ACS Medicinal Chemistry Letters最新文献_第9页

Discovery of a Phosphodiesterase 7A Inhibitor of High Isozyme Selectivity Exhibiting In Vivo Anti-Osteoporotic Effects

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-26 DOI: 10.1021/acsmedchemlett.4c0057010.1021/acsmedchemlett.4c00570

Kentaro Kondo, Kazuki Otake, Tetsudo Kaya, Shohei Miwa, Yoshifumi Ueyama, Tsunemitsu Haruta, Jun Nishihata, Takashi Nakagawa, Nobuhide Azuma, Kayoko Takagi, Toshiki Urashima, Yuki Kitao and Makoto Shiozaki*,

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引用次数: 0

Tetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition. 四唑是一种抑制碳酸酐酶的新型锌结合剂化学型。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-25 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00562

Simone Giovannuzzi, Andrea Angeli, Paloma Begines, Marta Ferraroni, Alessio Nocentini, Claudiu T Supuran

引用次数: 0

Tetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-25 DOI: 10.1021/acsmedchemlett.4c0056210.1021/acsmedchemlett.4c00562

Simone Giovannuzzi*, Andrea Angeli, Paloma Begines, Marta Ferraroni, Alessio Nocentini and Claudiu T. Supuran*,

引用次数: 0

Expanding the Chemical Space of Reverse Fosmidomycin Analogs. 拓展反向磷霉素类似物的化学空间。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-23 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00501

Talea Knak, Sana Takada, Boris Illarionov, Violetta Krisilia, Lais Pessanha de Carvalho, Beate Lungerich, Yasumitsu Sakamoto, Stefan Höfmann, Adelbert Bacher, Rainer Kalscheuer, Jana Held, Markus Fischer, Nobutada Tanaka, Thomas Kurz

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引用次数: 0

N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-23 DOI: 10.1021/acsmedchemlett.4c0049110.1021/acsmedchemlett.4c00491

Bharti Rajesh Kumar Shyamlal, Amol T. Mahajan, Vikash Kumar, Aarohi Gupta, Rishabh Shrivastava Ronin, Manas Mathur, Janmejaya Sen and Sandeep Chaudhary*,

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引用次数: 0

Discovery of a Potent Triazole-Based Reversible Targeted Covalent Inhibitor of Cruzipain. 一种有效的三唑基可逆性靶向共价克鲁铂抑制剂的发现。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-23 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00460

Juan Pablo Cerutti, Lucas Abreu Diniz, Viviane Corrêa Santos, Salomé Catalina Vilchez Larrea, Guillermo Daniel Alonso, Rafaela Salgado Ferreira, Mario Alfredo Quevedo, Wim Dehaen

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引用次数: 0

N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents. n -芳基磺酰化c -同源阿啡作为一类新的抗血小板和抗菌药物。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-23 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00491

Bharti Rajesh Kumar Shyamlal, Amol T Mahajan, Vikash Kumar, Aarohi Gupta, Rishabh Shrivastava Ronin, Manas Mathur, Janmejaya Sen, Sandeep Chaudhary

{"title":"N-Arylsulfonylated C-Homoaporphines as a New Class of Antiplatelet and Antimicrobial Agents.","authors":"Bharti Rajesh Kumar Shyamlal, Amol T Mahajan, Vikash Kumar, Aarohi Gupta, Rishabh Shrivastava Ronin, Manas Mathur, Janmejaya Sen, Sandeep Chaudhary","doi":"10.1021/acsmedchemlett.4c00491","DOIUrl":"10.1021/acsmedchemlett.4c00491","url":null,"abstract":"A series of novel N-arylsulfonylated C-homoaporphine alkaloids were synthesized under microwave irradiation and evaluated for their in vitro antiplatelet and antimicrobial activities. Among the series, compounds 12a, 12c, 12e, 12f, 12h, 12j, 12k, 12m, and 12o demonstrated highly potent (∼3-fold) platelet aggregation inhibitory activity than acetylsalicylic acid (IC50 = 21.34 μg/mL). Several N-arylsulfonylated C-homoaporphines also exhibited promising antimicrobial activity against various strains, including Macrophoma phaseolina, Trichoderma reesei, and Aspergillus niger, with minimum inhibitory concentrations (MIC) of 12.5, 6.25, and 12.5 μg/mL, respectively, comparable to Ketoconazole [MIC = 12.5 μg/mL (MP and AN strain); 6.25 μg/mL (TR strain)]. 12h showed potent antibacterial activity (IC50 = 6.25 μg/mL against Escherichia coli and Bacillus subtilis) compared to Ampicillin (IC50 = 12.5 μg/mL). After thorough structure-activity relationship (SAR) and in silico studies, C-homoaporphines were identified as a novel class of antiplatelet and antimicrobial agents.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 1","pages":"116-125"},"PeriodicalIF":3.5,"publicationDate":"2024-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11726367/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982086","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

Expanding the Chemical Space of Reverse Fosmidomycin Analogs

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-22 DOI: 10.1021/acsmedchemlett.4c0050110.1021/acsmedchemlett.4c00501

Talea Knak, Sana Takada, Boris Illarionov, Violetta Krisilia, Lais Pessanha de Carvalho, Beate Lungerich, Yasumitsu Sakamoto, Stefan Höfmann, Adelbert Bacher, Rainer Kalscheuer, Jana Held, Markus Fischer, Nobutada Tanaka* and Thomas Kurz*,

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引用次数: 0

Discovery of a Potent Triazole-Based Reversible Targeted Covalent Inhibitor of Cruzipain

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-22 DOI: 10.1021/acsmedchemlett.4c0046010.1021/acsmedchemlett.4c00460

Juan Pablo Cerutti, Lucas Abreu Diniz, Viviane Corrêa Santos, Salomé Catalina Vilchez Larrea, Guillermo Daniel Alonso, Rafaela Salgado Ferreira, Mario Alfredo Quevedo* and Wim Dehaen*,

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引用次数: 0

Novel Ergoline Compounds as 5-HT2A Agonists for Treating Mood Disorders Such as Depressive Disorders and Bipolar Disorders. 新型麦角碱化合物作为5-HT2A激动剂治疗心境障碍如抑郁症和双相情感障碍。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-20 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00593

Ram W Sabnis

引用次数: 0