Heterocyclic compounds offer a high degree of structural diversity and have proven to be broadly and economically useful as therapeutic agents. Essential diet ingredients such as thiamine, riboflavin, nicotinamide, pyridoxine, and ascorbic acid are heterocyclic compounds. Thiophene is the backbone of several important products, including pharmaceuticals, dyes, and agrochemicals. In addition, this S-heterocyclic core is present in many natural products, several of which show antibacterial, antifungal, antiamoebic, antioxidant, antitumor, anticoagulant, and antithrombotic activities. 2-Aminothiophenes are important five-membered heterocyclic building blocks in organic synthesis and the chemistry of these small molecules is still developing based on the discovery of cyclization by Gewald. The most convergent and well-established approach for the preparation of 2-aminothiophenes is the Gewald method, which involves the three-component reaction of a ketone, an activated nitrile and elemental sulfur in the presence of morpholine as catalyst. In the continuation of our studies toward the development of new methodologies under green chemistry approaches, herein we reported a mild, efficient, and simple "one pot" Gewald Synthesis of tetra substituted 2-aminothiophene derivatives.
No abstract
This dreadful disease is found in all parts of the world and is becoming a serious threat to the mankind. There are a lot of chemical agents available to control and to treat diabetic patients but total recovery from diabetes has not been reported up to this date. Alternative to these synthetic agents' plants provide a potential source of hypoglycemic drugs and are used widely in several traditional systems of medicine to prevent diabetes. The aim of the present study was to evaluate the antidiabetic activity of methanolic leaf extract of Rhus mysorensis in alloxan-induced diabetic rats.
A simple, sensitive and fast throughput liquid chromatography tandem mass spectrometry (HPLC-ESI-MS/MS) method has been developed for the combined estimation of cabotegravir and rilpivirine in human plasma, using respective deuterated drug as internal standards. The method involved Liquid-Liquid Extraction (LLE) of the analytes and internal standards from human plasma. The chromatographic separation was achieved on a Column: Kromasil C18 column (150 mm x 4.6 mm i.d., 5 μm) analytical column using isocratic mobile phase, consisting of 10mM Ammonium Format and Acetonitrile (70:30 v/v), at a flow-rate of 0.8 mL/min with 75% flow splitting. The parent→product ion transitions 394.40./29106, 364.4/291.06, 398.10/295.06 and 368.4/295.06 (m/z) for Rubitecan, 9-amino rubitecan, Rubitecan-D4 and 9-amino rubitecan-D4, respectively were monitored on a triple quadrupole mass spectrometer, operating in the multiple reactions monitoring (MRM) positive ion mode. The method was validated over the concentration range of 2.5-500ng for Rubitecan and 9-amino rubitecan. The mean recovery values for both the drugs from spiked plasma samples were reproducible. The method was rugged and rapid with a total run time of 4.0 minutes. The retention times were found to be 2.396 for rubitecan and 1.976 for 9-amino rubitecan.
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