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Design and synthesis of bioactive sm...

Brown University.

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Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess.

Record Type:	Electronic resources : Monograph/item
Title/Author:	Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess./
Author:	Onaran, Mehmet B.
Description:	233 p.
Notes:	Source: Dissertation Abstracts International, Volume: 69-06, Section: B, page: 3589.
Contained By:	Dissertation Abstracts International69-06B.
Subject:	Chemistry, Biochemistry. -
Online resource:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3319114
ISBN:	9780549689843

Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess.
Onaran, Mehmet B.

Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess. - 233 p.

Source: Dissertation Abstracts International, Volume: 69-06, Section: B, page: 3589.

Thesis (Ph.D.)--Brown University, 2008.

Aryl alpha-ketocarboxylic acids were evaluated as a new type of phosphotyrosine mimic. Their inhibition potency was measured against the protein tyrosine phosphatase from Yersinia enterocolitica resulting in IC 50 values ranging from 79 to 2700 muM. We found that compounds with larger aromatic groups, or higher electron density in their aromatic groups showed higher inhibition activity. The alpha-hydroxycarboxylic acids, in general, were less potent inhibitors compared to the corresponding alpha-ketocarboxylic acids. One exception to this observation was the furan-based alpha-hydroxycarboxylic acid, which had an IC50 value of 27 muM.

ISBN: 9780549689843Subjects--Topical Terms:

1017722
Chemistry, Biochemistry.

Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess.
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020 $a 9780549689843
035 $a (UMI)AAI3319114
035 $a AAI3319114
040 $a UMI $c UMI
100 1 $a Onaran, Mehmet B. $3 1029767
245 1 0 $a Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess.
300 $a 233 p.
500 $a Source: Dissertation Abstracts International, Volume: 69-06, Section: B, page: 3589.
502 $a Thesis (Ph.D.)--Brown University, 2008.
520 $a Aryl alpha-ketocarboxylic acids were evaluated as a new type of phosphotyrosine mimic. Their inhibition potency was measured against the protein tyrosine phosphatase from Yersinia enterocolitica resulting in IC 50 values ranging from 79 to 2700 muM. We found that compounds with larger aromatic groups, or higher electron density in their aromatic groups showed higher inhibition activity. The alpha-hydroxycarboxylic acids, in general, were less potent inhibitors compared to the corresponding alpha-ketocarboxylic acids. One exception to this observation was the furan-based alpha-hydroxycarboxylic acid, which had an IC50 value of 27 muM.
520 $a Matrix metalloproteases (MMPs) are a family of structurally related endopeptidases that degrade and remodel components of a number of tissues to maintain normal physiology. Overexpression of MMPs is associated with a variety of pathological conditions including tumor growth and metastasis, angiogenesis, destruction of joints that causes osteoarthritis and rheumatoid arthritis, and periodontal disease. There is significant interest in developing MMP inhibitors for therapeutic applications. We have designed and synthesized a series of squarate based peptidic inhibitors and evaluated them as a new type of Matrix Metalloprotease-1 inhibitor.
520 $a Tetrahydroisoquinolines (THIQs) substituted at the C-1 position constitute the framework of many bioactive compounds. We have developed chiral ligands that promote the enantioselective addition of arylzinc reagents to 3,4-dihydroisoquinoline N-oxide to yield chiral 1-aryl-THIQs. Our optimized conditions generated up to 99% enantiomeric excess and 99% isolated yield.
520 $a In another area of research, we have developed a new enzyme based high-throughput screening assay to measure the enantiomeric excess of allylic acetates. This assay accommodates reaction products that range in stereochemistry from 100% (S) to 100% (R), functions well with crude samples utilizing only mug quantities of analyte per sample. Using this enzymatic method we measured the enantiomeric excess of approximately 200 crude reaction products in one hour.
590 $a School code: 0024.
650 4 $a Chemistry, Biochemistry. $3 1017722
650 4 $a Chemistry, Organic. $3 516206
650 4 $a Chemistry, Pharmaceutical. $3 550957
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710 2 $a Brown University. $3 766761
773 0 $t Dissertation Abstracts International $g 69-06B.
790 $a 0024
791 $a Ph.D.
792 $a 2008
856 4 0 $u http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3319114