Microwave-Assisted Synthesis and Pharmacological Activity of Pyrazolyl Benzofuran Deravatives

Abstract

Microwave-assisted Organic Reaction Enhancement (MORE) has emerged as a new 'lead' in organic synthesis. During the studies we observed that microwave -assisted organic synthesis requires 2-4 min. of time whereas the conventional ones takes 4-6 hrs and often with poor yields. Hence, with an objective of reducing the reaction time, application of microwave technique has proved to be advantageous in case of synthesis of new benzofuran derivatives. The structures of synthesized derivatives emerged is confirmed by their IR, NMR and Mass spectra. The representative compounds synthesized with this route is further screened for anti-bacterial, analgesic, anti-inflammatory and ulcerogenic studies. In this study we have observed that the benzofuran derivatives are less ulcerogenic compared to phenyl butazone. The structural comparisons have revealed that the chloro substitution will increase the ulcerogenic toxicity.

Synthesis and Evaluation of Antioxidant Activity of Some New Heterocyclic Compounds Bearing the Benzo[B]Furan Moiety

“…Reaction of 2 with p-anisaldehyde afforded the corresponding anisal derivative 2-cyano-N-[1-(5-methoxy-2-methylbenzofuran-3-yl)ethylidene)-3-(4-methoxyphenyl]acrylohydrazide (5). The IR spectrum of 5 showed absorption bands at 3318 for (NH), 2212 for (CN) and at 1660 cm -1 for (CO).…”

Synthesis, characterization and evaluation of biological activities of some 2,3-diaryl bicyclo methanones

“…were recorded on Thermo Scientific Nicolet iS5, USmade Fourier transform spectrophotometer. The NMR spectra of selective compounds were recorded on a Bruker AV 400 spectrometer operating at 400 MHz for 1 H NMR spectra and 100 MHz for 13 C NMR spectra in CDCl3 solvent using TMS as internal standard. Electron impact and chemical ionization mode FAB + mass spectra were recorded with a Shimadzu spectrometer.…”

“…Methyl ketones and bicyclo methanones possess many pharmacological activities such as, AVP release and activation of vasopressin receptors [3], antimicrobial [4][5][6][7][8][9][10][11][12][13][14][15], cannabinoid receptor agonists [16], neuronal nicotinic acetylcholine receptors (nAChRs) [17], anti-inflammatory [12,13,18,19], analgesic [10,19], anticonvulsant [10,19], antitumor [19], anticancer [10], antiviral [19], anti-diabetic [10,20], antitubercular [20], antihelminthic [12,20], antidepressant [21], ulcerogenic [18], antinociceptive [10], protein tyrosine kinase inhibitor [22], DNA cleavage [23], Alzheimer's disease curing agent [24], antioxidant [25], acute toxicity [18], antihypertensive [10] and insect antifeedant activities [25]. Numerous solvent-free and solvent assisted synthetic methods with or without catalysts were reported in the literature for the synthesis of stereo selective monoand bicyclo-methanones [26][27]…”

Silver(i)-catalyzed dehydrogenative cross-coupling of 2-aroylbenzofurans with phosphites

“…3 Several derivatives of benzofuran have been recognized as biologically and pharmacologically relevant molecules. 4 Besides these, a large number of benzofuran-based compounds have anti-inflammatory and/or antiarrhythmic, 5 antidepressant, 6 antimicrobial, 7 antitumor, 8 antioxidant, 9 anti-AD (Alzheimer's disease), 10 anti-HIV/HCV, 11 anti-TB, anticoagulant, analgesic, anti-diabetic, hypoglycemic and immunosuppressive activities. 12 Furthermore, many benzofuran derivatives have been used in a wide range of pharmaceutical agents and functionalized materials.…”