Synthesis and Antimicrobial Activity of Novel Thiazoles with Reactive Functional Groups

Abstract

A series of substituted thiazoles bearing different functional groups, such as carboxyethylamino, carboxyl, chloromethyl, (phenylamino)methyl, ethoxyoxoethyl, methoxyoxoethylidene, ethoxycarbonyl, (methoxy or hydrazinyl)oxopropyl, carbohydrazinyl, formyl, and ((phenyl, carbamothioyl or isonicotinoyl)hydrazono)methyl, incorporated into their structure were synthesized. The synthesized compounds were tested for their antimicrobial activity against Escherichia coli, Staphylococcus aureus, and Mycobacterium luteum bacteria strains, and Candida tenuis and Aspergillus niger fungi. Compounds exhibiting exclusive antifungal activity against Aspergillus niger (MIC 0.9, 1.9 μg/mL) and Candida tenuis (MIC 7.8 μg/mL) have been identified among the novel thiazole derivatives.

Design, Synthesis, and Evaluation of New Hybrid Derivatives of 5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-2(1H)-one as Potential Dual Inhibitors of Blood Coagulation Factors Xa and XIa

“…Thus, methyl 2-(4-oxothiazol-5(4 H )-ylidene)acetate, which is easy to prepare, was chosen as the thiazole-containing fragment. This heterocyclic fragment is a well-known pharmacophore among the functional derivatives of which compounds with antitumor [ 69 , 70 , 71 , 72 ], antimicrobial [ 65 , 73 , 74 , 75 ], antifungal [ 75 ], antiviral [ 76 , 77 ], antioxidant [ 65 , 78 ], anti-inflammatory [ 79 ], as well as anticoagulant [ 80 ] activity have been found.…”

Synthesis, Characterization and Antibacterial Assays of Novel N,N1‐Disubstituted 2,2′‐Dithiodianiline Derivatives

“…[43] Previously, we have synthesized a library of N,N-disubstituted β-aminoacids derivatives containing hydrazone and azole fragments and have evaluated their biological properties, which appeared to possess the convincing anticancer effect against triple-negative breast cancer and glioblastoma cells in vitro. [44] They demonstrated promising antimicrobial, [45][46][47][48] significant antibacterial, [49][50][51][52] and in addition, antiviral and antioxidant [51,52] activities.…”

Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens

“…Profound biological activity of azole derivatives makes them as attractive building blocks to develop novel antimicrobial candidates for the further pre-clinical development [ 55 , 56 , 57 , 58 , 59 , 60 ]. In this paper we describe the synthesis and in vitro antimicrobial activity characterization of novel thiazole derivatives bearing N-acyl hydrazone, pyrrole, pyrazole, and triazole.…”