The anti Parkinson drug, rasagiline [R-(+)-N-propargyl-1-aminoindan], an inhibitor of type B monoamine oxidase, has been shown to suppress apoptosis induced by neurotoxins and oxidative stress. A series of novel propargylaminoindans with a carbamate moiety to inhibit cholinesterase were developed from phamacophore of rasagiline to protect or rescue deteriorated neurons in Alzheimer's and Lewy B...

Urease (urea amidohydrolase) is usually found in different bacteria, fungi, algae and plants. It is accountable for the hydrolysis of urea and thus, forming ammonia and carbamate, which is the final step of nitrogen metabolism in living organisms [1,2]. The carbamate intern quickly and spontaneously decomposes, yielding a second molecule of ammonia. These reactions may cause significant increas...

The protecting-group-free asymmetric synthesis of 1,2,4-trideoxy-1,4-imino-L-xylitol is readily achieved in five steps from 2-deoxy-D-ribose and with an overall yield of 48%. Key in this synthesis is the application of our recently developed Vasella-reductive amination and carbamate annulation methodologies to the synthesis of 2-deoxy-aza-sugars. The carbamate annulation occurred with excellent...

An ultrasonic reaction of Ag(2)O, 4,4'-bipyridine (bipy) and (2S, 3R)-3-amino-2-hydroxybutanoic acid (L-Thr) gives an unexpected Ag(I) supramolecular framework, {[Ag(3)(bipy)(3)(cahba)]·HCO(3)·10H(2)O}(n) (1), in which the (2S, 3R)-3-(carboxyamino)-2-hydroxybutanoic acid (H(2)cahba) is a carbamate derivative of L-Thr, obtained via in situ transformation of amino group of L-Thr into carbamate by...

Organophosphorus and carbamate insecticides are toxic to insects and mammals by virtue of their ability to inactivate the enzyme acetylcholinesterase. This review addresses the mechanism of inhibition of acetylcholinesterase by organophosphorus and carbamate esters, focusing on structural requirements necessary for anticholinesterase activity. The inhibition of acetylcholinesterase by these com...

The FeCl3·6H2O-catalyzed three-component aza-Friedel-Crafts reaction of aromatic/heteroaromatic compounds, aromatic aldehydes and tert-butyl carbamate was reported. The subsequent Friedel-Crafts-type alkylation of the resulting tert-butyl diarylmethyl carbamate with heteroaromatic compounds under "open-flask" at room temperature was also performed. The two-step reaction was especially useful fo...

The carbamate group is a key structural motif in many approved drugs and prodrugs. There is an increasing use of carbamates in medicinal chemistry and many derivatives are specifically designed to make drug-target interactions through their carbamate moiety. In this Perspective, we present properties and stabilities of carbamates, reagents and chemical methodologies for the synthesis of carbama...

The synthesis of the pharmaceutical (R)-tolterodine is reported using lithiation/borylation-protodeboronation of a homoallyl carbamate as the key step. This step was tested with two permutations: an electron-neutral aryl Li-carbamate reacting with an electron-rich boronic ester and an electron-rich aryl Li-carbamate reacting with an electron-neutral boronic ester. It was found that the latter a...