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Asymmetric Synthesis of Biological Active Amino Derivatives and Multi-target Drug

Award Number: R15GM112109
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: 05/01/2015
PERIOD OF PERFORMANCE END DATE: 04/30/2019

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Asymmetric Synthesis of Biological Active Amino Derivatives and Multi-target Drug - Program Director/Principal Investigator (Last, First, Middle): Project Summary/Abstract Our long term general goal is to develop novel organic synthetic methodologies for the preparation of potential nonracemic amino drugs that can affect different cholinergic pathways and have neuroprotective properties, which will be valuable for the treatment of neurodegenerative diseases. Nonracemic compounds, particularly non natural amino acids and heterocyclic amino compounds are important biologically active small molecules as drugs themselves, or as chiral building blocks for the synthesis of a variety of drugs. Non-natural amino alcohols and amino acids are important tools in drug discovery and when they are used in therapeutic peptidomimetics as chemical probes to understand the mechanism of biological systems. Thus, new suitable and facile asymmetric methods for the synthesis of these amino compounds are strongly needed. The main objective in this proposal is to design novel synthetic transformations using facile and environmentally friendly chiral boron compounds with high stereo-selectivity for the preparation of enantiopure key amino compounds. The previous expertise obtained in the enantioselective borane-mediated reductions catalyzed by novel aminoborate esters will be directed to: 1) To design new protocols for the asymmetric synthesis of novel amino alcohols, and non-natural amino acid and multi-functional amines with pharmaceutical potential. 2) To develop new multifunctional nicotine and benzazepine analogues for the treatment of neurodegenerative diseases such as Alzheimer's Disease. The synthetic aspects of these processes, including the structural factors affecting the reactivity and stereo chemical outcome, will be studied by computational methods. Thus, new large scale asymmetric methodologies will be established, particularly, for the synthesis of non-natural amino alcohols, amino acids and heterocyclic amino derivatives of neurological interest that will open new avenues to prepare important enantiopure non-natural peptides and other bioactive intermediaries. Likewise, this project will provide a positive impact on the education of a significant number of disadvantage undergraduate students from Puerto Rico offering them advanced knowledge and experience in synthetic organic and medicinal chemistry. PHS 398/2590 (Rev. 06/09) Page Continuation Format Page


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: 2019 ( Subtotal = -$2,537 )
2019	2018	UNIVERSITY OF PUERTO RICO	CARR 908 KM 1.0 BO TEJAS	HUMACAO	PR	00791	HUMACAO	USA	Biomedical Research and Research Training	000	1	5/24/2019	SUPPLEMENT FOR EXPANSION	-$2,537
														Subtotal = -$2,537

Issue Date FY: 2018 ( Subtotal = $63,176 )
2018	2018	UNIVERSITY OF PUERTO RICO	CARR 908 KM 1.0 BO TEJAS	HUMACAO	PR	00791	HUMACAO	USA	Biomedical Research and Research Training	000	1	9/5/2018	SUPPLEMENT FOR EXPANSION	$63,176
														Subtotal = $63,176

Issue Date FY: 2015 ( Subtotal = $325,153 )
2015	2015	HUMACAO UNIVERSITY COLLEGE	CUH STATION	HUMACAO	PR			USA	Biomedical Research and Research Training	000	1	5/1/2015	NEW	$325,153
														Subtotal = $325,153

Grand Total All Awards = $385,792

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Asymmetric Synthesis of Biological Active Amino Derivatives and Multi-target Drug

Award Number: R15GM112109

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: 05/01/2015

PERIOD OF PERFORMANCE END DATE: 04/30/2019

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