60857-16-1Relevant academic research and scientific papers
The human immunodeficiency virus-reverse transcriptase inhibition activity of novel pyridine/pyridinium-type fullerene derivatives
Yasuno, Takumi,Ohe, Tomoyuki,Takahashi, Kyoko,Nakamura, Shigeo,Mashino, Tadahiko
, p. 3226 - 3229 (2015)
Abstract In the present study, we describe the synthesis of a novel set of pyridine/pyridinium-type fullerene derivatives. The products were assessed for human immunodeficiency virus-reverse transcriptase inhibition activities. All novel fullerene derivat
Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease
Yasuno, Takumi,Ohe, Tomoyuki,Kataoka, Hiroki,Hashimoto, Kosho,Ishikawa, Yumiko,Furukawa, Keigo,Tateishi, Yasuhiro,Kobayashi, Toi,Takahashi, Kyoko,Nakamura, Shigeo,Mashino, Tadahiko
supporting information, (2020/11/20)
In the present study, we newly synthesized three types of novel fullerene derivatives: pyridinium-type derivatives trans-3a and 4a-5b, piperidinium-type derivative 9, and proline-type derivatives 10a-12. Among the assessed compounds, 5a, 10e, 10f, 10i, 11
Selective Functionalization of Aliphatic Amines via Myoglobin-Catalyzed Carbene N-H Insertion
Fasan, Rudi,Sreenilayam, Gopeekrishnan,Steck, Viktoria
, p. 224 - 229 (2020/02/15)
Engineered myoglobins have recently gained attention for their ability to catalyze a variety of abiological carbene transfer reactions including the functionalization of amines via carbene insertion into N-H bonds. However, the scope of myoglobin and other hemoprotein-based biocatalysts in the context of this transformation has been largely limited to aniline derivatives as the amine substrates and ethyl diazoacetate as the carbene donor reagent. In this report, we describe the development of an engineered myoglobin-based catalyst that is useful for promoting carbene N-H insertion reactions across a broad range of substituted benzylamines and α-diazo acetates with high efficiency (82-99percent conversion), elevated catalytic turnovers (up to 7,000), and excellent chemoselectivity for the desired single insertion product (up to 99percent). The scope of this transformation could be extended to cyclic aliphatic amines. These studies expand the biocatalytic toolbox available for the selective formation of C-N bonds, which are ubiquitous in many natural and synthetic bioactive compounds.
COMPOUND USED AS AUTOPHAGY REGULATOR, AND PREPARATION METHOD THEREFOR AND USES THEREOF
-
Paragraph 0328-0329, (2020/07/07)
It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.
Discovery of disubstituted xylylene derivatives as small molecule direct inhibitors of Keap1-Nrf2 protein-protein interaction
Abed, Dhulfiqar Ali,Hu, Longqin,Lee, Sumi
, (2020/02/13)
The Keap1–Nrf2–ARE system represents a crucial antioxidant defense mechanism that protects cells against reactive oxygen species. Targeting Keap1–Nrf2 protein–protein interaction (PPI) has become a promising drug target for several oxidative stress-relate
Synthesis of a leopolic acid-inspired tetramic acid with antimicrobial activity against multidrug-resistant bacteria
Mattio, Luce,Musso, Loana,Scaglioni, Leonardo,Pinto, Andrea,Martino, Piera Anna,Dallavalle, Sabrina
, p. 2482 - 2487 (2018/10/04)
The increasing emergence of multidrug-resistant pathogens is one of the biggest threats to human health and food security. The discovery of new antibacterials, and in particular the finding of new scaffolds, is an imperative goal to stay ahead of the evolution of antibiotic resistance. Herein we report the synthesis of a 3-decyltetramic acid analogue of the ureido dipeptide natural antibiotic leopolic acid A. The key step in the synthetic strategy is an intramolecular Lacey-Dieckmann cyclization reaction of a linear precursor to obtain the desired 3-alkyl-substituted tetramic acid core. The synthesized analogue is more effective than the parent leopolic acid A against Gram-positive (Staphylococcus pseudintermedius) and Gram-negative (E. coli) bacteria (MIC 8 μg/mL and 64 μg/mL, respectively). Interestingly, the compound shows a significant activity against Staphylococcus pseudintermedius strains expressing a multidrug-resistant phenotype (average MIC 32 μg/mL on 30 strains tested). These results suggest that this molecule can be considered a promising starting point for the development of a novel class of antibacterial agents active also against resistant strains.
SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
-
Page/Page column 249, (2019/01/05)
Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
Cs2CO3-Promoted Direct N-Alkylation: Highly Chemoselective Synthesis of N-Alkylated Benzylamines and Anilines
Castillo, Juan-Carlos,Orrego-Hernández, Jessica,Portilla, Jaime
, p. 3824 - 3835 (2016/08/20)
Herein is described an efficient and chemoselective method for the synthesis of diversely substituted secondary amines in yields up to 98 %. Direct mono-N-alkylation of primary benzylamines and anilines with a wide range of alkyl halides is promoted by a cesium base in the absence of any additive or catalyst. The basicity and solubility of cesium carbonate in anhydrous N,N-dimethylformamide not only enables mono-N-alkylation of primary amines but also suppresses undesired dialkylation of the desired amines.
Microwave-assisted synthesis of 2,5-piperazinediones under solvent-free conditions
Lopez-Cobenas, Alberto,Cledera, Pilar,Sanchez, J. Domingo,Lopez-Alvarado, Pilar,Ramos, M. Teresa,Avendano, Carmen,Menendez, J. Carlos
, p. 3412 - 3422 (2007/10/03)
A general, efficient and environmentally friendly procedure for the synthesis of 2,5-piperazinediones is described, involving the microwave irradiation of N-Boc dipeptide esters. Georg Thieme Verlag Stuttgart.
Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
-
Page/Page column 4, (2008/06/13)
The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a phys
