265119-94-6Relevant articles and documents
Highly Potent Host-Specific Small-Molecule Inhibitor of Paramyxovirus and Pneumovirus Replication with High Resistance Barrier
Alves, Marco P.,Banfi, Damiano,Brügger, Melanie,Chambon, Marc,Fotiadis, Dimitrios,Gall, Flavio Max,Hierweger, Melanie Michaela,Horvat, Branka,Kalbermatter, David,Mathieu, Cyrille,Plattet, Philippe,Riedl, Rainer,Shrestha, Neeta,Turcatti, Gerardo,Vesin, Jonathan
, (2022/01/03)
Multiple enveloped RNA viruses of the family Paramyxoviridae and Pneumoviridae, like measles virus (MeV), Nipah virus (NiV), canine distemper virus (CDV), or respiratory syncytial virus (RSV), are of high clinical relevance. Each year a huge number of lives are lost as a result of these viral infections. Worldwide, MeV infection alone is responsible for over a hundred thousand deaths each year despite available vaccine. Therefore, there is an urgent need for treatment options to counteract these viral infections. The development of antiviral drugs in general stands as a huge challenge due to the rapid emergence of viral escape mutants. Here, we disclose the discovery of a small-molecule antiviral, compound 1 (ZHAWOC9045), active against several pneumo-/paramyxoviruses, including MeV, NiV, CDV, RSV, and parainfluenza virus type 5 (PIV-5). A series of mechanistic characterizations revealed that compound 1 targets a host factor which is indispensable for viral genome replication. Drug resistance profiling against a paramyxovirus model (CDV) demonstrated no detectable adaptation despite prolonged time of investigation, thereby mitigating the rapid emergence of escape variants. Furthermore, a thorough structure-activity relationship analysis of compound 1 led to the invention of 100-times-more potent-derivatives, e.g., compound 2 (ZHAWOC21026). Collectively, we present in this study an attractive host-directed pneumoviral/paramyxoviral replication inhibitor with potential therapeutic application.
Rational hapten design to produce high-quality antibodies against carbamate pesticides and development of immunochromatographic assays for simultaneous pesticide screening
Chen, Zi-Jian,Wu, Hui-Ling,Xiao, Zhi-Li,Fu, Hui-Jun,Shen, Yu-Dong,Luo, Lin,Wang, Hong,Lei, Hong-Tao,Hongsibsong, Surat,Xu, Zhen-Lin
, (2021/02/09)
Carbamate pesticides (CPs) are the most used pesticides in agricultural production and pest control. In this study, carbofuran, isoprocarb and carbaryl were employed as models, and a general hapten strategy based on carbamate moiety recognition was propos
5-benzofuran-1, 3, 4-thiadiazole-2-substituted amide compound and preparation method and application thereof
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Paragraph 0042-0045, (2020/10/20)
The invention provides a 5-benzofuran-1, 3, 4-thiadiazole-2-substituted amide compound and a preparation method and application of the 5-benzofuran-1, 3, 4-thiadiazole-2-substituted amide compound, and the 5-benzofuran-1, 3, 4-thiadiazole-2-substituted amide compound is shown as a formula (I). The preparation method of the compound or the pharmaceutically acceptable salt thereof is simple, the yield is high, the cost is low, and the obtained 5-benzofuran-1, 3, 4-thiadiazole-2-substituted amide compound or the pharmaceutically acceptable salt thereof has relatively high activity on plant pathogenic bacteria such as downy mildew and powdery mildew, has a good prevention and treatment effect, can be used as an alternative drug of a plant bactericide, and has a wide application prospect.
SMALL MOLECULE MODULATORS OF MHC-I
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Paragraph 0516; 0517, (2019/11/19)
The invention disclosed herein are embodiments of compounds capable of treating a viral infection. For example, the compounds are capable of inhibiting viral downmodulation of major histocompatibility complex I (MHC-I), such as by acting as immunomodulato
