ABSTRACT
A series of 27 new barbiturates and thiobarbiturates have been synthesized by a convenient multi-component reaction in overall excellent yields (87-96%). All the synthesized compounds were characterized by 1H, 13C NMR, EIMS and elemental analysis (C, H, N and S). Furthermore, all compounds were screened for in vitro antioxidant (DPPH radical scavenging), lipoxygenase, chymotrypsin, α-glucosidase and anti-urease activities. Out of the series, 23 in DPPH, 14 in lipoxygenase, 2 in chymotrypsin have shown appreciable IC50 values.
Subject(s)
Antioxidants/chemical synthesis , Barbiturates/chemical synthesis , Enzyme Inhibitors/chemical synthesis , Thiobarbiturates/chemical synthesis , Antioxidants/chemistry , Barbiturates/chemistry , Biphenyl Compounds/antagonists & inhibitors , Chymotrypsin/antagonists & inhibitors , Chymotrypsin/chemistry , Enzyme Assays , Enzyme Inhibitors/chemistry , Lipoxygenase/chemistry , Picrates/antagonists & inhibitors , Thiobarbiturates/chemistry , Urease/antagonists & inhibitors , Urease/chemistry , alpha-Glucosidases/chemistryABSTRACT
Four new ecdysteroids (1-4), along with three known steroids, ß-ecdysone (5), 5-ß-2-deoxyintegristerone A (6) and 24-epi-makisterone A (7) (Fig. 1), were isolated from the methanolic extract of the flowers of Aerva javanica by using normal and reverse phase chromatography. The structures of the new compounds (1-4) were determined due to 1D ((1)H and (13)C), 2D NMR (HSQC, HMBC, COSY, NOESY) techniques and high resolution mass spectrometry (HREIMS). The known compounds (5-7) were characterized based on the 1D NMR spectroscopy and mass spectrometry and by comparison with the literature values. All isolates were evaluated for their inhibitory activities against enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase (LOX).
Subject(s)
Amaranthaceae/chemistry , Ecdysteroids/chemistry , Ecdysteroids/isolation & purification , Flowers/chemistryABSTRACT
An antibiotic polyketide, Cryptosporioptide (1) was isolated from the culture extract of the endophytic fungus Cryptosporiopsis sp. The structure of Cryptosporioptide has been established with the help of 1D ((1)H, (13)C), 2D NMR (HSQC, HMBC, COSY, NOESY) techniques and mass spectrometry (FABMS, HRFABMS). The absolute configuration was established by means of electronic circular dichroism (ECD). Cryptosporioptide exhibited both lipoxygenase inhibitory and anti-Bacillus megaterium activities.
