“多样体”：一种实现非肽、非寡聚化学多样性的方法。
"Diversomers": an approach to nonpeptide, nonoligomeric chemical diversity.
作者信息
DeWitt S H, Kiely J S, Stankovic C J, Schroeder M C, Cody D M, Pavia M R
机构信息
Department of Chemistry, Warner-Lambert Co., Ann Arbor, MI 48106.
出版信息
Proc Natl Acad Sci U S A. 1993 Aug 1;90(15):6909-13. doi: 10.1073/pnas.90.15.6909.
Abstract
Solid-phase chemistry, organic synthesis, and an apparatus for multiple, simultaneous synthesis have been combined to generate libraries of organic compounds ("diversomers"). Arrays of compounds were synthesized over two to three steps incorporating chemically diverse building blocks on a polystyrene-based solid support in a multiple, simultaneous manner. The generality of this approach is illustrated by the syntheses of dipeptides, hydantoins, and benzodiazepines.
摘要
固相化学、有机合成以及一种用于多重同步合成的仪器已被结合起来，以生成有机化合物文库（“多样异构体”）。通过两到三步反应，以多重同步的方式在聚苯乙烯基固相载体上掺入化学性质各异的结构单元，合成了化合物阵列。二肽、乙内酰脲和苯二氮䓬的合成证明了这种方法的通用性。
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本文引用的文献
1
p-alkoxybenzyl alcohol resin and p-alkoxybenzyloxycarbonylhydrazide resin for solid phase synthesis of protected peptide fragments.用于固相合成保护肽片段的对烷氧基苄醇树脂和对烷氧基苄氧基羰基酰肼树脂
J Am Chem Soc. 1973 Feb 21;95(4):1328-33. doi: 10.1021/ja00785a602.
2
Examination of the secondary structure of proteins by deconvolved FTIR spectra.通过去卷积傅里叶变换红外光谱对蛋白质二级结构进行检测。
Biopolymers. 1986 Mar;25(3):469-87. doi: 10.1002/bip.360250307.
3
1-Azacycloalkyl-1,4-benzodiazepin-2-ones with antianxiety-antidepressant actions.具有抗焦虑和抗抑郁作用的1-氮杂环烷基-1,4-苯并二氮杂䓬-2-酮
J Med Chem. 1985 Jun;28(6):699-707. doi: 10.1021/jm00383a003.
4
Peptides on phage: a vast library of peptides for identifying ligands.噬菌体展示的肽：用于鉴定配体的庞大肽库。
Proc Natl Acad Sci U S A. 1990 Aug;87(16):6378-82. doi: 10.1073/pnas.87.16.6378.
5
Random peptide libraries: a source of specific protein binding molecules.随机肽文库：特异性蛋白质结合分子的来源。
Science. 1990 Jul 27;249(4967):404-6. doi: 10.1126/science.2143033.
6
Light-directed, spatially addressable parallel chemical synthesis.光导向、空间可寻址的平行化学合成。
Science. 1991 Feb 15;251(4995):767-73. doi: 10.1126/science.1990438.
7
Searching for peptide ligands with an epitope library.利用表位文库寻找肽配体。
Science. 1990 Jul 27;249(4967):386-90. doi: 10.1126/science.1696028.
8
Identification of highest-affinity ligands by affinity selection from equimolar peptide mixtures generated by robotic synthesis.通过对机器人合成产生的等摩尔肽混合物进行亲和选择来鉴定高亲和力配体。
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