A5024619762- Synthesis and biological activity
- Cholinesterase and Neurodegenerative Diseases
- Bioactive Compounds and Antitumor Agents
- Steroid Chemistry and Biochemistry
- Microbial Natural Products and Biosynthesis
- Multicomponent Synthesis of Heterocycles
- Enzyme function and inhibition
- Phosphodiesterase function and regulation
- Synthesis of heterocyclic compounds
- Carbohydrate Chemistry and Synthesis
- Synthesis and Catalytic Reactions
Benemérita Universidad Autónoma de Puebla
2020-2025
Abstract New conformationally‐restricted steroids were synthesized by incorporating a spiranic heterocyclic motif at the C‐17 position, using trans ‐androsterone, ‐dehydroandrosterone, and estrone as starting materials. A cyclocondensation process with o ‐disubstituted aromatic bis ‐nucleophiles enabled modification of structure. In silico calculations employed to predict diastereoselectivity assignment new chiral center stereochemistry. Spiranic derivatives evaluated in vitro for...
The involvement of carbonic anhydrases (CAs) in a myriad biological events makes the development new inhibitors these metalloenzymes hot topic current Medicinal Chemistry. In particular, CA IX and XII are membrane-bound enzymes, responsible for tumour survival chemoresistance. Herein, bicyclic carbohydrate-based hydrophilic tail (imidazolidine-2-thione) has been appended to CA-targeting pharmacophore (arylsulfonamide, coumarin) with aim studying influence conformational restriction on...
We have designed unprecedented cholinesterase inhibitors based on 1-deoxynojirimycin as potential anti-Alzheimer's agents. Compounds are comprised of three key structural motifs: the iminosugar, for interaction with catalytic anionic site (CAS); a hydrocarbon tether variable lengths, and fragment derived from 2-phenylethanol promoting interactions peripheral (PAS). Title compounds exhibited good selectivity towards BuChE, strongly depending substitution pattern length tether. The lead were...
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