An earlier study (1) from this laboratory proved conclusively that Amytal, 5-ethyl-5-isoamylbarbituric acid (I), is not detoxified by simple hydrolysis of the barbituric acid ring and indicated that the alkyl side chain (or chains) must suffer alteration in viva. Recently (2), it was discovered that the isomeric drug, pentobarbital, is excreted as the diastereoisomers of 5-ethyl-5-(3-hydroxy-1-...

nifedipine (nif), a 1,4-dihydropyridine calcium channel antagonist, undergoes photo-degradation to dehydro-nifedipine (dnif) upon exposure to ultraviolet (uv) light and to the nitroso analogue of dehydro-nifedipine (ndnif) when exposed to sunlight or some kinds of artificial lights. nif photo-degradation products do not contribute to clinical activity, thus prevention of photo-degradation of ni...

Antioxidant activities of wampee peel extracts using five different solvents (ethanol, hexane, ethyl acetate, butanol and water) were determined by using in-vitro antioxidant models including total antioxidant capability, 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity, reducing power, and superoxide scavenging activity. Ethyl acetate fraction (EAF) exhibited the highest antio...

Respiratory tract reflex responses are an important defense mechanism against noxious airborne materials. This study was aimed at defining the effects of adenosine on sensory irritation responsiveness and its role in odorant-irritant interactions. These experiments were aimed at testing the hypothesis that adenosine, through the A2 receptor, enhances trigeminal nerve responses to multiple irrit...

Inhibitory effects of root endophytic actinomycete A-12 from Azadirachta indica A. Juss (Indian lilac, neem) against α-amylase and α-glucosidase were studied. The antioxidant capability was assessed through 2,2-diphenyl-picrylhydrazyl (DPPH), hydroxy radical scavenging and reducing power assays. In vitro antidiabetic activity of ethyl acetate extract revealed good inhibition exhibiting IC50 val...

The antioxidant potential of crude methanol extract (CE) as well as chloroform (CF), ethyl acetate (EF) and n-butanol (NF) soluble fractions of Enhydra fluctuans Lour, which is widely used in indigenous system of medicine for different purposes, were studied. The antioxidant potential of extract/different fractions were evaluated using different in vitro antioxidant models. In addition, total a...

In the cystal structure of the title compound, (2-hy-droxy-ethyl)trimethylammonium dihydrogen phosphate, C(5)H(14)NO(+)·H(2)PO(4) (-), two anions create dimeric structures via two O-H⋯O hydrogen bonds. The hydrogen-bonded dimers are connected by another O-H⋯O hydrogen bond with the hydroxyl groups of the cations, constructing a columner structure along the a axis. A number of C-H⋯O interactions...

An intermolecular C-H functionalization method is developed for the synthesis of 3-hydroxy-2-oxindoles. Rh(III)-catalyzed N-nitroso-directed C-H addition to ethyl 2-oxoacetate allows subsequent denitrosation-triggered cyclization construction of 3-hydroxy-2-oxindoles. The method features a broad substrate scope and its synthetic utility is demonstrated on the synthesis of target compounds beari...

transfusion-dependent patients such as those suffering from β-thalassaemia develop a fatal secondary haemosiderosis and consequently a selective iron chelator must be used to relieve such iron overload. 3- hydroxypyridin-4-ones are selective for iron(iii) under most biological conditions, but unlike desferrioxamine, are efficiently absorbed when administered orally. in this study, the synthesis...