A Review on Synthesis and Biological Activity of Thiazole and its Derivatives

Thiazole, a five-membered heteroaromatic ring, is an important framework of a large number of synthetic compounds. Its diverse pharmacological activity is mirrored in many clinically approved thiazole-containing molecules with, wide range of biological activities, such as antibacterial, antifungal, antiviral, anthelmintic, antitumor, and anti-inflammatory effects. The current review provides an overview of the biological activities of thiazole during the past years.

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

Thiazole, a five-membered heteroaromatic ring, is an important scaffold of a large number of synthetic compounds. Its diverse pharmacological activity is reflected in many clinically approved thiazole-containing molecules, with an extensive range of biological activities, such as antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects. Due to its significance in the field of medicinal chemistry, numerous biologically active thiazole and bisthiazole derivatives have been reported in the scientific literature. The current review provides an overview of different methods for the synthesis of thiazole and bisthiazole derivatives and describes various compounds bearing a thiazole and bisthiazole moiety possessing antibacterial, antifungal, antiprotozoal, and antitumor activity, encouraging further research on the discovery of thiazole-containing drugs.

Chan–Lam N-arylation and C–H amination with heteroaromatic ring-NH: an approach to access extended-fused imidazo[1,2-a]-pyridines/pyrazines

An arene 1,2-diamination reaction of areneboronic acid with heterocyclic azines mediated by Cu(ii) constructs N-fused imidazole rings.

Synthesis and antitubercular activity of new N-[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]-(nitroheteroaryl)carboxamides

Nitro-substituted heteroaromatic carboxamides 1a-e were synthesized and tested against three Mycobacterium tuberculosis cell lines. The activities can be explained in terms of the distribution of the electronic density across the nitro-substituted heteroaromatic ring attached to the amide group. 1,3,5-Oxadiazole derivatives 1c-e are candidates for the development of novel antitubercular agents. Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth.

Planarity and out-of-plane vibrational modes of tryptophan and tyrosine in biomolecular modeling

Vibrations of tryptophan and tyrosine are analyzed to quantify magnitudes of heteroaromatic ring out-of-plane fluctuations in MD of aqueous solutions. Frequencies from normal-mode analysis are compared to experimental data for modified force fields.

Green halogenation reactions for (hetero)aromatic ring systems in alcohol, water, or no solvent

A new method of brominating aromatic and heteroaromatic ring systems is investigated. The combination of hydrobromic acid as the halogen source, hydrogen peroxide as the oxidant, and ethanol, water, or no solvent are evaluated as greener conditions than those that have been previously published. The new conditions give high yields and good regioselectivity for a variety of substrates when the ring is activated by electron-donating groups or heteroatoms. Phenols, anisole, thiophenes, and pyrrole give comparable or superior results when compared to a traditional bromination by N-bromosuccinimide in tetrahydrofuran. Other nitrogen-containing heterocycles do not react under the conditions because they are protonated and hence deactivated; similarly, substrates with electron-withdrawing groups are not brominated. The reaction is very tolerant of a variety of functional groups.

Polycyclic heteroaromatic ring construction driven by silver/cobalt co-catalyzed desulfonylative and defluorinative fragment-recombination of enol nonaflates with amidines

A novel Ag(i)/Co(ii) co-catalyzed tandem fragmentation and recombination reaction commencing from detachable nonaflates and amidines has been developed.