Synthesis and in-vitro evaluation of 2-amino-4-arylthiazole as inhibitor of 3D polymerase against foot-and-mouth disease (FMD)

Jeong, Kwiwan; Lee, Jung-Hun; Park, Sun-mi; Choi, Joo-Hyung; Jeong, Dae-Youn; Choi, Dongkyu; Nam, Yeon-Ju; Park, Jong Hyeon; Lee, Kwang-Nyeong; Kim, Su-Mi; Ku, Jin‐Mo

doi:10.1016/j.ejmech.2015.08.020

Cited by 27 publications

(11 citation statements)

References 35 publications

(25 reference statements)

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“…The mortality rates are alreadylow but rate of morbidity are high when FMD out break occurs, with the decrease in milk yield, meat production andpoor skin quality and cause abortion with repeat breeding problem in animals and causes in severe economic losses to the flock industry, especially in FMD-free countries of the world (Ko et al 2012;Rajasekhar et al 2013;Jeong et al 2015).…”

Section: Introductionmentioning

confidence: 99%

The Effect of Used Immunostimulating Drugs with FMD Vaccine on Immunoglobulins in Sheep

Abdullah¹,

Başbuğan

2020

Van Veterinary Journal

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In this study, the effect of used immunostimulating drugs with FMD vaccine on immunoglobulins was aimed to investigate in sheep. For this purpose 40 healthy sheep were divided into 4 groups. Blood and serum samples were taken from all animals from 0 days before the study. Blood samples were measured immediately, and IgA, IgG, IgM, IgE and Zn values from biochemical parameters were stored for measurement. Group I was applied only FMD vaccine, group II Levamisole with the FMD vaccine, group III Zinc with FMD vaccine and the last group IV AD3E was applied with FMD vaccine. After 21 days, blood and serum samples from all groups were taken again and hematologic and IgA, IgG, IgM, IgE and Zn values were compared according to the values of day 0. No statistical difference was found between the groups except for PLT in hematological parameters (p> 0, 05) when compared to pre-vaccination and post-vaccination. In groups II and III there was a significant increase in PLT levels. Biochemical analysis showed IgA, IgG, IgM and IgE levels to be higher in IgG (p <0, 05) and IgE (p <0,001) in groups II and III when levels compared to before vaccination. There were statistically significant increases in IgM (p <0.05) in group IV.

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Section: Introductionmentioning

confidence: 99%

The Effect of Used Immunostimulating Drugs with FMD Vaccine on Immunoglobulins in Sheep

Abdullah¹,

Başbuğan

2020

Van Veterinary Journal

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“…Then, various aryl thioureas 4 were prepared from isothiocyanates 3 upon reaction with ammonia [23,24]. Finally, thioureas 4 were condensed with diverse α-bromophenylethanones [24,25], synthesized separately via reaction of acetophenones with Br2 in DCM [24], to afford the 2-amino-1,3-thiazole heterocyclic skeleton, and the targeted compound N-phenylacetamide derivatives containing thiazole moieties were thus obtained. The structures of all target compounds were confirmed by 1 H-NMR, 13 C-NMR and HRMS.…”

Section: Chemistrymentioning

confidence: 99%

“…The structures of all target compounds were confirmed by 1 H-NMR, 13 C-NMR and HRMS. Among them, it was unexpectedly found that compounds A4, A7, A11, A12 have been previously reported [25].…”

Section: Chemistrymentioning

confidence: 99%

Synthesis and Antibacterial Evaluation of N-phenylacetamide Derivatives Containing 4-Arylthiazole Moieties

Zhou

Wang

et al. 2020

Molecules

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A series of new N-phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Their in vitro antibacterial activities were evaluated against three kinds of bacteria—Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac) and X.oryzae pv. oryzicola (Xoc)—showing promising results. The minimum 50% effective concentration (EC50) value of N-(4-((4-(4-fluoro-phenyl)thiazol-2-yl)amino)phenyl)acetamide (A1) is 156.7 µM, which is superior to bismerthiazol (230.5 µM) and thiodiazole copper (545.2 µM). A scanning electron microscopy (SEM) investigation has confirmed that compound A1 could cause cell membrane rupture of Xoo. In addition, the nematicidal activity of the compounds against Meloidogyne incognita (M. incognita) was also tested, and compound A23 displayed excellent nematicidal activity, with mortality of 100% and 53.2% at 500 μg/mL and 100 μg/mL after 24 h of treatment, respectively. The preliminary structure-activity relationship (SAR) studies of these compounds are also briefly described. These results demonstrated that phenylacetamide derivatives may be considered as potential leads in the design of antibacterial agents.

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“…[17] Bromides 17 a-d were obtained by Friedel-Crafts acylation of 15 a-d with bromoacetylb romide, [18] which was followed by reduction of the carbonyl group with the dimethylamineborane complex in the presence of titanium tetrachloride (Scheme 2). [19] Compound 17 e was prepared as outlined in Scheme 3. p-Hydroxyacetophenone was first alkylated by using n-heptyl bromide in the presence of K 2 CO 3 in DMF (70 8C), andt hen obtained phenyl ether 15 e was subjected to radicalb romination with CuBr 2 /EtOAc to afford desired bromoacetophenone 16 e. [20] Reduction of the carbonyl group in 16 e provided compound 17 e. As shown in Scheme 4, compounds 17 f and 17 g were prepared via intermediates 15 f and 15 g,w hichw ere obtained by aromaticn ucleophilic substitution of 2-chloro-4-fluoroacetophenonew ith p-(n-butyl)phenol and p-(n-butyl)thiophenol.…”

Section: Chemistrymentioning

confidence: 99%

Synthesis of N‐Substituted Iminosugar Derivatives and Evaluation of Their Immunosuppressive Activities

Song

Niu

et al. 2018

ChemMedChem

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It is important to find more effective and safer immunosuppressants, because clinically used immunosuppressive agents have significant side effects. A series of N-substituted iminosugar derivatives were designed and synthesized, and their immunosuppressive effects were evaluated by the CCK-8 assay. The results revealed that iminosugars 10 e and 10 i, that is, (3R,4S)-1-(4-heptyloxylphenylethyl)pyrrolidine-3,4-diol and (3R,4S)-1-[2-(2-chloro-4-(p-tolylthio)-phenyl-1-yl)ethyl]pyrrolidine-3,4-diol, respectively, exhibited the strongest inhibitory effects on mouse splenocyte proliferation (IC =2.16 and 2.48 μm, respectively), whereas the iminosugars containing an amide group near the hydrophilic head (compounds 10 j-n) exhibited no inhibitory effects. Further studies revealed that the inhibitory effects on splenocyte proliferation may have come from the suppression of both IFN-γ and IL-4 cytokines. Our results suggest that synthetic iminosugars, especially compounds 10 e and 10 i, hold potential as immunosuppressive agents.

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Synthesis and in-vitro evaluation of 2-amino-4-arylthiazole as inhibitor of 3D polymerase against foot-and-mouth disease (FMD)

Cited by 27 publications

References 35 publications

The Effect of Used Immunostimulating Drugs with FMD Vaccine on Immunoglobulins in Sheep

The Effect of Used Immunostimulating Drugs with FMD Vaccine on Immunoglobulins in Sheep

Synthesis and Antibacterial Evaluation of N-phenylacetamide Derivatives Containing 4-Arylthiazole Moieties

Synthesis of N‐Substituted Iminosugar Derivatives and Evaluation of Their Immunosuppressive Activities

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