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D Cabel

Publications and source records attributed to D Cabel.

3 recordsLinked to original sources

Structurally homogeneous and heterogeneous synthetic combinatorial libraries.

We have designed and synthesized structurally homogeneous and heterogeneous nonpeptide libraries. Structurally homogeneous libraries are characterized by the presence of one common structural unit, a scaffold, in all library compounds (e.g. cyclopentane, cyclohexane, diketopiperazine, thiazolidine). In structurally heterogeneous libraries different organic reactions (acylation, etherification, reductive amination, nucleophilic displacement) were applied to connect bifunctional building blocks unrelated in structure (aromatic hydroxy acids, aromatic hydroxy aldehydes, amino alcohols, diamines, and amino acids). The focus of this communication is to document the use of bifunctional building blocks for the design and synthesis of structurally heterogeneous libraries of N-(alkoxy acyl)amino acids, N,N'-bis-(alkoxy acyl)diamino acids, N-acylamino ethers, N-(alkoxy acyl)amino alcohols, N-alkylamino ethers, and N-(alkoxy aryl)diamines.

Aldehydes↗

Linear presentation of variable side-chain spacing in a highly diverse combinatorial library.

A synthetic library that presents potential pharmacophores in a linear fashion with variable spacing was designed (alpha, beta, gamma-library). To prove the concept, we synthesized a number of individual compounds as well as a model library. Diamino acids connected by amide bonds via their alpha- or side-chain amino groups were used to form the backbone (scaffold) of this library. The remaining amino group of the diamino acids were acylated by a variety of carboxylic acids, generating an appreciable diversity of compounds in this library. The compositions of compounds in the library were identified by reading a peptide tag synthesized concurrently with the library structures. This code contained the information regarding the carboxylic acid coupled, and the diamino acid and amino group to which the acid was coupled.

Amino Acid Sequence↗

MARS--multiple automated robotic synthesizer for continuous flow of peptides.

We have designed and constructed a multiple automated robotic synthesizer, the MARS. Its novel timing procedure for handling multiple synthetic tasks eliminates unnecessary respite time by keeping the robotic arm in continuous operation. Polypropylene syringes equipped at the bottom with polypropylene frits serve as physically independent reaction vessels. All operations are performed by the robotic arm, which is equipped with a specially designed gripper to hold a syringe and to aspirate and dispense liquid. Typically, the MARS synthesizes concurrently 5 to 15 peptides of different length, and once one peptide is finished it automatically starts the synthesis of the next peptide in the queue, assuring a continuous flow of peptides.

Automation↗