93448-34-1Relevant academic research and scientific papers
An Alternative Approach to the Hydrated Imidazoline Ring Expansion (HIRE) of Diarene-Fused [1.4]Oxazepines
Grintsevich, Sergey,Sapegin, Alexander,Reutskaya, Elena,Peintner, Stefan,Erdélyi, Máté,Krasavin, Mikhail
, p. 5664 - 5676 (2020/07/21)
A four-step approach to the “hydrated imidazoline ring expansion” (HIRE) is presented. In most cases, the ring expansion was the sole process. However, for the first time, an alternative course of the hydrated imidazoline evolution was discovered which gave N-aminoethyl derivatives. These can, in principle, be converted into the target HIRE products under sufficiently forcing conditions. The approach offers improved flexibility with respect to the peripheral substituents and is also applicable to the synthesis of eleven-membered lactams. We observed that the latter can exist in two stable isomeric forms due to lactam–amide bond isomerization. The latter finding further demonstrates the value of medium-sized rings as multiple-conformer probes for biological target interrogation.
Synthesis and antibacterial activity of aromatic and heteroaromatic amino alcohols
de Almeida, Camila G.,Reis, Samira G.,de Almeida, Angelina M.,Diniz, Claudio G.,da Silva, Vania L.,Le Hyaric, Mireille
experimental part, p. 876 - 880 (2012/06/18)
Two series of aromatic and heteroaromatic amino alcohols were synthesized from alcohols and aldehydes and evaluated for their antibacterial activities. All the octylated compounds displayed a better activity against the four bacteria tested when evaluated by the agar diffusion method and were selected for the evaluation of minimal inhibitory concentration. The best results were obtained for p-octyloxybenzyl derivatives against Staphylococcus epidermidis (minimal inhibitory concentrations = 32μm).
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARδ-selective agonists
Fujieda, Hiroki,Usui, Shinya,Suzuki, Takayoshi,Nakagawa, Hidehiko,Ogura, Michitaka,Makishima, Makoto,Miyata, Naoki
, p. 4351 - 4357 (2008/02/12)
To find novel PPARδ-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARδ agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARδ appropriately.
Propanoic acid derivatives that inhibit the binding of integrins to their receptors
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Page column 42-43, (2008/06/13)
A compound of the structure A method for the inhibition of the binding of α4β1integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which α4β1is involved are also disclosed.
Solution-phase parallel synthesis of substituted 1,2-ethyl and 1,3-propyl diamines
Dagan, Ido D.,Lowden, Christopher T.
, p. 7575 - 7577 (2007/10/03)
A solution-phase synthesis for the preparation of substituted 1,2-ethyl and 1,3-propyl diamines has been developed for the purpose of producing diverse lead generation libraries with a minimal scaffold. Crude products were obtained in high purity and further purified through mass guided preparative HPLC.
Propanoic acid derivatives that inhibit the binding of integrins to their receptors
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Page 31, (2008/06/13)
A method for the inhibition of the binding of α4β1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds (I) that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which α4β1 is involved. All substituents are as defined in the application.
