Article
Biochemistry & Molecular Biology
Daibao Wei, Tianwen Hu, Yumin Zhang, Wei Zheng, Haitao Xue, Jingshan Shen, Yuanchao Xie, Haji A. Aisa
Summary: Nucleoside metabolite GS-441524, an analog of remdesivir, shows potent anti-SARS-CoV-2 efficacy but has poor oral bioavailability in non-human primates. Various GS-441524 analogs with modifications and prodrug forms were developed, with the 7-fluoro analog 3c and certain prodrugs demonstrating moderate to excellent activities and oral bioavailabilities, providing insights for pharmacokinetic optimization.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Agronomy
Miao Yu, He Liu, Longyu Guo, Tao Zhou, Yuhang Shan, Zihao Xia, Xinghai Li, Mengnan An, Yuanhua Wu
Summary: This study synthesized a series of compounds containing the structure of pyrimidine and moroxydine, and found that GLY-15 exhibited good antiviral activity against tobacco mosaic virus by activating the defense response of plants and inhibiting the transmission, accumulation, and RNA accumulation of the virus.
PEST MANAGEMENT SCIENCE
(2022)
Article
Chemistry, Multidisciplinary
Xuemei Tang, Wenliang Zhan, Shuai Chen, Ran Zhou, Die Hu, Nan Sun, Qiang Fei, Wenneng Wu, Wei Xue
Summary: In this study, a series of trifluoromethyl pyrimidine derivatives were designed and synthesized. Bioassay results showed that some of these compounds exhibited higher antiviral and antifungal activities than commercial agents. In particular, compounds 5j and 5m demonstrated lower EC50 values compared to ningnan-mycin. Microscale thermophoresis experiment confirmed a strong interaction between compound 5m and TMV-CP. Moreover, compound 5u displayed significant in vitro antifungal activity against Rhizoctonia solani (RS) and effectively controlled RS in vivo.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Engineering, Electrical & Electronic
Xi-Tao Yin, Wen-Dong Zhou, Davoud Dastan, Jing Li, Xiao-Ming Tan, Ying Liu, Xiao-Chun Gao, Xiao-Guang Ma
Summary: This study fabricated a ZnO-xCo(3)O(4) composite and measured its gas sensing selectivity, crystal structure, morphology, and chemical element state. It was found that the gas sensing behavior of the material was influenced by the concentrations of n- and p-type materials. The optimized ZnO-0.269Co(3)O(4) composite showed a high selectivity value of 24.2 to CO against CH4. This research offers a promising way to solve the poor selectivity of metal oxide semiconductor sensors to homogeneous gases.
MATERIALS SCIENCE IN SEMICONDUCTOR PROCESSING
(2022)
Article
Chemistry, Multidisciplinary
Chenxi Wang, Huiting Yang, Yanxin Xiang, Shihao Pang, Chunyan Bao, Linyong Zhu
Summary: Inspired by natural phospholipid structures, a synthetic phospholipid LC has been developed with ion transport capabilities, particularly for K+. LC may transport ions through a channel mechanism and shows selectivity for Rb+. Additionally, LC displays toxicity to HeLa cells.
FRONTIERS IN CHEMISTRY
(2021)
Article
Infectious Diseases
Tinnakorn Theansungnoen, Santi Phosri, Sureewan Bumrungthai, Jureerut Daduang, Sompong Klaynongsruang, Sakda Daduang
Summary: This study developed two novel antimicrobial peptides (WSKK11 and WSRR11) that demonstrated high antimicrobial activity against the acne-causing bacterium Cutibacterium acnes. These peptides exhibited low cytotoxicity to human cells and have potential applications.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Jitendra Subhash Rane, Preeti Pandey, Aroni Chatterjee, Rajni Khan, Abhijeet Kumar, Amresh Prakash, Shashikant Ray
Summary: The global human population is currently dealing with the horrific impact of the COVID-19 pandemic, and research targeting the spike glycoprotein of the virus for drug development holds significant therapeutic potential in combatting infection. This study used computational techniques to identify potential inhibitors that disrupt the interaction between the spike glycoprotein and the hACE2 receptor, providing a promising avenue for future antiviral drug development.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Horticulture
Raheeba Tun Nisa, Khurshid Ahmad Bhat, Umer Basu, Rameesa Rashid, Xiukang Wang, Shaheen Kauser Jan, H. S. Viswanath, Walid Soufan, Muntazir Mushtaq, Muhammad Habib ur Rahman, Farooq Ahmad Bhat, Ayman EL Sabagh
Summary: The study focused on isolating potential bio-agents exhibiting resistance to copper oxychloride and evaluating their efficacy in seed treatment for the management of Fusarium wilt of lentil. Isolates H10 and C9 showed excellent compatibility with copper oxychloride and high inhibitory percentages against Fusarium oxysporum f. sp. lentis. These bioagents also demonstrated superior ability to reduce disease incidence and severity in pot cultures when used alone or in combination with copper oxychloride fungicide.
Article
Chemistry, Multidisciplinary
Mamdouh A. Abu-Zaied, Galal H. Elgemeie, Nashwa M. Mahmoud
Summary: A class of pyrimidine thioglycoside analogs were synthesized and evaluated for their pharmacological activity against SARS-COV-2 and H5N1 virus strains, showing promising results.
Article
Chemistry, Multidisciplinary
Omkar Zilka, Jia-Fei Poon, Derek A. Pratt
Summary: CuATSM is a potent radical-trapping antioxidant and (phospho)lipid peroxidation inhibitor, with a mechanism differing from conventional antioxidants like alpha-tocopherol. Its ability to reversibly bind peroxyl radicals allows for effective ferroptosis inhibition. Experiments demonstrate CuATSM's high potency in rescuing ferroptosis, with compounds like CuATSP showing even greater efficacy.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Biochemistry & Molecular Biology
Ignacio Lizana, Gina Pecchi, Elena A. Uribe, Eduardo J. Delgado
Summary: This article theoretically studied the inhibitory mechanisms of ETX2514 and avibactam against OXA-24. The results showed that both inhibitors share similar steps and intermediates in the inhibition process, but have different activation barriers. The endocyclic double bond and methyl substituent in the piperidine ring of ETX2514 contribute to its stronger inhibitory ability. Additionally, Lys218 and carboxylated Lys84 of ETX2514 play a crucial role in the mechanism by coordinating their protonation states.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
(2022)
Article
Food Science & Technology
Huihui Li, Lijun Tan, Bowen Chen, Jiaming Huang, Qiaohui Zeng, Haiquan Liu, Yong Zhao, Jing Jing Wang
Summary: This study demonstrated the antibacterial potency of novel riboflavin-mediated blue LED PDI against Salmonella and its biofilms, as well as its effectiveness in reducing Salmonella on tuna. Higher irradiation dosage was found to accelerate lipid oxidation, but had no significant negative impact on the total protein and total volatile basic nitrogen content of tuna.
LWT-FOOD SCIENCE AND TECHNOLOGY
(2021)
Article
Biochemistry & Molecular Biology
An-Ping Li, Ying-Hui He, Shao-Yong Zhang, Yan-Ping Shi
Summary: Phytopathogenic bacteria, the most difficult plant disease to control, cause significant losses to agricultural products and the economy globally. This study evaluated 50 flavonoids for their antibacterial activities against two challenging plant bacterial pathogens and found that kaempferol exhibited excellent antibacterial activity against Xanthomonas oryzae (Xo) and quercetin showed the best antibacterial activity against Xanthomonas axo-nopodis pv citri (Xac). Further investigation revealed that kaempferol mainly exerted bacteriostatic effects by affecting bacterial energy metabolism, reducing pathogenicity, and leading to cellular damage and death.
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Infectious Diseases
Gabriela Marinho Righetto, Jose Luiz de Souza Lopes, Paulo Jose Martins Bispo, Camille Andre, Julia Medeiros Souza, Adriano Defini Andricopulo, Leila Maria Beltramini, Ilana Lopes Baratella da Cunha Camargo
Summary: Antimicrobial resistance is a major public health concern and there is a need for novel antimicrobial therapies. This study designed a new antimicrobial peptide Pln149-PEP20 and tested its activity against 60 different species of bacteria. The results showed that Pln149-PEP20 had excellent bactericidal activity and its target was likely genes associated with membrane metabolism.
Article
Infectious Diseases
Kirsten E. Knoll, Zander Lindeque, Adetomiwa A. Adeniji, Carel B. Oosthuizen, Namrita Lall, Du Toit Loots
Summary: Tuberculosis, caused by Mycobacterium tuberculosis, remains a leading cause of death globally due to drug resistance and lack of patient adherence. A decoquinate derivative RMB041 has shown promising antimicrobial activity against Mtb, but its mechanism of action remains unknown. Metabolic analysis suggests that the drug primarily affects fatty acid and amino acid metabolism in Mtb, supporting previous findings of its action on cell wall and DNA metabolism.
Article
Biochemistry & Molecular Biology
Saida Lachhab, Az-eddine El Mansouri, Ahmad Mehdi, Indira Dennemont, Johan Neyts, Dirk Jochmans, Graciela Andrei, Robert Snoeck, Yogesh S. Sanghvi, Mustapha Ait Ali, Philippe M. Loiseau, Hassan B. Lazrek
Summary: A new series of 3-acetyl-1,3,4-oxadiazoline hybrid molecules were designed and synthesized, and their activities against pathogens were screened. One of the intermediates exhibited significant antileishmanial activity.
MOLECULAR DIVERSITY
(2023)
Article
Pharmacology & Pharmacy
Iwona E. Glowacka, Katarzyna Gawron, Dorota G. Piotrowska, Mirthe Graus, Graciela Andrei, Dominique Schols, Robert Snoeck, Anita Camps, Emiel Vanhulle, Kurt Vermeire
Summary: In this study, a series of 48 hybrids were synthesised and evaluated for antiviral activity. The hybrids contained a diethoxyphosphoryl group connected to the triazole moiety via ethylene or propylene linker, and substituted benzyl or benzoyl function in the quinazoline-2,4-dione moiety. The hybrids showed potent antiviral activities against Respiratory Syncytial Virus (RSV), with some weak activity against varicella zoster virus and human cytomegalovirus.
ANTIVIRAL RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Jianyang Han, Jakob Arnold, Christophe Pannecouque, Graciela Andrei, Robert Snoeck, Clemens Richert
Summary: Strongly pairing ethynylpyridone C-nucleosides are being explored as substitutes for thymidine in oligonucleotides. However, the strong lipophilicity of ethynylpyridone has been found to limit its antiviral activity. Two strategies are being pursued to overcome this issue, including replacing the ethynyl group with a cyano group and using less lipophilic amino acid esters in a phosphoramidate prodrug design. These findings contribute to the development of next-generation pyridone C-nucleosides as potential antivirals.
HELVETICA CHIMICA ACTA
(2023)
Article
Biochemistry & Molecular Biology
Zhao-Hui Wen, Meng-Meng Wang, Ling-Yun Li, Piet Herdewijn, Robert Snoeck, Graciela Andrei, Zhao-Peng Liu, Chao Liu
Summary: In this study, the synthesis of lipid prodrugs of beta-D-N4-hydroxycytidine (NHC) and a 3'-fluoro modified NHC analogue was reported, and their antiviral activity against five variants of SARS-CoV-2 was evaluated. The lipid prodrugs showed potent antiviral activity against the tested variants, with comparable or higher EC50 values than remdesivir and molnupiravir. The 3'-F analogue of NHC only exhibited minor antiviral activity against the Omicron variant, while no activity was observed against other variants. The promising antiviral data of the lipid prodrugs suggest their potential as new anti-SARS-CoV-2 drugs.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
M. P. Paramonova, E. S. Gureeva, A. A. Ozerov, R. Snoeck, G. Andrei, D. A. Aleksandrov, A. L. Khandazhinskaya, M. S. Novikov, S. N. Kochetkov
Summary: A new series of 1-[ω-(bromophenoxy)alkyl]-uracil derivatives containing various fragments were synthesized and tested for their antiviral activity against human cytomegalovirus. It was found that the compound with a bridge of five methylene groups exhibited high anti-cytomegalovirus activity in vitro.
DOKLADY BIOCHEMISTRY AND BIOPHYSICS
(2023)
Article
Pharmacology & Pharmacy
Evelien Vanderlinden, Arnaud Boonen, Sam Noppen, Geert Schoofs, Maya Imbrechts, Nick Geukens, Robert Snoeck, Annelies Stevaert, Lieve Naesens, Graciela Andrei, Dominique Schols
Summary: PRO-2000, a sulfonated polyanionic compound, has anti-SARS-CoV-2 activity by blocking the entry pathway and inhibiting the binding of the S protein to its receptor. It can potentially inhibit a broad range of SARS-CoV-2 variants.
ANTIVIRAL RESEARCH
(2023)
Article
Urology & Nephrology
Evert Cleenders, Priyanka Koshy, Elisabet Van Loon, Katrien Lagrou, Kurt Beuselinck, Graciela Andrei, Marta Crespo, Katrien De Vusser, Dirk Kuypers, Evelyne Lerut, Kris Mertens, Olga Mineeva-Sangwo, Parmjeet Randhawa, Aleksandar Senev, Robert Snoeck, Ben Sprangers, Claire Tinel, Amaryllis Van Craenenbroeck, Jan van den Brand, Marc Van Ranst, Geert Verbeke, Maarten Coemans, Maarten Naesens
Summary: This study aimed to investigate the value of performing a biopsy at the time of BKPyV-DNAemia in distinguishing presumptive and proven PyVAN. The results showed that plasma viral load had good predictive value for SV40 positivity, while the dichotomy of SV40 immunohistochemistry did not predict viral clearance. Therefore, the distinction between presumptive and proven PyVAN based on SV40 immunohistochemistry has limited clinical value.
KIDNEY INTERNATIONAL
(2023)
Review
Pharmacology & Pharmacy
Graciela Andrei, Robert Snoeck
Summary: This article discusses the global outbreak of mpox virus (MPXV) since May 2022 and its differences from the traditional mpox virus endemic in Africa. The study explores the genomic changes and drivers of MPXV evolution, as well as the use of vaccines and antivirals developed against smallpox virus in containing the mpox outbreak.
TRENDS IN PHARMACOLOGICAL SCIENCES
(2023)
Article
Multidisciplinary Sciences
Olga Mineeva-Sangwo, Elisabet Van Loon, Graciela Andrei, Dirk Kuypers, Maarten Naesens, Robert Snoeck
Summary: BK polyomavirus (BKPyV) is a latent human DNA virus in renal tissue that can reactivate and cause polyomavirus-associated nephropathy (PVAN), particularly in kidney transplant recipients. There are currently no specific antivirals for BKPyV, so reducing immunosuppression is the main treatment approach. Mutations in the major capsid protein VP1 of BKPyV can accumulate over time and lead to neutralization escape in kidney transplant recipients. A study found mutations throughout the entire BKPyV genome, including VP1, and these changes should be considered in future approaches for treating BKPyV infection in kidney transplant recipients.
SCIENTIFIC REPORTS
(2023)