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更新于：2025-05-07

Denotivir

更新于：2025-05-07

概要

概要

基本信息

药物类型

小分子化药

别名

Denotivir (INN)、ITCL

+ [1]

靶点-

作用方式

抑制剂

作用机制

DNA合成抑制剂

治疗领域

感染

在研适应症-

非在研适应症

病毒感染

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

权益机构-

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C18H14ClN3O2S

InChIKeyZPBLNADJHWHOEP-UHFFFAOYSA-N

CAS号51287-57-1

关联

100 项与 Denotivir 相关的临床结果

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100 项与 Denotivir 相关的转化医学

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100 项与 Denotivir 相关的专利（医药）

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项与 Denotivir 相关的文献（医药）

2025-01-01·Poultry Science

Dietary supplementation with 15% tomato pomace (Solanum lycopersicum L.) improves sperm production and antioxidant status in aged male broiler breeders

Article

作者: Nabiloo, Mehdi ; Karimi Torshizi, Mohammad Amir ; Eslami, Mohsen ; Mosayyeb Zadeh, Amir ; Hasanloo, Peyman ; Nadri, Touba ; Mirghelenj, Seyyed Ali ; Daneshyar, Mohsen ; Kastelic, John Patrick ; Zhandi, Mahdi

The objective was to investigate effects of dietary tomato pomace (TP) and L-Arginine (L-Arg; 10% above nutritional recommendation) in aged male broiler breeders. Thirty male broiler breeders (Ross 308), 58 wk old, were randomly and equally allocated into five experimental groups: basal diet (C); 5% TP-supplemented (T-5); 10% TP-supplemented (T-10); 15% TP-supplemented (T-15); and L-Arg supplemented (L-10) groups. In contrast to the Control and TP-supplemented groups, sperm of L-10 roosters had higher C14:1, C16:0 and C18:1 n-9c proportions, total saturated fatty acid (FA) contents, and n-6:n-3 ratios, but a lower C22:4 n-6 content (P<0.05). However, sperm of T-15 roosters had increased C18:2 n-6, C22:6 n-3 and total unsaturated FA contents but reduced n-6:n-3 ratios compared to Control birds (P<0.05). Additionally, serum of T-15 roosters had lower cholesterol and triglyceride (TG) concentrations, along with decreased aspartate aminotransferase (AST) activity (P<0.05). In serum of T-15 and L-10 roosters, there were increases (P<0.05) in total antioxidant capacity (TAC) and uric acid (UA) and a reduction (P<0.05) in malondialdehyde (MDA) concentration. The T-15 roosters had higher (P<0.05) serum testosterone concentration and testes glutathione peroxidase (GPx) activity. Superoxide dismutase (SOD) content was reduced (P<0.05) in L-10 roosters. Seminiferous tubule diameter (STD) and seminiferous epithelium thickness (SET) were increased in all groups fed TP (P<0.05) and T-10 and T-15 roosters had increases (P<0.05) in tubular differentiation indices (TDI). The T-15 and L-10 groups had higher mRNA expressions of AKT1 and Nrf2 (P<0.05). In conclusion, in aged male broiler breeders, up to 15% TP supplementation is recommended to improve reproductive performance by enhancing testes histology and antioxidant status.

2025-01-01·Current HIV Research

Design, In Silico, and In vitro Evaluation of Polymer-Based Drug Conjugates Incorporated with Derivative of Cinnamic Acid, Zidovudine, and 4-Aminosalicylic Acid against Pseudo-HIV-1

Article

作者: Matshe, W.M.R. ; Obisesan, O. ; Oselusi, S.O. ; Naki, T. ; Ray, S.S. ; Balogun, M.O. ; Aderibigbe, B.A.

Background:The incorporation of anti-HIV drugs into polymer to form polymer-drug conjugates has been reported to result in improved therapeutic activity. Zidovudine, an anti-HIV drug, was explored alone and in combination with known drug molecules using polyamidoaminebased carriers.Objective:Polymer-drug conjugates incorporated with zidovudine, cinnamic acid, and 4-aminosalicylic acid were prepared and evaluated for their potential efficacy in vitro against pseudo- HIV-1.Methods:Aqueous Michael addition polymerization reaction was employed to prepare the conjugates. The conjugates were incorporated with zidovudine, cinnamic acid, and 4-aminosalicylic acid. They were characterized by SEM/EDX, XRD, FTIR, NMR, LC-MS, particle size analysis, in vitro analysis, computational studies, and in silico toxicity predictions.Results:The conjugates displayed spherically shaped morphology. The in vitro findings showed that polymer-drug conjugates, T15 and T16, with a single drug were effective against pseudo- HIV-1 at high concentrations of 111.11 and 333.33 μg/mL, respectively. The molecular docking studies confirmed the in vitro results. The Swiss ADME, ProTox-II, and GUSAR (General Unrestricted Structure-Activity Relationships) revealed that these compounds are promising antiviral compounds.Conclusion:The prepared polymer-drug conjugates with a single drug showed promising effects against the Pseudo-HIV-1, and the conjugates displayed features that make them potential anti- HIV therapeutics that require further studies.

2023-04-23·Microorganisms

Rhizobacterial Colonization and Management of Bacterial Speck Pathogen in Tomato by Pseudomonas spp.

Article

作者: Elsharkawy, Mohsen M ; Behiry, Said I ; El-Kady, Elsayed M ; Alwutayd, Khairiah Mubarak ; Mehiar, Farid ; Khedr, Amr A

Plants and soil microorganisms interact at every stage of growth. Pseudomonas spp. are highly regarded for their ability to increase crop production and protection from diseases. The aim of this study is to understand the mechanisms of the rhizobacterial colonization of tomato roots via chemotaxis assay and the activation of tomato resistance against the pathogenic bacterium, Pseudomonas syringae pv. tomato DC3000 (Pst). The capillary assay was used to evaluate the chemotaxis response of PGPRs (plant growth-promoting rhizobacteria). The activities of defense enzymes and the expressions of PR (pathogenesis-related) genes were measured using real-time qPCR. Chemotactic responses to malic and citric acids (the most important root exudates found in different plant species) at low concentrations varied substantially among the rhizobacterial isolates (63 species). Beneficial isolates including Pseudomonas resinovorans A5, P. vranovensis A30, P. resinovorans A28, P. umsongensis O26, P. stutzeri N42, and P. putida T15 reacted well to different concentrations of root exudates. P. putida T15 demonstrated the most potent anti-Pst activity. At three and six days after inoculation, the greatest levels of polyphenol oxidase and peroxidase activity were reported in the A5 and T15 groups. In tomato, transcript levels of four PR (pathogenesis-related) genes were elevated by rhizobacterial treatments. PGPR isolates alone or in combination with BABA (β-amino butyric acid) up-regulated the transcriptions of PR1, PR2, LOX, and PAL genes. Treatments with N42 and T15 resulted in the greatest improvements in tomato growth and yield traits. In conclusion, the results explain the mechanisms of rhizobacterial colonization for the improved management of Pst. Rhizobacterial isolates play a role in tomato's resistance to Pst via salicylic acid and jasmonic acid pathways.

100 项与 Denotivir 相关的药物交易

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