scholarly journals Investigation of Novel Pesticides with Insecticidal and Antifungal Activities: Design, Synthesis and SAR Studies of Benzoylpyrimidinylurea Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2203 ◽  
Author(s):  
Peiqi Chen ◽  
Xiangmin Song ◽  
Yongmei Fan ◽  
Weihao Kong ◽  
Hao Zhang ◽  
...  
Keyword(s):  
Phytopathogenic Fungi ◽  
Design Synthesis ◽  
Antifungal Activities ◽  
In Vivo Experiments ◽  
Sar Studies ◽  
Low Toxicity ◽  
Inhibitory Activities ◽  
Commercial Pesticide ◽  
Pipiens Pallens

In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 µg mL−1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 µg mL−1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.

scholarly journals Effect of some ent -Kaurenes on the Viability of Human Peripheral Blood Mononuclear Cells

2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700
Author(s):  
Yndra Cordero ◽  
Grecia M. Corao ◽  
José A. Cova ◽  
Alfredo Usubillaga
Keyword(s):  
Peripheral Blood ◽  
Mononuclear Cells ◽  
Human Peripheral Blood ◽  
Peripheral Blood Mononuclear ◽  
Toxic Compounds ◽  
Future Studies ◽  
In Vivo Experiments ◽  
Human Mononuclear Cells ◽  
Low Toxicity

The possible cytotoxic activity of some ent-kaurenes on human mononuclear cells, obtained from peripheral blood, was studied having in mind future studies on their antitumor activity. The cells were obtained using the Ficoll-Hypaque method, adjusted to 2×106cells/mL, and incubated with kaurenes for 48 hours at 3×10-5, 30×10−5, 300×10−5 and 3000×10−5μmol/well. Ent-kaurenic acid showed no toxicity at all concentrations studied. The least toxic of all the kaurene derivatives studied was ent -15,16-epoxy-17-acetoxy-(-)-kauran-19-oic acid, with a cellular viability of 99% at 3×10−5μmol/well, and 94% at 30×10−5μmol/well. Another compound that showed low toxicity was the 2,3,4,6-tetra-acetyl-α-D-pyranosyl ester of ent-15-oxo-(-)-kaur-16-en-19-oic acid with 44% viability at 3000×10−5Vmol/well. The most toxic compounds at all concentrations tested were ent-kaur-16-en-19-ol acetate and ent-16α-hydroxy-(-)-kauran-19-oic acid. On the other hand, ent-kaur-9(11)16-dien-19-oic acid, ent-kauran-19-oic acid, and ent-kaur-16-en-19-ol were toxic only at the highest concentration studied. According to these results, and considering the concentrations employed, ent-kaur-16-en-19-oic acid and ent-15,16-epoxy-17-acetoxy-(-)-kauran-19-oic acid could be used for in vivo experiments and possibly for therapeutic purposes on humans, without much risk.

scholarly journals Discovery of Cysteine and Its Derivatives as Novel Antiviral and Antifungal Agents

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 383
Author(s):  
Shan Yang ◽  
Tienan Wang ◽  
Yanan Zhou ◽  
Li Shi ◽  
Aidang Lu ◽  
...  
Keyword(s):  
Virus Assembly ◽  
Alternaria Solani ◽  
Phytopathogenic Fungi ◽  
Cercospora Arachidicola ◽  
Antifungal Activities ◽  
Inhibitory Rate ◽  
Commercial Plant ◽  
Protection Activity

Based on the structure of the natural product cysteine, a series of thiazolidine-4-carboxylic acids were designed and synthesized. All target compounds bearing thiazolidine-4-carboxylic acid were characterized by 1H-NMR, 13C-NMR, and HRMS techniques. The antiviral and antifungal activities of cysteine and its derivatives were evaluated in vitro and in vivo. The results of anti-TMV activity revealed that all compounds exhibited moderate to excellent activities against tobacco mosaic virus (TMV) at the concentration of 500 μg/mL. The compounds cysteine (1), 3–4, 7, 10, 13, 20,23, and 24 displayed higher anti-TMV activities than the commercial plant virucide ribavirin (inhibitory rate: 40, 40, and 38% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively), especially compound 3 (inhibitory rate: 51%, 47%, and 49% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively) with excellent antiviral activity emerged as a new antiviral candidate. Antiviral mechanism research by TEM exhibited that compound 3 could inhibit virus assembly by aggregated the 20S protein disk. Molecular docking results revealed that compound 3 with higher antiviral activities than that of compound 24 did show stronger interaction with TMV CP. Further fungicidal activity tests against 14 kinds of phytopathogenic fungi revealed that these cysteine derivatives displayed broad-spectrum fungicidal activities. Compound 16 exhibited higher antifungal activities against Cercospora arachidicola Hori and Alternaria solani than commercial fungicides carbendazim and chlorothalonil, which emerged as a new candidate for fungicidal research.

scholarly journals Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Fluconazole-Based Compounds with Promising Antifungal Activities

ACS Omega ◽  
2021 ◽  
Author(s):  
Mohammad Shafiei ◽  
Hossein Toreyhi ◽  
Loghman Firoozpour ◽  
Tahmineh Akbarzadeh ◽  
Mohsen Amini ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Antifungal Activities

Development of a multifunctional gold nanoplatform for combined chemo-photothermal therapy against oral cancer

Nanomedicine ◽  
2020 ◽  
Vol 15 (7) ◽  
pp. 661-676 ◽  
Author(s):  
Zengying Liu ◽  
Jianbo Shi ◽  
Bangshang Zhu ◽  
Qin Xu
Keyword(s):  
Drug Delivery ◽  
Oral Cancer ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Antitumor Efficacy ◽  
Antitumor Effects ◽  
In Vivo Experiments ◽  
Low Toxicity

Aim: To design and fabricate a multifunctional drug-delivery nanoplatform for oral cancer therapy. Materials & methods: Polyethylene glycol-stabilized, PDPN antibody (PDPN Ab)- and doxorubicin (DOX)-conjugated gold nanoparticles (AuNPs) were prepared and evaluated for their cytotoxicity and antitumor efficacy in both chemotherapy and photothermal therapy. Results: The obtained (PDPN Ab)-AuNP-DOX system presents low toxicity, a high drug loading capacity and cellular uptake efficiency. Both in vitro and in vivo experiments demonstrate that (PDPN Ab)-AuNP-DOX has enhanced antitumor efficacy. Treatment with (PDPN Ab)-AuNP-DOX combined with laser irradiation exhibits superior antitumor effects. Conclusion: This (PDPN Ab)-AuNP-DOX system may be used as a versatile drug-delivery nanoplatform for targeted and combined chemo-photothermal therapy against oral cancer.

Design, Synthesis and Antifungal Activities of 6‐Substituted 3‐Butylphthalide Derivatives against Phytopathogenic Fungi

2020 ◽  
Vol 17 (10) ◽  
Author(s):  
Yong Li ◽  
Zhongfu Luo ◽  
Bilan Luo ◽  
Qing Lan ◽  
Judi Fan ◽  
...  
Keyword(s):  
Phytopathogenic Fungi ◽  
Design Synthesis ◽  
Antifungal Activities

scholarly journals Engineering a highly elastic human protein–based sealant for surgical applications

2017 ◽  
Vol 9 (410) ◽  
pp. eaai7466 ◽  
Author(s):  
Nasim Annabi ◽  
Yi-Nan Zhang ◽  
Alexander Assmann ◽  
Ehsan Shirzaei Sani ◽  
George Cheng ◽  
...  
Keyword(s):  
Blood Circulation ◽  
Poor Performance ◽  
Human Protein ◽  
Adhesion Properties ◽  
In Vivo Experiments ◽  
Low Toxicity ◽  
Surgically Induced ◽  
Surgical Sealants

Surgical sealants have been used for sealing or reconnecting ruptured tissues but often have low adhesion, inappropriate mechanical strength, cytotoxicity concerns, and poor performance in biological environments. To address these challenges, we engineered a biocompatible and highly elastic hydrogel sealant with tunable adhesion properties by photocrosslinking the recombinant human protein tropoelastin. The subcutaneous implantation of the methacryloyl-substituted tropoelastin (MeTro) sealant in rodents demonstrated low toxicity and controlled degradation. All animals survived surgical procedures with adequate blood circulation by using MeTro in an incisional model of artery sealing in rats, and animals showed normal breathing and lung function in a model of surgically induced rat lung leakage. In vivo experiments in a porcine model demonstrated complete sealing of severely leaking lung tissue in the absence of sutures or staples, with no clinical or sonographic signs of pneumothorax during 14 days of follow-up. The engineered MeTro sealant has high potential for clinical applications because of superior adhesion and mechanical properties compared to commercially available sealants, as well as opportunity for further optimization of the degradation rate to fit desired surgical applications on different tissues.

Rationale design, synthesis, and pharmacological evaluation of isatin analogues as antiseizure agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Sandip Firke ◽  
Rameshwar Cheke ◽  
Vinod Ugale ◽  
Saurabh Khadse ◽  
Manish Gagarani ◽  
...  
Keyword(s):  
Amino Acids ◽  
Anticonvulsant Activity ◽  
Structural Features ◽  
Spectroscopic Techniques ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
In Vivo Experiments ◽  
Mes Test ◽  
Seizure Models

Background: Epilepsy is one of the most common and devastating neurological disease affecting about 1% of the world’s population at any time. Herein, we have reported rationale design and synthesis of 5-acetyl-3-((4-substitutedphenyl)imino)indolin-2-one analogues 3(a-k) as antiseizure agents. Objective: These analogues were designed as four component pharmacophoric model by clubbing structural fragments of potent antiepileptic drugs. Aim of this study was to synthesize structurally designed isatin analogues and screened them for anticonvulsant activity and neurotoxicity. Methods: Designed derivatives were synthesized using bulky scale feasible and inexpensive microwave methodology. All the synthesized compounds were then characterized by multiple spectroscopic techniques and screened for anticonvulsant activity through preclinical in-vivo experiments. Results: The compound 3d have exhibited good anticonvulsant activity in preclinical seizure models with better toxicity profile when compared to standard drugs (3d: ED50 = 31.5 mg/kg, MES test; ED50 = 37.4 mg/kg, scPTZ test; TD50 = 384.3 mg/kg,). Compound 3d have also shown good binding affinity at crucial amino acids of GluN1 subunit of NMDAR (Docking score = -9.30) and fit adequately in the cavity of receptor (Amino acids involved and H-bonding distance = GLY93: acetyl >C=O, 2.38Å; PHE92: acetyl >C=O, 2.22Å; and THR26: >C=O of isatin, 1.71Å). Results of molecular docking supported the structural features present over isatins to persuade potent antiseizure activity. Conclusion: Rationale designing strategy, in-vivo pharmacological profile, and computational studies make us to anticipate the emergence of these molecules as novel antiseizure agents which can be further explored to develop probes for the treatment of epilepsy.

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