European Journal of Medicinal Chemistry This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases
Eur J Med Chem. 2024 Apr 6;271:116386. doi: 10.1016/j.ejmech.2024.116386. Online ahead of print.ABSTRACTPhosphodiesterase (PDE) is a superfamily of enzymes that are responsible for the hydrolysis of two second messengers: cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). PDE inhibition promotes the gene transcription by activating cAMP-response element binding protein (CREB), initiating gene transcription of brain-derived neurotrophic factor (BDNF). The procedure exerts neuroprotective profile, and motor and cognitive improving efficacy. From this point of view, PDE inhibition will provide a ...
Source: European Journal of Medicinal Chemistry - April 13, 2024 Category: Chemistry Authors: Qi Li Qinghong Liao Shulei Qi He Huang Siyu He Weiping Lyu Jinxin Liang Huan Qin Zimeng Cheng Fan Yu Xue Dong Ziming Wang Lingfei Han Yantao Han Source Type: research

Quinoxaline derivatives: Recent discoveries and development strategies towards anticancer agents
Eur J Med Chem. 2024 Apr 7;271:116360. doi: 10.1016/j.ejmech.2024.116360. Online ahead of print.ABSTRACTCancer is a leading cause of death and a major health problem worldwide. While many effective anticancer agents are available, most drugs currently on the market are not specific, raising issues like the common side effects of chemotherapy. However, recent research hold promises for the development of more efficient and safer anticancer drugs. Quinoxaline and its derivatives are becoming recognized as a novel class of chemotherapeutic agents with activity against different tumors. The present review compiles and discusse...
Source: European Journal of Medicinal Chemistry - April 13, 2024 Category: Chemistry Authors: Vincent Montero Marc Montana Manon Carr é Patrice Vanelle Source Type: research

Research progress of fullerenes and their derivatives in the field of PDT
Eur J Med Chem. 2024 Apr 7;271:116398. doi: 10.1016/j.ejmech.2024.116398. Online ahead of print.ABSTRACTIn contemporary studies, the predominant utilization of C60 derivatives pertains to their role as photosensitizers or agents that scavenge free radicals. The intriguing coexistence of these divergent functionalities has prompted extensive investigation into water-soluble fullerenes. The photodynamic properties of these compounds find practical applications in DNA cleavage, antitumor interventions, and antibacterial endeavors. Consequently, photodynamic therapy is progressively emerging as a pivotal therapeutic modality w...
Source: European Journal of Medicinal Chemistry - April 13, 2024 Category: Chemistry Authors: Xue Bai Chungeng Dong Xinle Shao Faiz-Ur Rahman Huifang Hao Yongmin Zhang Source Type: research

Tetrazole derivatives in the management of neurological disorders: Recent advances on synthesis and pharmacological aspects
Eur J Med Chem. 2024 Apr 9;271:116388. doi: 10.1016/j.ejmech.2024.116388. Online ahead of print.ABSTRACTNeurological disorders are the leading cause of a large number of mortalities and morbidities. Nitrogen heterocyclic compounds have been pivotal in exhibiting wide array of therapeutic applications. Among them, tetrazole is a ubiquitous class of organic heterocyclic compounds that have attracted much attention because of its unique structural and chemical properties, and a wide range of pharmacological activities comprising anti-convulsant effect, antibiotic, anti-allergic, anti-hypertensive to name a few. Owing to signi...
Source: European Journal of Medicinal Chemistry - April 13, 2024 Category: Chemistry Authors: Shivangi Jaiswal Kanika Verma Jaya Dwivedi Swapnil Sharma Source Type: research

Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates
Eur J Med Chem. 2024 Apr 7;270:116392. doi: 10.1016/j.ejmech.2024.116392. Online ahead of print.ABSTRACTThe emergence of serious bacterial resistance towards clinical oxacins poses a considerable threat to global public health, necessitating the development of novel structural antibacterial agents. Seven types of novel indolylacryloyl-derived oxacins (IDOs) were designed and synthesized for the first time from commercial 3,4-difluoroaniline via an eight-step procedure. The synthesized compounds were characterized by modern spectroscopic techniques. All target molecules were evaluated for antimicrobial activities. Most of t...
Source: European Journal of Medicinal Chemistry - April 12, 2024 Category: Chemistry Authors: Yue-Gao Hu Narsaiah Battini Bo Fang Cheng-He Zhou Source Type: research

Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors
Eur J Med Chem. 2024 Apr 4;270:116375. doi: 10.1016/j.ejmech.2024.116375. Online ahead of print.ABSTRACTSpleen tyrosine kinase (Syk) is a key signal transduction mediator of the B cell receptor (BCR) signaling pathway. Abnormal BCR signaling plays a key role in initiation and development of B-cell-derived hematological malignancies, therefore, Syk represents a potential target for inhibiting the BCR signaling resulting in a therapeutic effect in these cancers. Herein, we describe a novel series of SYK inhibitors with 4-(3'-pyrazolyl)-2-amino-pyrimidine scaffold. Extensive study of structure-activity relationships led to th...
Source: European Journal of Medicinal Chemistry - April 11, 2024 Category: Chemistry Authors: Giovanni Cervi Roberto D'Alessio Simona Bindi Laura Buffa Alessia Burocchi Giulia Canevari Michele Modugno Ilaria Motto Grazia Saturno Paolo Orsini Source Type: research

Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors
Eur J Med Chem. 2024 Apr 5;270:116390. doi: 10.1016/j.ejmech.2024.116390. Online ahead of print.ABSTRACTProtein tyrosine phosphatases PTPN2 and PTPN1 (also known as PTP1B) have been implicated in a number of intracellular signaling pathways of immune cells. The inhibition of PTPN2 and PTPN1 has emerged as an attractive approach to sensitize T cell anti-tumor immunity. Two small molecule inhibitors have been entered the clinic. Here we report the design and development of compound 4, a novel small molecule PTPN2/N1 inhibitor demonstrating nanomolar inhibitory potency, good in vivo oral bioavailability, and robust in vivo an...
Source: European Journal of Medicinal Chemistry - April 11, 2024 Category: Chemistry Authors: Jiamin Zheng Zhisen Zhang Xiaoyu Ding Deheng Sun Lihua Min Feng Wang Sujing Shi Xin Cai Man Zhang Alex Aliper Feng Ren Xiao Ding Alex Zhavoronkov Source Type: research

Discovery of novel Thymol-TPP antibiotics that eradicate MRSA persisters
Eur J Med Chem. 2024 Apr 3;270:116381. doi: 10.1016/j.ejmech.2024.116381. Online ahead of print.ABSTRACTThe high prevalence of methicillin-resistant Staphylococcus aureus (MRSA) strains and the formation of non-growing, dormant "persisters" subsets help bacteria evade antibiotic treatment and enhance bacterial resistance, which poses a serious threat to human life and health. It is urgent to discover novel antibacterial therapies effective against MRSA persisters. Thymol is a common nutraceutical with weak antibacterial and antitumor activities. A series of Thymol triphenylphosphine (TPP) conjugates (TPP-Thy3) was designed...
Source: European Journal of Medicinal Chemistry - April 11, 2024 Category: Chemistry Authors: Ziyi Tang Jizhou Feng Mahesh Challa Sankara Rao Rowthu Shuxin Xiong Cheng Zou Jianguo Li Chandra Shekhar Verma Haibo Peng Xiaoli He Chao Huang Yun He Source Type: research

Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents
Eur J Med Chem. 2024 Apr 2;270:116378. doi: 10.1016/j.ejmech.2024.116378. Online ahead of print.ABSTRACTInfections caused by Staphylococcus aureus (S. aureus) are increasing difficult to treat because this pathogen is easily resistant to antibiotics. However, the development of novel antibacterial agents with high antimicrobial activity and low frequency of resistance remains a huge challenge. Here, building on the coupling strategy, an adamantane moiety was linked to the membrane-active Ru-based structure and then developed three novel metalloantibiotics: [Ru(bpy)2(L)](PF6)2 (Ru1) (bpy = 2,2-bipyridine, L = amantadine mod...
Source: European Journal of Medicinal Chemistry - April 11, 2024 Category: Chemistry Authors: Liqiang Wang Lianghong Liu Chunyan Zhang Guangying Yu Wenjing Lin Xuemin Duan Yanshi Xiong Guijuan Jiang Jintao Wang Xiangwen Liao Source Type: research

Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer
Eur J Med Chem. 2024 Mar 29;270:116363. doi: 10.1016/j.ejmech.2024.116363. Online ahead of print.ABSTRACTOvercoming multidrug resistance (MDR) is one of the major challenges in cancer therapy. In this respect, Schiff base-related compounds (bearing a R1R2CNR3 bond) gained high interest during the past decades. Schiff bases are considered privileged ligands for various reasons, including the easiness of their preparation and the possibility to form complexes with almost all transition metal ions. Schiff bases and their metal complexes exhibit many types of biological activities and are used for the treatment and diagnosis o...
Source: European Journal of Medicinal Chemistry - April 9, 2024 Category: Chemistry Authors: Ana Podolski-Reni ć Ana Čipak Gašparović Andreia Valente Óscar López Julia H Bormio Nunes Christian R Kowol Petra Heffeter Nenad R Filipovi ć Source Type: research