57699-89-5Relevant academic research and scientific papers
The first synthesis of 1,5-diazacyclooctan-2-one and differentially protected 1,5-diazacyclooctanes
Sherrill, Ronald G.
, p. 7053 - 7056 (2007)
An efficient, high-yielding synthesis of 1,5-diazacyclooctan-2-one and subsequent elaboration to a differentially protected 1,5-diazacyclooctane is disclosed.
Design, synthesis, and biological evaluation of stable β6.3-Helices: Discovery of non-hemolytic antibacterial peptides
Reddy, Damodara N.,Singh, Sukrit,Ho, Chris M.W.,Patel, Janki,Schlesinger, Paul,Rodgers, Stephen,Doctor, Allan,Marshall, Garland R.
supporting information, p. 193 - 210 (2018/03/06)
Gramicidin A, a topical antibiotic made from alternating L and D amino acids, is characterized by its wide central pore; upon insertion into membranes, it forms channels that disrupts ion gradients. We present helical peptidomimetics with this characteris
METHOD OF DRUG DESIGN AND OPTIMISATION UTILIZING STEREOCHEMICAL MIMICRY
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, (2017/12/09)
The invention relates to a method of designing or optimizing a drug candidate by making stereodynamic derivatives as well as novel derivatives of Glyx-13 with improved biological and pharmacological properties.
Mimicking a proline tripeptide with pyrazolidines and a cyclopentane linker
Vertesaljai, Peter,Lebedyeva, Iryna O.,Oliferenko, Alexander A.,Qi, Xin,Fu, Junjie,Ostrov, David A.,Asiri, Abdullah M.,Dennis Hall,Katritzky, Alan
, p. 6653 - 6655 (2016/01/28)
In this work the five-step assembly of a peptidomimetic structurally resembling Prolyl-Prolyl-Proline tripeptide is reported. Proline units are mimicked by two pyrazolidine rings connected to trans-1,2-cyclopentanedicarboxylic acid. The Pro-Pro-Pro mimetic resembles a tri-l-proline unit but with increased lipophilicity and structural constraints imposed by the linker.
Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
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, (2011/04/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
Peptidomimetic inhibitors of bacterial peptide deformylase
East, Stephen P.,Ayscough, Andrew,Toogood-Johnson, Ian,Taylor, Steven,Thomas, Wayne
scheme or table, p. 4032 - 4035 (2011/08/06)
A series of N-formyl hydroxylamine peptide deformylase inhibitors containing a cyclic azaamino acid moiety between the P1′ and P3′ substituents are presented. Selected compounds display antibacterial activity against pathogens associated with respiratory
Peptide analogues comprising at least one type of aminoacylaza-γ(b)3and the use thereof, in particular for therapy
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, (2011/04/14)
The object of the present invention is analogues of peptides or parent proteins, these peptide analogues, comprising at least one aza-β3 aminoacyl residue, and also their uses in pharmaceutical compositions or for the diagnosis of pathologies w
HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
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Page/Page column 115, (2010/08/18)
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
Development of cyclic hydrazine and hydrazide type organocatalyst-mechanistic aspects of cyclic hydrazine/hydrazide-catalyzed diels-alder reactions
Suzuki, Ichiro,Hirata, Ai,Takeda, Kei
scheme or table, p. 851 - 863 (2009/12/01)
Some hydrazines and hydrazides were prepared and screened for their catalytic efficiencies in Diels-Alder reactions. 1H-NMR studies and ab initio calculations revealed that catalytic efficiencies of these catalysts are greatly dependent on the release of the catalysts from the Diels-Alder adducts.
CHEMOKINE RECEPTOR MODULATORS
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Page/Page column 564, (2008/12/07)
The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I). These compounds are useful treating or preventing HIV infections, and in treating proliferative disorders such as inhibiting the metastasis of various cancers.
