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Diffractaic acid and its ethers as anti-respiratory syncytial virus agents Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-11 Aleksandr S. Filimonov, Diana U. Ismangulova, Anastasia A. Diveikina, Nina I. Komarova, Olga A. Luzina, Anna A. Shtro, Anastasia V. Galochkina, Yulia V. Nikolaeva, Artem M. Klabukov, Vera Z. Krivitskaya, Nariman F. Salakhutdinov
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Synthesis, urease inhibitory and anticancer evaluation of glucosamine-sulfonylurea conjugates Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-07 Ghadeer A. R. Y. Suaifan, Mayadah Shehadeh, Dua’a Tahboub, Aya A. M. Mohammed, Michael D. Threadgill, Anand Gaurav, Majid Khan
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Motor and non-motor symptoms, drugs, and their mode of action in Parkinson’s disease (PD): a review Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-07
Abstract Parkinson’s disease is second most common neurodegenerative disorder neurological illness that primarily affects patients in their later years of life. Specific neurons in the brain begin to malfunction resulting in a loss of a substance called dopamine which is characterized by the accumulation of α-synuclein aggregates within cells, forming structures known as Lewy bodies and Lewy neurites
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Evaluation of ortho-substituted Bis-Functionalized Triazoles as Tyrosinase Inhibitors: Modulating Dopamine Synthesis and Behavior in Zebrafish Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-06 Shainaz Landge, Jack Philp, Aikohi Ugboya, Isaac Graves, Emmanuel Fasusi, Kamari Jordan, Karelle Aiken, Vinoth Sittaramane
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Bioassay-guided fractionations of Cannabis sativa extract and HPLC-assisted purifications of anti-proliferative active fractions lead to the isolation of 16 known and one new phytomolecule and their in-silico analysis Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-05 Yedukondalu Nalli, Sahil Bharti, Tanzeeva Amin, Rohit Singh, Jayaprakash Behera, Sagar S. Bhayye, Yogesh P. Bharitkar, Anindya Goswami, Mahendra Kumar Verma
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Design, synthesis, and biochemical and computational screening of novel oxindole derivatives as inhibitors of Aurora A kinase and SARS-CoV-2 spike/host ACE2 interaction Med. Chem. Res. (IF 2.6) Pub Date : 2024-03-05 Donatus B. Eni, Joel Cassel, Cyril T. Namba-Nzanguim, Conrad V. Simoben, Ian Tietjen, Ravikumar Akunuri, Joseph M. Salvino, Fidele Ntie-Kang
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Evolution and challenges of opioids in pain management: Understanding mechanisms and exploring strategies for safer analgesics Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-29 Toluwalope Temitope Bakare, Henrietta Onyinye Uzoeto, Laywonmen Newon Gonlepa, Samuel Cosmas, Judith Nnedimkpa Ajima, Amarachukwu Vivian Arazu, Somtochukwu Precious Ezechukwu, Chizoba Maryann Didiugwu, Glory Omini Ibiang, Abayomi Gaius Osotuyi, Olanrewaju Ayodeji Durojaye
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Adenine derivatives as inhibitors of the casein kinase CK1delta enzyme Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-28
Abstract Overexpression of CK1δ has been associated to the development of cancer and neurodegenerative disorders, making ligands of this protein very promising drug candidates for the treatment these diseases and/or pharmacological tools for their study. A screening campaign of an in-house adenine derivative library revealed that some compounds are able to inhibit the CK1δ enzyme isoform with IC50
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Development of novel chalcone derivatives as multifunctional agents for the treatment of Alzheimer’s disease Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-26 Xinjuan Li, Yuting Li, Zhengwei Liu, Qiyao Zhang, Yi Zhou, Lintao Yu, Wenmin Liu, Zhipei Sang
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2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-24
Abstract α-amylase and α-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes for the first time their inhibition by a group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic inhibition of α-glucosidase rather
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Synthesis, characterization, and anticancer activity of syringaldehyde-derived chalcones against female cancers Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-19 Qionghui Pan, Huamao Yang, Zongxuan Du, Zefeng Ni, Qianqian Zhu, Sijun Tu, Yunjie Zhao, Faqing Ye
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The use of single-molecule FRET for the characterization of Holliday junctions containing human telomeric DNA: a methodological approach for nanoscale distance, mobility, and stability measurements Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-19 Abeer F. R. Alanazi, Shozeb Haider, Gary N. Parkinson
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Synthesis and pharmacological activities of Schiff bases with some transition metal complexes: a review Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-19 Kibrom Mezgebe, Endale Mulugeta
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Targeting disease with benzoxazoles: a comprehensive review of recent developments Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-18 Abdulrahman Abdullahi, Keng Yoon Yeong
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Insights on synthetic strategies and structure-activity relationship of donepezil and its derivatives Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-17 Saraswati Patel, Sonika Jain, Ritika Gururani, Swapnil Sharma, Jaya Dwivedi
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Preliminary structure−activity relationships analysis on N-(3,5-dichlorophenyl)-4,5-dihydronaphtho[1,2-d]thiazol-2-amine, a disruptor of mycobacterial energetics Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-17 Miriam Girardini, Diana Machado, Giannamaria Annunziato, Bianca Papotti, Marcella Palumbo, Chiara Spaggiari, Gabriele Costantino, Miguel Viveiros, Marco Pieroni
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Identification of novel benzoyl hydrazine derivatives as activators of neddylation pathway to inhibit the tumor progression in vitro Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-15 Xuan Wang, Sumeng Guan, Zunming Tian, Mei Zhao, Mengyu Li, Hua Yang, Ling Zhu, Moran Sun
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Novel biologically active pyridine derivatives: Synthesis, structure characterization, in vitro antimicrobial evaluation and structure-activity relationship Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-14 Mohamed A. Elsayed, Alshaimaa M. Elsayed, Farid M. Sroor
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Selectivity of N(2)-substituted oxotriazinoindole aldose reductase inhibitors is determined by the interaction pattern with Pro301-Arg312 loop of aldehyde reductase Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-14
Abstract Novel oxotriazinoindoles (OTIs) were recently reported as highly efficient and selective aldose reductase inhibitors. Here, a series of novel N(2)-substituted oxotriazinoindoles was developed with the aim to investigate molecular interactions within the aldose reductase (ALR2) inhibitor binding site. About twice increased inhibition efficacy of the most efficient derivative 14 (N(2)-CH2CH2COOH)
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Benzocaine-N-acylindoline conjugates: synthesis and antiviral activity against Coxsackievirus B3 Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-13 Alexandrina S. Volobueva, Anton A. Shetnev, Mikhail G. Mikhalski, Valeria A. Panova, Darina D. Barkhatova, Ekaterina D. Korshunova, Sergey A. Ivanovskiy, Vladimir V. Zarubaev, Sergey V. Baykov
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Exploring the latest breakthroughs in rhodesain inhibitors for African trypanosomiasis Med. Chem. Res. (IF 2.6) Pub Date : 2024-02-02 Diego Eidy Chiba, Guilherme Felipe dos Santos Fernandes, Jean Leandro dos Santos, Cauê Benito Scarim
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Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications Med. Chem. Res. (IF 2.6) Pub Date : 2024-01-29 Neha V. Bhilare, Rushikesh Shedge, Prashant M. Tambe, Ajinkya More
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Synthesis of adamantane-monoterpene conjugates with 1,3,4-thiadiazol-2(3H)-imine linker and evaluation of their inhibitory activity against TDP1 Med. Chem. Res. (IF 2.6) Pub Date : 2024-01-12 Aldar A. Munkuev, Alexandra L. Zakharenko, Tatyana E. Kornienko, Nadezhda S. Dyrkheeva, Ekaterina S. Ilina, Evgeniy V. Suslov, Fatima Issa, Chigozie Achara, Jóhannes Reynisson, Konstantin P. Volcho, Nariman F. Salakhutdinov, Olga I. Lavrik
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Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48 Med. Chem. Res. (IF 2.6) Pub Date : 2024-01-10 Wenhui Cheng, Yuejuan Zhang, Cheng Chen, Lei Gao, Yuwei Lv, Dian Yu, Bin Chen, Yi Wan
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Rehmannia glutinosa polysaccharides: a review on structure-activity relationship and biological activity Med. Chem. Res. (IF 2.6) Pub Date : 2024-01-10
Abstract Rehmannia glutinosa has been used historically and is now listed in the 2020 Chinese Pharmacopoeia as a traditional Chinese medicine for nourishing yin and tonifying kidney. Polysaccharides are one of the main active ingredients in Rehmannia glutinosa. In recent years, Rehmannia glutinosa polysaccharides have received widespread attention due to their various biological activities such as
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Polyketides from Neohelicosporium griseum: structure assignment and bioactivity investigation Med. Chem. Res. (IF 2.6) Pub Date : 2024-01-04 Lijuan Zhang, Jian Ma, Mingfei Yang, Tianming Zhao, Mei Yan Han, Dege Zheng, Ausana Mapook, Yongzhong Lu, Ruvishika S. Jayawardena
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Research progress on the mechanism of anti-myocardial infarction effect and clinical application of effective components of Salvia miltiorrhiza Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-30
Abstract Salvia miltiorrhiza, a plant in the Labiatae family, is a traditional Chinese herb. The small molecular components in S. miltiorrhiza can be divided into tanshinones and salvianolic acids, which have anti-inflammatory and anti-apoptotic effects by inhibiting the expression of inflammatory factors such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6) and some
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Indazole derivatives as selective inhibitors of butyrylcholinesterase with effective blood-brain-barrier permeability profile Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-30 Asuka Joy Tobuse, Christine Shing Wei Law, Chun Keng Thy, Jason Jonah James, Chin Fei Chee, Keng Yoon Yeong
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Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-29 Benjamin E. Blass, Rong Gao, Kevin M. Blattner, John C. Gordon, Douglas A. Pippin, Daniel J. Canney
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Synthesis and pharmacological evaluation of novel coumarin based triazolyl glycoconjugates as potential antibacterial and anti-proliferative agents Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-28 Surendra Jatav, Ranjit Singh, Nishant Pandey, Pratibha Dwivedi, Jyoti, Monika Thakur, Sudhir Pratap Singh, Ranju Bansal, Bhuwan B. Mishra
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Bioactivities and the structural modification of Parthenolide: a review Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-23 Jie Wu, Xiaoqian Wang, Yunlei Hou, Ping Gong
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Self-assembled amphiphilic bipyridine and bisquinoline cisplatin analogues: synthesis and anticancer properties Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-23 Gabriel A. Gonzalez, Javier Hernandez-Ortega, Sudakha Kalagara, Bonifacio Alvarado-Tenorio, Alejandro Martinez-Martinez, Angel G. Diaz-Sanchez, Juan C. Noveron
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A concise review on anti-breast cancer effectiveness of s-triazines through EGFR kinase inhibition Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-21 Pooja Tandel, Rachana Upadhyay, Amit B. Patel
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Design, synthesis and evaluation of aurone and indanone derivatives as novel antitumor agents Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-20 Baoxing Xie, Gulmira Turdu, Chao Niu, Haji Akber Aisa
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Design, synthesis, molecular docking, and biological activity of pyrazolo[3,4-b]pyridines as promising lead candidates against Mycobacterium tuberculosis Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-19 H. Surya Prakash Rao, R. Gunasundari, Lakshmi Narayana Adigopula, Jayaraman Muthukumaran
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Pyrrolobenzodiazepines: natural sources, therapeutic uses, and future in neurological treatments Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-18 Hadi Obaji, Abbas G. Shilabin, Soumyajit Majumdar, Mohamed A. Ibrahim
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Indazole derivatives as novel inhibitors of monoamine oxidase and D-amino acid oxidase Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-15 Chezélle Stear, Anél Petzer, Chantalle Crous, Jacobus P. Petzer
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Computer-aided design, synthesis and evaluation of new SARS-CoV-2 Mpro inhibitors based on 1,5,6,7-tetrahydro-4H-indazol-4-one scaffold Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-11 Yuri A. Piven, Veronica G. Zinovich, Dmitriy N. Shcherbakov, Varvara Yu. Chirkova, Svetlana V. Belenkaya, Raman M. Puzanau, Tatyana S. Khlebnicova, Fedor A. Lakhvich
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Discovery of novel fatty acid amide hydrolase (FAAH) inhibitors as anti-Alzheimer’s agents through pharmacophore-based virtual screening, molecular docking and experimental validation Med. Chem. Res. (IF 2.6) Pub Date : 2023-12-09 Smita Jain, Swapnil Sharma, Ajita Paliwal, Jaya Dwivedi, Shailendra Paliwal, Vartika Paliwal, Sarvesh Paliwal, Jaiprakash Sharma
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Enantioselectivity of pinene against Leishmania amazonensis Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-25 Ingrid S. Adão, Andreza R. Garcia, Kamila M. Sette, Camila M. Adade, Jefferson R. de Andrade Silva, Ana Claudia F. Amaral, Anderson S. Pinheiro, Igor A. Rodrigues
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Characterization of novel angiotensin-I converting enzyme inhibitory peptides derived from Taiwan red quinoa (Chenopodium formosanum Koidz.) seed proteins using two sequential bioassay-guided fractionations Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-23 Dininurilmi Putri Suleman, Christoper Caesar Yudho Sutopo, Jue-Liang Hsu
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One-pot synthesis and in vitro bioactivity of novel 4-aminopyrazolo[3,4-b]pyridine derivatives as potential antimicrobial compounds Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-23 Ranjana Aggarwal, Suresh Kumar, Garima Sumran, Deepansh Sharma
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Kaempferia diterpenoids and flavonoids: an overview on phytochemistry, biosynthesis, synthesis, pharmacology, and pharmacokinetics Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-21 Chu Anh Van, Dau Xuan Duc, Ninh The Son
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Design and synthesis of novel cycloalkanecarboxamide parabanic acid hybrids as anticonvulsants Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-15 Walaa Hamada Abd-Allah, Mohamed Samir Abd El-Maksoud, Marawan A. Elbaset, Alyaa F. Hessin, Rasha Mohamed Hassan
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Design, synthesis and antimicrobial activities of 1,2,3-triazole hybrids with amine-ester functionality Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-04 Jyoti Sangwan, C. P. Kaushik, Lokesh Kumar, Jayant Sindhu, Manisha Chahal
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Design, synthesis, and in silico studies of novel di-(2-aryl hydrozonopropanal) arene derivatives as potent anticancer for targeting A2AR and LRP6 in HCT116 cell Med. Chem. Res. (IF 2.6) Pub Date : 2023-11-03 Tahani Bakhsh, Tamer S. Saleh, Dalal A. Al-Saedi, Khadijah M. Al-Zaydi
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Discovery of potent maternal embryonic leucine zipper kinase (MELK) inhibitors of novel chemotypes using structure-based pharmacophores Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-28 Safa Daoud, Shada J. Alabed, Sanaa K. Bardaweel, Mutasem O. Taha
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Screening of small molecule compounds targeting hnRNPA2 protein Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-28 Yuan-Rong Zheng, Chao-Jie Wang, Ling Yang, Yu-Jun Zhang, Mei-Juan Fang, He Chang, Kai-Qiang Guo, Song-Lin Shi
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Novel aloe emodin–hydroxyethyl piperazine hybrid dihydrochloride induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-19 Xing Long, Peilin Yang, Lin Chen, Wen Zhong, Shaofeng Chen, Yanping Li, Shijie Lin, Wei Tian
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The trimethoxyphenyl (TMP) functional group: a versatile pharmacophore Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-16 Mohammad Amin Langarizadeh, Alieh Ameri, Marziye Ranjbar Tavakoli, Ardavan Abiri, Hamid Forootanfar
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Synthesis of 6,6-Dimethyl-3-azabicyclo [3.1.0]hexane via Ru (II)-catalyzed intramolecular cyclopropanation Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-14 Yu Li, Yujie Ma, Shihao Cheng, Chenhu Dong, Xueer Zhong, Jun Xu, Yu Zhao
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1,2,3-triazole derivatives as antiviral agents Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-09 Naima Agouram
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Evaluation of chemical constituents of Rooibos (Aspalathus linearis) and Honeybush (Cyclopia intermedia) as adenosine A1/A2A receptor ligands Med. Chem. Res. (IF 2.6) Pub Date : 2023-10-05 Liezel Gouws, Helena D. Janse van Rensburg, Gisella Terre’Blanche, Mietha M. Van der Walt
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Current progress toward synthetic routes and medicinal significance of quinoline Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-28 Wesam S. Shehab, Mostafa M. K. Amer, Doaa A. Elsayed, Krishna Kumar Yadav, Magda H. Abdellattif
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Lipase inhibitory activity of constituents of Physalis glutinosa and Physalis latiphysa Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-25 Emma Maldonado, Areli Mineros, Oscar D. Torres, Berenice Ovalle-Magallanes, Abraham Madariaga-Mazón, Ana L. Pérez-Castorena, Mahinda Martínez
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New indolo-β-lactam hybrids as potential anticancer and anti-inflammatory agents Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-25 Saeedeh Ghaffari, Aliasghar Jarrahpour, Namik Özdemir, Jean Michel Brunel, Banafsheh Rastegari, Elham Riazimontazer, Edward Turos
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Advances in research of ursolic acid and its derivatives as potential drug candidates against various types of lung cancers Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-25 Li Song, Ling Dai, Yan Tan, Kailin Jiang, Xueni Wei, Yufei Hu, Yalin Hu, Jieying Lin, Xu Yao, Pengbing Mi, Xing Zheng
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Design, synthesis and antiproliferative activity of ACY-1215 analogs as potent selective histone deacetylases 6 inhibitors Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-20 Hongfei Duan, Jiayun Wang, Guoliang Gong, Xin Chen, Xinyang Chen
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Synthetic coumarin derivatives with anticoagulation and antiplatelet aggregation inhibitory effects Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-16 Triveena M. Ramsis, Maha A. Ebrahim, Eman A. Fayed
Thrombosis is the leading cause of illness and mortality worldwide, posing a serious risk to human health and life. Because antithrombotic drugs can prevent the beginning and progression of thrombotic disorders, they are essential in the management of thrombotic diseases. The substantial side effects and unsatisfactory efficacy of present antithrombotic drugs stimulate the search for novel, effective
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Minimizing the DILI potential of carboxylic acid-containing drugs: a perspective Med. Chem. Res. (IF 2.6) Pub Date : 2023-09-09 Lars Weidolf, Ian Wilson