Benzofuran/Benzothiophene

Introduction

Benzofuran, whose molecular formula is C8H6O, also known as coumarinone, oxindene and β - benzofuran, is a heterocyclic aromatic organic compound. Benzofuran compounds are widely distributed in higher plants such as Asteraceae, Rutaceae, Liliaceae and Cyperaceae.

Benzofuran is composed of fused heterocyclic compounds. It is the "parent" of many related compounds. There are only eight carbon atoms in the carbon skeleton of benzofurans, but with a variety of biochemical processes in plants, many other functional groups such as hydroxyl, benzene ring, acyloxy, double bond, ester and methoxy are attached to the parent nucleus of these compounds. Benzofuran derivatives can be synthesized by metal catalysis. As early as 1986, Pd(PPh3)2(OAC)2 was used as a catalyst and Cui as an assistant to make terminal alkynes react with 2-halophenol to synthesize polysubstituted benzofuran derivatives.

Application:

Benzofuran derivatives are important heterocyclic compounds with a wide range of biological functions, such as antibacterial, antitumor and anti-inflammatory. A large number of studies have shown that most benzofurans and their derivatives have strong biological activities and important biological functions, mainly including anti-inflammatory, antibacterial, anti tuberculosis, anti-tumor, anti diabetes, cytotoxicity, insecticidal, insect antifeedant and inhibition of histone deacetylase, They play an important role in the treatment of Alzheimer's disease, osteoporosis, arrhythmia, Parkinson's disease and tumor.

Introduction

Benzothiophene is a kind of organic chemical substance. Its molecular formula is C8H6S. It is a white leaf like crystal with naphthalene like odor. Benzothiophene can be volatilized with water vapor, soluble in ethanol, soluble in ether, acetone and general organic solvents, insoluble in water.

Application

Medicine: In recent years, due to the diversity of rotavirus (HRV) serum, HRV is a huge challenge for human beings. Recently, a new benzothiophene derivative was found to be able to inhibit the replication of HRV. The compound combines with the subtype of hrv-b14 and shows similar inhibitory activity to the known capsid inhibitor pleconaril. It can be used as an alternative capsid inhibitor in the treatment of common cold. It has been found that benzothiophene and the sulfonate derivatives of benzofuran are inhibitors of human bicarbonate enzyme II, IX and XII, which have the effect of isoenzyme and can eliminate the side effects of bicarbonate enzyme inhibitors in vivo.

References

  1. Agoni C, Ramharack P, Munsamy G, et al. Human Rhinovirus Inhibition Through Capsid “Canyon” Perturbation: Structural Insights into The Role of a Novel Benzothiophene Derivative[J]. Cell Biochemistry and Biophysics, 2019: 1-11.
  2. Zaraei S O, El-Gamal M I, Shafique Z, et al. Sulfonate and sulfamate derivatives possessing benzofuran or benzothiophene nucleus as potent carbonic anhydrase II/IX/XII inhibitors[J]. Bioorganic & medicinal chemistry, 2019, 27(17): 3889-3901.

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