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New Chemical Tools for the Synthesis of Trisubstituted Hydroxylamines and their Application as Bioisosteres in Medicinal Chemistry

Award Number: R21GM144753
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/15/2021
PERIOD OF PERFORMANCE END DATE: 08/31/2023

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New Chemical Tools for the Synthesis of Trisubstituted Hydroxylamines and their Application as Bioisosteres in Medicinal Chemistry - This is a proposal to develop new tools for the practical effective synthesis of N,N,O- trisubstituted hydroxylamines, or hydroxalogs, as novel isosteres for application in medicinal chemistry across a broad swath of compound classes and diseases states. The three specific aims presented encompass i) tools development for the synthesis of N,N,O-trisubstituted hydroxylamines by a variety of inter- and intramolecular methods; ii) synthesis of a series of phenylpropylpiperidine ligands for the σ-1 and σ-2 receptors and their use as models for the comparative study of the physical and drug-like properties of the hydroxalogs, thereby enhancing their applicability as tools in medicinal chemistry; iii) synthesis of a series of hydroxalogs of the ethanolamine H1 antagonists and comparative determination of their antihistamine activity in a cell-based assay, again with the view to validating the hydroxalogs as isosteres as tools in medicinal chemistry.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2024 ( Subtotal = -$97 )
2024	2022	UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.	310 E CAMPUS RD RM 409	ATHENS	GA	30602	CLARKE	USA	Biomedical Research and Research Training	000	2	4/8/2024	NON-COMPETING CONTINUATION	-$97
														Subtotal = -$97

Issue Date FY: 2022 ( Subtotal = $185,445 )
2022	2022	UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.	310 EAST CAMPUS RD TUCKER HALL ROOM 409	ATHENS	GA	30602	CLARKE	USA	Biomedical Research and Research Training	000	2	9/1/2022	NON-COMPETING CONTINUATION	$185,445
														Subtotal = $185,445

Issue Date FY: 2021 ( Subtotal = $223,195 )
2021	2021	UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.	310 EAST CAMPUS RD TUCKER HALL ROOM 409	ATHENS	GA	30602	CLARKE	USA	Biomedical Research and Research Training	000	1	9/8/2021	NEW	$223,195
														Subtotal = $223,195

Grand Total All Awards = $408,543

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New Chemical Tools for the Synthesis of Trisubstituted Hydroxylamines and their Application as Bioisosteres in Medicinal Chemistry

Award Number: R21GM144753

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/15/2021

PERIOD OF PERFORMANCE END DATE: 08/31/2023

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