Agonists at nicotinic acetylcholine receptors (nAChRs) constitute one drug class being evaluated as candidate analgesics. Previous preclinical studies have implicated α4β2 and α7 nAChRs as potential mediators of the antinociceptive effects of (–)-nicotine hydrogen tartrate (nicotine) and other nAChR agonists; however, these studies have relied exclusively on measures of pain-stimulated behavior...

The incorporation of enzyme-catalysed reactions as key features in multi-step organic syntheses is becoming more widespread. Various hydrolase and oxidoreductase enzymes have been used in syntheses of antibiotics and compounds of importance in inflammation and heart disease. The employment of enzymes as catalysts in synthetic organic chemistry is becoming widespread; comprehensive recent review...

Selective oxidation of ring C–H bonds is an attractive route to functionalized cyclic amines, which are versatile intermediates in drug synthesis and important fragment molecules discovery. Here we report a combined substrate enzyme engineering approach achieve enantioselective functionalization all unactivated azepane, azocane, 7-azabicyclo[2.2.1]heptane 8-azaspiro[4.5]decane by cytochrome P45...

A versatile and effectual, three-component one pot (2π + 2π) cycloaddition reaction to the synthesis of substituted azetidines in excellent yields is described. The isonicotinic acid hydrazide (1) as starting materials. Design preparation N-(7-R)-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isonicotinamide derivatives (4a-h) was carried out by condensation isoniazid with aromatic aldehyde (2a-h), ZnCr2O...