scholarly journals Facile synthesis of 7-alkyl-1,2,3,4-tetrahydro-1,8-naphthyridines as arginine mimetics using a Horner–Wadsworth–Emmons-based approach

2020 ◽  
Vol 16 ◽  
pp. 1617-1626 ◽  
Author(s):  
Rhys A Lippa ◽  
John A Murphy ◽  
Tim N Barrett
Keyword(s):  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Protecting Group ◽  
Facile Synthesis ◽  
Arginine Mimetics ◽  
Synthetic Sequence ◽  
High Yields ◽  
Potential Therapeutics

Integrin inhibitors based on the tripeptide sequence Arg–Gly–Asp (RGD) are potential therapeutics for the treatment of idiopathic pulmonary fibrosis (IPF). Herein, we describe an expeditious three-step synthetic sequence of Horner–Wadsworth–Emmons olefination, diimide reduction, and global deprotection to synthesise cores for these compounds in high yields (63–83% over 3 steps) with no need for chromatography. Key to this transformation is the phosphoramidate protecting group, which is stable to metalation steps.

scholarly journals Facile Synthesis of 7-Alkyl-1,2,3,4-tetrahydro-[1,8]-naphthyridines as Arginine Mimetics Using a Horner–Wadsworth–Emmons Based Approach

2020 ◽  
Author(s):  
Rhys A Lippa ◽  
John A Murphy ◽  
Tim Barrett
Keyword(s):  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Protecting Group ◽  
Facile Synthesis ◽  
Arginine Mimetics ◽  
Synthetic Sequence ◽  
High Yields ◽  
Potential Therapeutics

Integrin inhibitors based on the tripeptide sequence Arg-Gly-Asp (RGD) are potential therapeutics for the treatment of idiopathic pulmonary fibrosis (IPF). Herein, we describe an expeditious three-step synthetic sequence of Horner–Wadsworth–Emmons olefination, diimide reduction and global deprotection to synthesise cores for these compounds in high yields (63–83% over 3 steps) with no need for chromatography. Key to this transformation is the phosphoramidate protecting group, which is stable to metalation steps.

Active Components from Traditional Herbal Medicine for the Potential Therapeutics of Idiopathic Pulmonary Fibrosis: A Systemic Review

2021 ◽  
pp. 1-22
Author(s):  
Ebuka-Olisaemeka Nwafor ◽  
Peng Lu ◽  
Yiting Liu ◽  
Hui Peng ◽  
Huan Qin ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Adverse Reactions ◽  
Analytical Data ◽  
Systemic Review ◽  
Active Components ◽  
Traditional Herbal Medicine ◽  
Potential Therapeutics

Idiopathic pulmonary fibrosis (IPF), a tumor-like disease, is a serious and fatal pulmonary inflammatory condition usually characterized by irreversible destruction of the lung parenchyma, excessive matrix accumulation, and decline in lung function. IPF still remains a great burden to the universe. At the moment, the available therapeutic regimens utilized for IPF such as non-pharmacological therapies (lung transplantation) and pharmacological therapies (drugs, nintedanib, pirfenidone, etc.) are normally accompanied by significant limitations, such as adverse reactions, low bioavailability, poor selectivity, low-tissue distribution, in vivo instability, systemic toxicity, inconveniency and unsafe usage. There is a need for the exploration and discovery of new novel remedies by researchers and scientists globally. Recent numerous preliminary studies have laid significant emphasis and demonstrated the antifibrotic importance, good curative actions (little or no adverse reactions), and multiple target sites of the active components from traditional herbal medicine (THM) against IPF, which could serve as a modern, alternative and potential therapeutics or drug candidates in treating IPF. This paper extensively summarizes the pharmacological actions and signaling pathways or mechanisms of active components obtained from THM for treating IPF. Moreover, the sources and modernization, markets, relevant FDA and CFDA studies (the USA and China), preclinical analysis, and various compositions of THM currently under clinical trials are also highlighted. Additionally, this present analytical data would be instrumental towards further drug progression or advancement of active components from THM for the potential therapeutics of IPF in the future.

scholarly journals Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis

2017 ◽  
Vol 8 (11) ◽  
pp. 1142-1147 ◽  
Author(s):  
Zhenhua Huang ◽  
Heran Li ◽  
Qian Zhang ◽  
Fangzheng Lu ◽  
Mei Hong ◽  
...  
Keyword(s):  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Multikinase Inhibitors ◽  
Potential Therapeutics

scholarly journals Fatty Acid Metabolism and Idiopathic Pulmonary Fibrosis

2022 ◽  
Vol 12 ◽  
Author(s):  
Jing Geng ◽  
Yuan Liu ◽  
Huaping Dai ◽  
Chen Wang
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Fatty Acid Metabolism ◽  
Metabolic Pathway ◽  
Acid Metabolism ◽  
De Novo ◽  
Lung Cells ◽  
Potential Therapeutics

Fatty acid metabolism, including the de novo synthesis, uptake, oxidation, and derivation of fatty acids, plays several important roles at cellular and organ levels. Recent studies have identified characteristic changes in fatty acid metabolism in idiopathic pulmonary fibrosis (IPF) lungs, which implicates its dysregulation in the pathogenesis of this disorder. Here, we review the evidence for how fatty acid metabolism contributes to the development of pulmonary fibrosis, focusing on the profibrotic processes associated with specific types of lung cells, including epithelial cells, macrophages, and fibroblasts. We also summarize the potential therapeutics that target this metabolic pathway in treating IPF.

Role of Wnt/PCP pathway on bronchial cell function in Idiopathic Pulmonary Fibrosis

Pneumologie ◽  
2011 ◽  
Vol 65 (12) ◽  
Author(s):  
S Barkha ◽  
M Gegg ◽  
H Lickert ◽  
M Königshoff
Keyword(s):  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Cell Function

Regulation of Macroautophagy in Idiopathic Pulmonary Fibrosis

Pneumologie ◽  
2012 ◽  
Vol 66 (06) ◽  
Author(s):  
P Mahavadi ◽  
S Ahuja ◽  
I Henneke ◽  
W Klepetko ◽  
C Ruppert ◽  
...  
Keyword(s):  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis

Role of Bcl-xL in hepatocyte growth factor-elicited epithelial protection in idiopathic pulmonary fibrosis

Pneumologie ◽  
2014 ◽  
Vol 68 (06) ◽  
Author(s):  
S Skwarna ◽  
I Henneke ◽  
W Seeger ◽  
T Geiser ◽  
A Günther ◽  
...  
Keyword(s):  
Growth Factor ◽  
Idiopathic Pulmonary Fibrosis ◽  
Pulmonary Fibrosis ◽  
Hepatocyte Growth Factor ◽  
Hepatocyte Growth
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