Excursions in drug discovery

A novel 3-acetoxy-2-methyl-N-(4-methoxyphenyl)benzamide: Molecular structural describe, antioxidant activity with use X-ray diffractions and DFT calculations

“…peptides and proteins) [1][2][3][4][5][6][7][8][9] and potential drug compounds that contain an amide bond [10][11][12][13], such as acetaminophen (analgesic), lidocaine (Xylocaine, local anaesthetic) loperamide (Imodium AD, anti-diarrheal) [1,2], atorvastatin (cholesterollowering) [14], lisinopril (inhibitor of angiotensin converting enzyme) [15], valsartan (blockade of angiotensin-II receptors) [16], and diltiazem (calcium channel blocker used in the treatment of angina and hypertension) [17]. Amides represent an important class of compounds found in numerous bioactive products such as sorafenib [18], lipitor [19] and vyvanse [20], which have been widely used for the treatment of cancer, hypercholesterolemia, and juvenile hyperactivity, respectively [21].…”

A series of novel β-hydroxyamide based catalysts for borane-mediated enantioselective reductions of prochiral ketones

“…Amide bond formation 24 usually requires the activation of a carboxylic acid moiety in the presence of coupling reagents. 25 One of the most widely used reagents is N-(3-dimethylaminopropyl)-N 0 -ethylcarbodiimide hydrochloride (EDCI)/1-hydroxybenzotriazole hydrate (HOBt). They show moderate activity, are reasonably inexpensive and produce a water-soluble urea as a by-product, which can be easily removed from the product by aqueous washes.…”

β‐Hydroxyamide‐Based Ligands and Their Use in the Enantioselective Borane Reduction of Prochiral Ketones

“…31,32 Peptides and proteins play an important role in modern biology. 34 N-(3-Dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride (EDCl)/HOBt reagents have been widely used in amide synthesis to improve yields, because they show a moderate activity and they are reasonably cheap. 33 The process usually requires activation of a carboxylic acid moiety in the presence of coupling reagents.…”