Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.

Thiazole Ring-A Biologically Active Scaffold.

For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor–acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemical pathways and enzymes or stimulate/block the receptors in the biological systems. Therefore, medicinal chemists have been focusing their efforts on thiazole-bearing compounds in order to develop novel therapeutic agents for a variety of pathological conditions. This review attempts to inform the readers on three major classes of thiazole-bearing molecules: Thiazoles as treatment drugs, thiazoles in clinical trials, and thiazoles in preclinical and developmental stages. A compilation of preclinical and developmental thiazole-bearing molecules is presented, focusing on their brief synthetic description and preclinical studies relating to structure-based activity analysis. The authors expect that the current review may succeed in drawing the attention of medicinal chemists to finding new leads, which may later be translated into new drugs.

/pdf/thiazole-a-versatile-standalone-moiety-contributing-to-the-3tr99tyz.pdf

Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents

Synthesis, anti-proliferative activity, gene expression, docking and DFT investigation of novel Pyrazol-1-yl-thiazol-4(5H)-one derivatives

Synthesis, anti-proliferative activity, gene expression, docking and DFT investigation of novel pyrazol-1-yl-thiazol-4(5H)-one derivatives

Synthesis, Spectral, Crystal structure, Hirshfeld surface, Computational analysis, and Antimicrobial studies of Ethyl-(E)-4-(2-(2-arylidenehydrazinyl)-2-oxoethyl)piperazine-1-carboxylates

A new class of compounds formed by the linkage of -C(O)-NH- with pyridine and thiazole moieties was designed, synthesized, and characterized by various spectral approaches. The newly characterized compounds were evaluated for their antimicrobial as well as anti-inflammatory properties. The in vitro anti-inflammatory activity of these compounds was evaluated by denaturation of the bovine serum albumin method and showed inhibition in the range of IC50 values-46.29-100.60 μg/mL. Among all the tested compounds, compound 5l has the highest IC50 value and compound 5g has the least IC50 value. On the other hand, antimicrobial results revealed that compound 5j showed the lowest MIC values and compound 5a has the highest MIC values. Furthermore, molecular docking of the active compounds demonstrated a better docking score and interacted well with the target protein. Physicochemical parameters of the titled compounds were found suitable in the reference range only. The in silico molecular docking study revealed their COX-inhibitory action. Compound 5j emerged as a significant bioactive molecule among the synthesized analogues.

https://pubs.acs.org/doi/pdf/10.1021/acsomega.0c03386

Pyridine- and Thiazole-Based Hydrazides with Promising Anti-inflammatory and Antimicrobial Activities along with Their In Silico Studies.

Preparation and physicochemical assessment of bioactive films based on chitosan and starchy powder of white turmeric rhizomes (Curcuma Zedoaria) for green packaging applications.

This study explains the development of eco-friendly polyvinyl alcohol (PVA)/oxidized maize starch (OMS)/Betel leaves extract (BLE) blend films by employing a cost effective technique. The influence of BLE on structural, Thermal, Mechanical, Morphological, Optical, Antibacterial and Antioxidant properties of the PVA/OMS blend were investigated successfully by applying various characterization techniques. The hydrogen bonding interaction among the components of the blend films led to enhance thermal stability, miscibility, mechanical properties, smooth surface morphology and UV blocking properties of the blend films. The addition of BLE enormously improved the antibacterial and antioxidant properties of the PVA/OMS blend films. Moreover, the obtained films were hydrophilic, water soluble and biodegradable in nature. With regard to barrier properties the water vapour transmission rate and oxygen permeability of the blend films were enhanced after doping of BLE. These experimental outcomes suggest that the BLE containing PVA/OMS films can be used for the expansion of active packaging materials.

/pdf/exploration-of-multifunctional-properties-of-piper-betel-4ll8396sx3.pdf

Exploration of Multifunctional Properties of Piper Betel Leaves Extract Incorporated Polyvinyl Alcohol-Oxidized Maize Starch Blend Films for Active Packaging Application

Sheela Khanapure

Papers

Pyridine- and Thiazole-Based Hydrazides with Promising Anti-inflammatory and Antimicrobial Activities along with Their In Silico Studies.

Preparation and physicochemical assessment of bioactive films based on chitosan and starchy powder of white turmeric rhizomes (Curcuma Zedoaria) for green packaging applications.

Exploration of Multifunctional Properties of Piper Betel Leaves Extract Incorporated Polyvinyl Alcohol-Oxidized Maize Starch Blend Films for Active Packaging Application

Ionically Crosslinked Chitosan/Tragacanth Gum Based Polyelectrolyte Complexes for Antimicrobial Biopackaging Applications

Multifunctional ZnO/CeO2 nanocomposites for Photoinduced dye degradation and Antibacterial activities