A silver nitrate-mediated, efficient phosphorylation of benzothiazoles and thiazoles with diarylphosphine oxides was developed. This process provides a convenient route for the synthesis of a variety of 2-diarylphosphoryl benzothiazoles and thiazoles which are promising precursors of a series of hemilabile P,N-ligands with small bite angles.

Thiazoles displayed broad range of biological activities and found in many potent biologically active molecules such as Sulfathiazol (antimicrobial drug), Ritonavir (antiretroviral drug), Abafungin (antifungal drug) and Tiazofurin (antineoplastic drug). So far, modifications of the thiazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlight...

A wide range of 5-substituted thiazoles are easily accessible via cross coupling of thiazolyl triflates. These activated thiazoles can be obtained by Ugi reactions using thioacids (thio-Ugi-reaction) and subsequent cyclisation of the endo thiopeptides formed with triflic anhydride. In addition, cyclisations with acyl halides give rise to 5-acyloxysubstituted derivatives.

A novel and efficient method for the one-pot synthesis of 2,4-disubstituted thiazoles from carboxylic acids or anhydrides is presented. Based on this new method, the total synthesis of the bis-2,4-disubstituted bis(thiazoles) natural product cystothiazole C is also presented.

Structurally diverse thiazoles with electron-donating and electron-withdrawing groups were conveniently synthesized through manganese dioxide (MnO(2)) oxidation of the corresponding thiazolines. The effect of substitution at the 2- and 4-positions was investigated. The desired thiazoles with aryl or vinyl substitutions at the 2- or 4-position can be obtained in good to excellent yields.

Citation: Ibrar A, Khan A, Ali M, Sarwar R, Mehsud S, Farooq U, Halimi SMA, Khan I and Al-Harrasi A (2018) Combined in Vitro and in Silico Studies for the Anticholinesterase Activity and Pharmacokinetics of Coumarinyl Thiazoles and Oxadiazoles. Front. Chem. 6:61. doi: 10.3389/fchem.2018.00061 Combined in Vitro and in Silico Studies for the Anticholinesterase Activity and Pharmacokinetics of Cou...

Chagas disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affects approximately 6-7 million people worldwide. Benznidazole is the only drug approved for treatment during the acute and asymptomatic chronic phases; however, its efficacy during the symptomatic chronic phase is controversial. The present work reports the synthesis and anti-T. cruzi activities of a novel ser...

Thiazolines and thiazoles are an integral part of numerous natural products, a number of drugs, and many useful molecules such as ligands for metal catalysis. We report the first common synthetic protocol for the synthesis of thiazoles and thiazolines. Novel molecules are efficiently synthesized by using readily available and inexpensive substrates. The reaction conditions are mild and pure pro...

Remarkably high-speed synthesis of 2-substituted amino-4-aryl thiazoles in polar solvents with a minimum threshold polarity index of 4.8 was found to proceed to completion in just 30-40 sec. affording excellent yields of thiazoles under ambient temperature conditions without the use of any additional catalyst. The purification-free procedure afforded libraries based around a known pharmacophore...

The Front Cover picture shows structures of the key compounds and the change in the fluorescence. Although electron-donating and -accepting groups of monocyclic 5-N,N-diarylaminothiazoles are not in the same plane but highly deviated, they show relatively strong fluorescence from blue to orange. In particular, the addition of Brønsted and Lewis acids to 5-N,N-diaryl-2-(4-pyridyl)thiazoles shift...