The synthesis and aromatase inhibitory activity of androst-4-en-, androst-5-en-, 1β,2β-epoxy- and/or androsta-4,6-dien-, 4β,5β-epoxyandrostane-, and 4-substituted androst-4-en-17-oxime derivatives are described. Inhibition activity of synthesized compounds was assessed using aromatase enzyme and [1β-3H]androstenedione as substrate. Most of the compounds displayed similar to or more aromatase in...

We report here the discovery and development of boron-assisted oxime formation as a powerful connective reaction for chemical biology. Oximes proximal to boronic acids form in neutral aqueous buffer with rate constants of more than 10 M 1 s , the largest to date for any oxime condensation. Boron's dynamic coordination chemistry confers an adaptability that seems to aid a number of elementary st...

In the crystal structure of the title compound, C(7)H(8)N(2)O, mol-ecules are connected via inter-molecular N-H⋯O and O-H⋯N hydrogen bonds to form a two-dimensional supra-molecular structure. The oxime group has an E configuration and the dihedral angle between the mean planes of the benzene ring and the amidoxime grouping is 20.2 (3)°.

Selective syntheses are now available for compounds of many classes, based on C-centered radicals, exploiting a diverse range of mechanisms. The prospect for chemistry based around N- and O-centered radicals is probably more favorable because of the importance of heterocycles as biologically active materials. Heteroradical chemistry is still comparatively underdeveloped due to the need for safe...

Twenty-three new oxime ester derivatives of nafimidone were synthesized with the prospect of potential anticonvulsant activities. MES and ScM tests were employed for their anticonvulsant activities and rotorod test for neurological deficits. Eighteen compounds were found to be protective against MES seizures. Alkyl (1-8) and arylalkyl (9, 10) oxime ester derivatives were found to be more active...

Four N-phenyl substituted carbazole oxime ester photoinitiators were synthesized and their structure-activity relationship systematically investigated. These have a broad absorption in the range of 300-400 nm tail extends above 400 nm. Under 405 LED light irradiation, esters undergo photodecarboxylation generate active free radicals to induce polymerization acrylates. The tert-butyl aldehyde-ox...

Vicinal aminoalcohols are widespread structural motifs in bioactive molecules. We report the development of a new dioxazolone reagent containing p-nitrophenyldifluoromethyl group, which 1. displays good safety profile; 2. shows remarkably high reactivity oxime-directed iridium(III)-catalyzed amidation unactivated C(sp3)−H bonds; 3. leads to amide products can be hydrolyzed under mild conditions...

Organophosphorus compounds (OPs) are potent inhibitors of acetylcholinesterase (AChE). Treatment for OP poisoning is by administration of atropine sulfate, an oxime, and diazepam. Oximes such as 2-PAM are used to reactivate OP-inhibited AChE so as to restore normal enzymatic function and serve as a true antidote. There are reports of non-enzymatic hydrolysis by oximes of acetylthiocholine in in...