Search

Your search keyword '"Fabian Gusovsky"' showing total 3 results
Start Over Author "Fabian Gusovsky" Publisher american chemical society (acs)
3 results on '"Fabian Gusovsky"'

1. Transformation of the Manufacturing Process from Discovery to Kilogram Scale for AWZ1066S: A Highly Specific Anti-Wolbachia Drug Candidate for a Short-Course Treatment of Filariasis

Author

W. David Hong, Paul M. O’Neill, Mark J. Taylor, Joseph D. Turner, Stephen A. Ward, Fabian Gusovsky, Farid Benayoud, Nao Shibuguchi, Dixit Girish, Francis Gerard Fang, Ravi Kumar Talabhakthla, Anand Vaddi, Chiranjeevi Challa, Karri Satya Ammi Reddy, Vijay Kalla, Sugandham Srinivasa Rao, Durga Mahesh Kumar Nagireddi, Jayesh Patel, and Anil Shahaji Khile

Subjects
Organic Chemistry, Physical and Theoretical Chemistry
Published
2023

2. Crystallization-Based Synthetic Route to Antimalarial Agent BRD5018: Diazocene Ring Formation via a Staudinger-aza-Wittig Reaction on an Azetidine-Ribose Template

Author

Francis G. Fang, Fabian Gusovsky, Vijay Kalla, Venkata Sasidhar Balla, Dixit Girish, Chiranjeevi Terli, Branko Mitasev, Ravi Kumar Talabhakthula, Venugopalarao Vikram, Srinivasa Rao Sugandham, Bruno Melillo, Anand Vaddi, Jiong Yang, Stuart L. Schreiber, Srikanth Bathula, Pavan Kumar Rayaprolu, Anil Shahaji Khile, and Masaharu Gotoda

Subjects
chemistry.chemical_compound, law, Chemistry, Stereochemistry, Organic Chemistry, Wittig reaction, Azetidine, Ribose, Antimalarial Agent, Physical and Theoretical Chemistry, Crystallization, Ring (chemistry), law.invention
Published
2021

3. Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity

Author

Cyrus R. Creveling, Fabian Gusovsky, George Chen, Kenneth L. Kirk, Bang Hua Chen, Jun Ying Nie, John W. Daly, and Michael King

Subjects
Epinephrine, Adrenergic receptor, Stereochemistry, Inositol Phosphates, Fluorine Compounds, Guinea Pigs, Adrenergic, Electrophilic aromatic substitution, Dioxanes, Norepinephrine, Phenylephrine, Structure-Activity Relationship, Electrophilic substitution, chemistry.chemical_compound, Ethanolamine, Receptors, Adrenergic, beta, Drug Discovery, Prazosin, medicine, Animals, Cerebral Cortex, Cell Membrane, Biological activity, Receptors, Adrenergic, alpha, Rats, chemistry, Electrophile, Molecular Medicine, Synaptosomes, medicine.drug
Abstract

Synthetic routes to difluorinated analogs of the adrenergic agonists, norepinephrine (NE), epinephrine (E), and phenylephrine (PE) have been developed. The syntheses were based on elaboration of the ethanolamine side chains from the appropriately polyfunctionalized benzaldehydes. The benzaldehydes were prepared from precursor difluorinated benzenes by sequential regioselective lithiations and reaction with electrophiles to introduce hydroxyl and carboxaldehyde functionalities. Binding and functional assay data demonstrate that the 2,6-difluorinated analogs are relatively inactive at both alpha- and beta-adrenergic receptors. These results are consistent with earlier observations that 2-fluoro substitution of adrenergic agonists decreases alpha-adrenergic activity whereas 6-fluoro substitution decreases beta-adrenergic activity.

Published
1993

Catalog

Books, media, physical & digital resources
See catalog results