Useful scaffolds and handles for creating diversity in the preparation of chemical libraries

Miriam Royo; Montserrat Del Fresno; Ariadna Frieden; Wim Van Den Nest; Marina Sanseverino; Jordi Alsina; Steven A. Kates; George Barany; Fernando Albericio

doi:10.1016/S1381-5148(99)00015-2

Useful scaffolds and handles for creating diversity in the preparation of chemical libraries

Miriam Royo, Montserrat Del Fresno, Ariadna Frieden, Wim Van Den Nest, Marina Sanseverino, Jordi Alsina, Steven A. Kates, George Barany, Fernando Albericio

Chemistry (Twin Cities)

Research output: Contribution to journal › Conference article › peer-review

11 Scopus citations

Abstract

Several scaffolds having two reactive points and anchored to a solid support were prepared. These structures can display a wide range of pendant functionalities to give libraries of structurally diverse substances which can be used to search for new lead compounds and to achieve their subsequent optimization in a medicinal chemistry program. The scaffolds are based upon diketopiperazine-, cis-aminoproline-, hydrazine-, and alkylenediamine-resins, which contain in all cases two amino functions blocked selectively with orthogonally removable protecting groups.

Original language	English (US)
Pages (from-to)	103-110
Number of pages	8
Journal	Reactive and Functional Polymers
Volume	41
Issue number	1
DOIs	https://doi.org/10.1016/S1381-5148(99)00015-2
State	Published - Jul 15 1999
Event	Proceedings of the 1998 8th International Conference on Polymer-Based Technology (POC '98) - Ma'ale Hachamisha, Isr Duration: Jun 29 1998 → Jul 2 1998

Bibliographical note

Funding Information:
Research at Barcelona was supported by CICYT (PB96-1490) and Generalitat de Catalunya [Grup Consolidat (1995SGR 494) i Centre de Referència en Biotecnologia] and at Minnesota by the National Institutes of Health (Grant GM 42722). We are grateful to the Conde de Barcelona Foundation, Spain, for a fellowship to J.A., and to the University of Barcelona for a predoctoral fellowship to M.d.F.

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abstract = "Several scaffolds having two reactive points and anchored to a solid support were prepared. These structures can display a wide range of pendant functionalities to give libraries of structurally diverse substances which can be used to search for new lead compounds and to achieve their subsequent optimization in a medicinal chemistry program. The scaffolds are based upon diketopiperazine-, cis-aminoproline-, hydrazine-, and alkylenediamine-resins, which contain in all cases two amino functions blocked selectively with orthogonally removable protecting groups.",

author = "Miriam Royo and {Del Fresno}, Montserrat and Ariadna Frieden and {Van Den Nest}, Wim and Marina Sanseverino and Jordi Alsina and Kates, {Steven A.} and George Barany and Fernando Albericio",

note = "Funding Information: Research at Barcelona was supported by CICYT (PB96-1490) and Generalitat de Catalunya [Grup Consolidat (1995SGR 494) i Centre de Refer{\`e}ncia en Biotecnologia] and at Minnesota by the National Institutes of Health (Grant GM 42722). We are grateful to the Conde de Barcelona Foundation, Spain, for a fellowship to J.A., and to the University of Barcelona for a predoctoral fellowship to M.d.F.; Proceedings of the 1998 8th International Conference on Polymer-Based Technology (POC '98) ; Conference date: 29-06-1998 Through 02-07-1998",

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AU - Royo, Miriam

AU - Del Fresno, Montserrat

AU - Frieden, Ariadna

AU - Van Den Nest, Wim

AU - Sanseverino, Marina

AU - Alsina, Jordi

AU - Kates, Steven A.

AU - Barany, George

AU - Albericio, Fernando

N1 - Funding Information: Research at Barcelona was supported by CICYT (PB96-1490) and Generalitat de Catalunya [Grup Consolidat (1995SGR 494) i Centre de Referència en Biotecnologia] and at Minnesota by the National Institutes of Health (Grant GM 42722). We are grateful to the Conde de Barcelona Foundation, Spain, for a fellowship to J.A., and to the University of Barcelona for a predoctoral fellowship to M.d.F.

PY - 1999/7/15

Y1 - 1999/7/15

N2 - Several scaffolds having two reactive points and anchored to a solid support were prepared. These structures can display a wide range of pendant functionalities to give libraries of structurally diverse substances which can be used to search for new lead compounds and to achieve their subsequent optimization in a medicinal chemistry program. The scaffolds are based upon diketopiperazine-, cis-aminoproline-, hydrazine-, and alkylenediamine-resins, which contain in all cases two amino functions blocked selectively with orthogonally removable protecting groups.

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Useful scaffolds and handles for creating diversity in the preparation of chemical libraries

Abstract

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