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ACS Medicinal Chemistry Letters最新文献

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The Relaxin Family Peptide Receptor 1 (RXFP1) Agonists as Potential Treatment for Heart Failure 松弛素家族肽受体1 （RXFP1）激动剂作为心力衰竭的潜在治疗方法
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-23 DOI: 10.1021/acsmedchemlett.5c0027310.1021/acsmedchemlett.5c00273
Ahmed F. Abdel-Magid*, 
{"title":"The Relaxin Family Peptide Receptor 1 (RXFP1) Agonists as Potential Treatment for Heart Failure","authors":"Ahmed F. Abdel-Magid*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0027310.1021/acsmedchemlett.5c00273","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00273https://doi.org/10.1021/acsmedchemlett.5c00273","url":null,"abstract":"<p >The invention in this patent application relates to bicyclo[2.2.1]heptane derivatives represented herein by formula 1. The compounds of formula 1 are relaxin family peptide receptor 1 (RXFP1) agonists and may provide treatments for heart failure, fibrotic diseases, and related diseases such as lung, kidney, and hepatic diseases.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"955–958 955–958"},"PeriodicalIF":3.5,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144261147","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The Relaxin Family Peptide Receptor 1 (RXFP1) Agonists as Potential Treatment for Heart Failure. 松弛素家族肽受体1 （RXFP1）激动剂作为心力衰竭的潜在治疗方法。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-23 eCollection Date: 2025-06-12 DOI: 10.1021/acsmedchemlett.5c00273
Ahmed F Abdel-Magid
{"title":"The Relaxin Family Peptide Receptor 1 (RXFP1) Agonists as Potential Treatment for Heart Failure.","authors":"Ahmed F Abdel-Magid","doi":"10.1021/acsmedchemlett.5c00273","DOIUrl":"10.1021/acsmedchemlett.5c00273","url":null,"abstract":"<p><p>The invention in this patent application relates to bicyclo[2.2.1]-heptane derivatives represented herein by formula 1. The compounds of formula 1 are relaxin family peptide receptor 1 (RXFP1) agonists and may provide treatments for heart failure, fibrotic diseases, and related diseases such as lung, kidney, and hepatic diseases.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"955-958"},"PeriodicalIF":3.5,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12169483/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144315467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Desamide Isotryptamine Tetracycles as 5‑HT2C Agonists for Treating Brain Disorders. 新型去酰胺异色胺四环素作为5‑HT2C激动剂治疗脑部疾病。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 eCollection Date: 2025-06-12 DOI: 10.1021/acsmedchemlett.5c00286
Ram W Sabnis
{"title":"Novel Desamide Isotryptamine Tetracycles as 5‑HT2C Agonists for Treating Brain Disorders.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00286","DOIUrl":"10.1021/acsmedchemlett.5c00286","url":null,"abstract":"<p><p>Provided herein are novel desamide isotryptamine tetracycles as 5-HT2C agonists, pharmaceutical compositions, use of such compounds in treating brain disorders, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"976-977"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12169470/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144315529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Application of Free Energy Perturbation (FEP) Methodology for Predicting the Binding Affinity of Macrocyclic JAK2 Inhibitor Analogues of Pacritinib. 应用自由能摄动（FEP）方法预测Pacritinib大环JAK2抑制剂类似物的结合亲和力。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 eCollection Date: 2025-06-12 DOI: 10.1021/acsmedchemlett.5c00105
Natércia F Braz, Martin J Slater, Stuart Lang
{"title":"Application of Free Energy Perturbation (FEP) Methodology for Predicting the Binding Affinity of Macrocyclic JAK2 Inhibitor Analogues of Pacritinib.","authors":"Natércia F Braz, Martin J Slater, Stuart Lang","doi":"10.1021/acsmedchemlett.5c00105","DOIUrl":"10.1021/acsmedchemlett.5c00105","url":null,"abstract":"<p><p>Pacritinib, an orally bioavailable macrocyclic inhibitor of Janus Kinase 2, has shown efficacy for the treatment of myelofibrosis. Due to the synthetic challenges associated with synthesizing macrocyclic analogues, we applied electrostatic complementarity, 3D-field QSAR, and free energy perturbation methods for the profiling of a set of known ligands with a view to developing a prioritization method for selecting new macrocyclic designs for synthesis. The importance of understanding the 3D conformation and flexibility of a ligand is demonstrated, with these effects having a significant implication on the accuracy of predictions.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"1066-1072"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12169459/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144315509","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Application of Free Energy Perturbation (FEP) Methodology for Predicting the Binding Affinity of Macrocyclic JAK2 Inhibitor Analogues of Pacritinib 应用自由能摄动（FEP）方法预测Pacritinib大环JAK2抑制剂类似物的结合亲和力
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 DOI: 10.1021/acsmedchemlett.5c0010510.1021/acsmedchemlett.5c00105
Natércia F. Braz, Martin J. Slater and Stuart Lang*, 
{"title":"Application of Free Energy Perturbation (FEP) Methodology for Predicting the Binding Affinity of Macrocyclic JAK2 Inhibitor Analogues of Pacritinib","authors":"Natércia F. Braz,&nbsp;Martin J. Slater and Stuart Lang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0010510.1021/acsmedchemlett.5c00105","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00105https://doi.org/10.1021/acsmedchemlett.5c00105","url":null,"abstract":"<p >Pacritinib, an orally bioavailable macrocyclic inhibitor of Janus Kinase 2, has shown efficacy for the treatment of myelofibrosis. Due to the synthetic challenges associated with synthesizing macrocyclic analogues, we applied electrostatic complementarity, 3D-field QSAR, and free energy perturbation methods for the profiling of a set of known ligands with a view to developing a prioritization method for selecting new macrocyclic designs for synthesis. The importance of understanding the 3D conformation and flexibility of a ligand is demonstrated, with these effects having a significant implication on the accuracy of predictions.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"1066–1072 1066–1072"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/epdf/10.1021/acsmedchemlett.5c00105","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144260899","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Ergolines as 5-HT2A Agonists for Treating Mood Disorders 新型麦角碱作为5-HT2A激动剂治疗心境障碍
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 DOI: 10.1021/acsmedchemlett.5c0028810.1021/acsmedchemlett.5c00288
Ram W. Sabnis*, 
{"title":"Novel Ergolines as 5-HT2A Agonists for Treating Mood Disorders","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0028810.1021/acsmedchemlett.5c00288","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00288https://doi.org/10.1021/acsmedchemlett.5c00288","url":null,"abstract":"<p >Provided herein are novel ergolines as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating mood disorders, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"974–975 974–975"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144260895","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Tricyclic Compounds for Treating Bacterial Infections 治疗细菌感染的新型三环化合物
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 DOI: 10.1021/acsmedchemlett.5c0028910.1021/acsmedchemlett.5c00289
Ram W. Sabnis*, 
{"title":"Novel Tricyclic Compounds for Treating Bacterial Infections","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0028910.1021/acsmedchemlett.5c00289","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00289https://doi.org/10.1021/acsmedchemlett.5c00289","url":null,"abstract":"<p >Provided herein are novel tricyclic compounds, pharmaceutical compositions, use of such compounds in treating bacterial infections, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"972–973 972–973"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144260898","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Desamide Isotryptamine Tetracycles as 5-HT2C Agonists for Treating Brain Disorders 新型去酰胺异色胺四环作为5-HT2C激动剂治疗脑部疾病
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 DOI: 10.1021/acsmedchemlett.5c0028610.1021/acsmedchemlett.5c00286
Ram W. Sabnis*, 
{"title":"Novel Desamide Isotryptamine Tetracycles as 5-HT2C Agonists for Treating Brain Disorders","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0028610.1021/acsmedchemlett.5c00286","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00286https://doi.org/10.1021/acsmedchemlett.5c00286","url":null,"abstract":"<p >Provided herein are novel desamide isotryptamine tetracycles as 5-HT2C agonists, pharmaceutical compositions, use of such compounds in treating brain disorders, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"976–977 976–977"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144261125","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Tricyclic Compounds for Treating Bacterial Infections. 治疗细菌感染的新型三环化合物。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 eCollection Date: 2025-06-12 DOI: 10.1021/acsmedchemlett.5c00289
Ram W Sabnis
{"title":"Novel Tricyclic Compounds for Treating Bacterial Infections.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00289","DOIUrl":"10.1021/acsmedchemlett.5c00289","url":null,"abstract":"<p><p>Provided herein are novel tricyclic compounds, pharmaceutical compositions, use of such compounds in treating bacterial infections, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"972-973"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12169469/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144315540","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of Highly Selective Aldosterone Synthase Inhibitors. 高选择性醛固酮合成酶抑制剂的研究进展。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-05-21 eCollection Date: 2025-06-12 DOI: 10.1021/acsmedchemlett.5c00222
Guangyuan Shen, Zimo Yang, Yue Lv, Huisi Liu, Xiaopian Tian, Xiangyu Jia, Yuanfeng Xia, Siqin Wang, Lei Jin, Zhilong Hu, Fanglong Yang
{"title":"Development of Highly Selective Aldosterone Synthase Inhibitors.","authors":"Guangyuan Shen, Zimo Yang, Yue Lv, Huisi Liu, Xiaopian Tian, Xiangyu Jia, Yuanfeng Xia, Siqin Wang, Lei Jin, Zhilong Hu, Fanglong Yang","doi":"10.1021/acsmedchemlett.5c00222","DOIUrl":"10.1021/acsmedchemlett.5c00222","url":null,"abstract":"<p><p>Recent clinical studies have heralded aldosterone synthase inhibitors (ASIs) as a promising therapeutic option for managing resistant hypertension. The efficacy of these compounds is believed to stem from their ability to mitigate aldosterone production. Consequently, we delved into the potential of aldosterone synthase inhibition as a therapeutic strategy for patients with refractory hypertension. Our focus is on the synthesis and optimization of innovative heterocyclic compounds that exhibit aldosterone synthase inhibitory activity. The CYP11B2 inhibitor we have developed exhibits an encouraging pharmacokinetic (PK) profile, along with a robust pharmacokinetic-pharmacodynamic (PK-PD) relationship. This has enabled us to meticulously evaluate the trends in aldosterone inhibition and assess the compound's efficacy in vivo using nonhuman primate models.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 6","pages":"1175-1181"},"PeriodicalIF":3.5,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12169458/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144315514","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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