucenin/Prednaska%203/Doplnkove%20studijne%20materialy/Recent%20developments%20and%20biological%20activities%20of%20thiazolidinone%20derivatives%20-%20A%20review.pdf

Recent developments and biological activities of thiazolidinone derivatives: A review

Mannich bases in medicinal chemistry and drug design.

Biological and medicinal significance of benzofuran

Resistance to antibiotics is a major global problem and there is an urgent need to develop new therapeutic agents. Although many classes of active compounds have been established as efficient derivatives in diverse fields of antimicrobial therapy, they have not yet found wide application against a few deadly microbes. In recent years, compounds have been developed that have solved some of the problems posed; for example improved bioavailability is one of the targets achieved with most of the more recent compounds, allowing for once-daily dosing. Benzofuran and its derivatives are found to be suitable structures, existing widely in natural products and unnatural compounds with a wide range of biological and pharmacological applications; thus, considerable attention has been focused on the discovery of new drugs in the fields of drug invention and development. Some benzofuran derivatives, such as psoralen, 8-methoxypsoralen and angelicin have been used in the treatment of skin diseases such as cancer or psoriasis. The unique structural features of benzofuran and its wide array of biological activities make it a privileged structure in the field of drug discovery, especially in the search for efficient antimicrobial candidates. Recently, this scaffold has emerged as a pharmacophore of choice for designing antimicrobial agents that are active toward different clinically approved targets. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we collated the published reports on this versatile core to provide a deeper insight, so that its full therapeutic potential can be utilized for the treatment of microbial diseases. This study systematically provides a comprehensive report on current developments in benzofuran-based compounds as antimicrobial agents and is also helpful for the researchers working on a substitution pattern around the nucleus, with an aim to help medicinal chemists to develop structure activity relationships (SAR) on these derivatives as antimicrobial drugs.

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Benzofuran: an emerging scaffold for antimicrobial agents

A review on antioxidant potential of bioactive heterocycle benzofuran: Natural and synthetic derivatives

Previously unknown biphenyl containing 5-phenyl-1-benzofuran-2-yl derivatives; methanones (2a–i), tertiary alcohols (3a–l), and carbinols (4a–f) were synthesized and evaluated for their antimicrobial and antioxidant activities to study the effect of functionalization at the carbonyl carbon and substitution at biphenyl ring on these activities. The introduction of hydroxyl group at carbonyl carbon enhanced the antioxidant property (3a, 3g, 3h, 4a, and 4b), while antimicrobial activity decreased; the carbinol and tertiary alcohols corresponding to methanone 2a and 2b showed no antimicrobial activity. Biphenyl methanones 1, 2a, 2f, and 2g exhibited antimicrobial activity with minimal inhibitory concentration ranging between 0.001 and 0.500 mg/mL, tertiary alcohols 3a, 3g, and 3h and carbinols 4a and 4b exhibited the promising antioxidant property. The mode of action of these active compounds was carried out by docking of receptor GlcN6P synthase with newly synthesized candidate ligands 1, 2a, 2e, 2f, 2g, 2h, 3a, 3g, 3h, 4c, and 4d.

5-phenyl-1-benzofuran-2-yl derivatives: synthesis, antimicrobial, and antioxidant activity

A series of β-amino carbonyl compounds containing coumarin (4a–h) and benzofuran (6a–i) moieties was synthesized by a three component Mannich reaction of 3-acetyl-2H-chromen-2-one (1) or 1-(1-benzofuran-2-yl) ethanone (5) with p-substituted aromatic aldehydes (2a–g) and aromatic amines (3a–b) in the presence of cerric ammonium nitrate as a catalyst. The newly synthesized compounds were screened for antimicrobial and antioxidant activities. Compounds 4b, 4e, 4f, 6f, 6g, and 6i showed microbial inhibition with minimal inhibition concentration ranging between 0.040 and 0.500 mg/mL, compounds 4b, 4c, 6c, 6e, and 6i showed promising free radical scavenging activity and compounds 4b, 4f, 6c, 6d, and 6h showed good chelating ability with Fe2+ ions. The synthesized compounds were studied for docking on the enzyme, glucosamine-6-phosphate synthase to predict the binding affinity and orientation at the active site of the receptor.

Synthesis of β-amino carbonyl derivatives of coumarin and benzofuran and evaluation of their biological activity

Treatment of 5-bromo-2-acetyl benzofuran with hydrazine followed by condensation of the resulting hydrazone with different quinoline derivatives gave the corresponding Schiff bases. Reaction of these Schiff bases with thioacetic acid furnished the target thiazolidinone molecule. Some of the newly synthesized compounds show promising analgesic and antimicrobial activity. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.

A Facile Synthesis of Bromo-Substituted Benzofuran Containing Thiazolidinone Nucleus Bridged with Quinoline Derivatives: Potent Analgesic and Antimicrobial Agents

Synthesis of Some Mannich Bases and Novel Benzofuran Derivatives Containing Imidazo[2,1-b][1,3,4]thiadiazoles as Biological Agents

Polymers have an endless scope in the recent era due to their flexibility, amendment, and insertion of organic and inorganic active components into the polymer backbone. There is strong competition between natural and synthetic biodegradable polymers in the sense of biodegradability and compatibility with modern technology. Biodegradable polymers play a significant role in sustaining mankind on the earth due to non-environment hazards. These polymers play a crucial role in the area of biomedicine technology such as tissues engineering, preparation of different scaffolds, drug delivery systems, industrial, agriculture, and food packaging. Here, we probed on an assortment of types of applications, challenges, and limitations of biodegradable polymers in life.

Venkatesh K. Bhovi

Papers

5-phenyl-1-benzofuran-2-yl derivatives: synthesis, antimicrobial, and antioxidant activity

Synthesis of β-amino carbonyl derivatives of coumarin and benzofuran and evaluation of their biological activity

A Facile Synthesis of Bromo-Substituted Benzofuran Containing Thiazolidinone Nucleus Bridged with Quinoline Derivatives: Potent Analgesic and Antimicrobial Agents

Synthesis of Some Mannich Bases and Novel Benzofuran Derivatives Containing Imidazo[2,1-b][1,3,4]thiadiazoles as Biological Agents

A Review - Biodegradable Polymers and their Applications.