Literature DB >> 24727489

Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE).

Young Taek Han1, Kyeojin Kim2, Gyeong-In Choi2, Hongchan An2, Dohyun Son3, Hee Kim4, Hee-Jin Ha4, Jun-Hyeng Son2, Suk-Jae Chung2, Hyun-Ju Park3, Jeewoo Lee2, Young-Ger Suh5.   

Abstract

In an effort to develop novel inhibitors of receptor for advanced glycation end products (RAGE) for the treatment of Alzheimer's disease, a series of pyrazole-5-carboxamides were designed, synthesized and biologically evaluated. Analyses of the extensive structure-activity relationship (SAR) led us to identify a 4-fluorophenoxy analog (40) that exhibited improved in vitro RAGE inhibitory activity and more favorable aqueous solubility than the parent 2-aminopyrimidine, 1. Surface plasmon resonance (SPR) and molecular docking study strongly supported the RAGE inhibitory activity of pyrazole-5-carboxamides. The brain Aβ-lowering effect of 40 is also described.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Alzheimer's disease, RAGE inhibitor; Pyrazole-5-carboxamide; RAGE (receptor for advanced glycation end products); SAR (structure–activity relationship)

Mesh：

Substances：

Year:  2014        PMID： 24727489     DOI： 10.1016/j.ejmech.2014.03.072

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  13 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

Review 2.  All the "RAGE" in lung disease: The receptor for advanced glycation endproducts (RAGE) is a major mediator of pulmonary inflammatory responses.

Authors:  Elizabeth A Oczypok; Timothy N Perkins; Tim D Oury
Journal:  Paediatr Respir Rev       Date:  2017-03-18       Impact factor: 2.726

Review 3.  Methylglyoxal and Its Adducts: Induction, Repair, and Association with Disease.

Authors:  Seigmund Wai Tsuen Lai; Edwin De Jesus Lopez Gonzalez; Tala Zoukari; Priscilla Ki; Sarah C Shuck
Journal:  Chem Res Toxicol       Date:  2022-10-05       Impact factor: 3.973

4.  Identification of pheophorbide a as an inhibitor of receptor for advanced glycation end products in Mallotus japonicus.

Authors:  Teruki Matsumoto; Michiyo Matsuno; Norihito Ikui; Yoshiyuki Mizushina; Yume Omiya; Rikako Ishibashi; Taro Ueda; Hajime Mizukami
Journal:  J Nat Med       Date:  2021-02-24       Impact factor: 2.343

5.  Synthesis and Evaluation of [(18)F]RAGER: A First Generation Small-Molecule PET Radioligand Targeting the Receptor for Advanced Glycation Endproducts.

Authors:  Brian P Cary; Allen F Brooks; Maria V Fawaz; Lindsey R Drake; Timothy J Desmond; Phillip Sherman; Carole A Quesada; Peter J H Scott
Journal:  ACS Chem Neurosci       Date:  2016-02-01       Impact factor: 4.418

6.  PET imaging study of brown adipose tissue (BAT) activity in mice devoid of receptor for advanced glycation end products (RAGE).

Authors:  Yu-Shin Ding; Noeen Malik; Sebastian Mendoza; Daniel Tuchman; Carmen Hurtado Del Pozo; Raquel Lopez Diez; Ann-Marie Schmidt
Journal:  J Biosci       Date:  2019-09       Impact factor: 1.826

Review 7.  Molecular Characteristics of RAGE and Advances in Small-Molecule Inhibitors.

Authors:  Hyeon Jin Kim; Mi Suk Jeong; Se Bok Jang
Journal:  Int J Mol Sci       Date:  2021-06-27       Impact factor: 5.923

8.  The receptor for advanced glycation end products (RAGE) enhances autophagy and neutrophil extracellular traps in pancreatic cancer.

Authors:  B A Boone; L Orlichenko; N E Schapiro; P Loughran; G C Gianfrate; J T Ellis; A D Singhi; R Kang; D Tang; M T Lotze; H J Zeh
Journal:  Cancer Gene Ther       Date:  2015-04-24       Impact factor: 5.987

9.  Virtual screening of RAGE inhibitors using molecular docking.

Authors:  Malini Devi Alaparthi; Gudipudi Gopinath; Srinivas Bandaru; Venu Sankeshi; Madhavi Mangalarapu; Swetha Sudha Nagamalla; Kota Sudhakar; Anupalli Roja Rani; Someswar Rao Sagurthi
Journal:  Bioinformation       Date:  2016-06-15

Review 10.  Advanced glycation end products (AGEs) and its receptor, RAGE, modulate age-dependent COVID-19 morbidity and mortality. A review and hypothesis.

Authors:  Durai Sellegounder; Parisa Zafari; Misagh Rajabinejad; Mahdi Taghadosi; Pankaj Kapahi
Journal:  Int Immunopharmacol       Date:  2021-05-24       Impact factor: 5.714
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