scholarly journals Design, Synthesis and Biological Activity of New Strobilurin Derivatives with a 1H-Pyrazol-5-oxy Side Chain

2009 ◽  
Vol 4 (9) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Miao Li ◽  
Chang-Ling Liu ◽  
Ji-Chun Yang ◽  
Lin Li ◽  
Zhi-Nian Li ◽  
...  
Keyword(s):  
Biological Activity ◽  
Powdery Mildew ◽  
Fungicidal Activity ◽  
Green Peach Aphid ◽  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
H Nmr ◽  
Elemental Analyses ◽  
Cucumber Downy Mildew

A series of new strobilurin derivatives with a substituted pyrazole side chain (5 and 6) were designed and synthesized. The new derivatives were synthesized from substituted phenones as starting material via esterification, cyclization and condensation reactions. All compounds were identified by 1H NMR and IR spectral and elemental analyses. Preliminary biological evaluation showed that some of the compounds had good fungicidal activity against cucumber downy mildew (CDM) and wheat powdery mildew (WPM) at 6.25 and 1.56 mg L−1, respectively. Some of the compounds showed insecticidal activity against armyworm (AW), green peach aphid (GPA) and culex mosquitoes at 600 mg L−1.

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

Design, synthesis and biological evaluation of cyclic angiotensin II analogues with 3,5 side-Chain bridges

2002 ◽  
Vol 12 (18) ◽  
pp. 2627-2633 ◽  
Author(s):  
Panagiota Roumelioti ◽  
Ludmila Polevaya ◽  
Panagiotis Zoumpoulakis ◽  
Nektarios Giatas ◽  
Ilze Mutule ◽  
...  
Keyword(s):  
Angiotensin Ii ◽  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
Angiotensin Ii Analogues ◽  
Synthesis And Biological Evaluation

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

scholarly journals Design, Synthesis, Antibacterial and Antifungal Activity of Novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones

2012 ◽  
Vol 9 (3) ◽  
pp. 1481-1489
Author(s):  
Anisetti Ravinder Nath ◽  
Malladi Srinivas Reddy
Keyword(s):  
Antifungal Activity ◽  
Knoevenagel Condensation ◽  
Catalytic Amount ◽  
The Novel ◽  
Plate Method ◽  
Design Synthesis ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal

The novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones (4a-j) analogs were synthesized by Knoevenagel condensation of a solution of 2-methyl-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4-dihydro-4-quinazolinone (3) with aromatic aldehyde in presence of catalytic amount of piperidine. Compounds (4a-j) showed significant biological activity against all the standard strains. All the synthesized compounds were characterized on the basis of their IR,1H NMR, MASS spectroscopic data and elemental analyses. All the compounds have been tested for antimicrobial and antifungal activity by the cup-plate method.

Design, Synthesis, Molecular Docking and Biological Evaluation of Bromo-Pyridyl Containing 3-Chloro 2-Azetidinone Derivatives as Potential Antimycobacterial Agents

2021 ◽  
Author(s):  
Rakesh V. Kusurkar ◽  
Rahul H. Rayani ◽  
Anand G. Vala ◽  
Deepa R. Parmar ◽  
Manoj N Bhoi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antitubercular Activity ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Dynamics Simulation ◽  
Design Synthesis ◽  
H Nmr ◽  
New Class ◽  
Lactam Ring ◽  
C Nmr

Abstract A new class of β-lactam pharmacophore series of 2-Bromo-N-[4-(2-{[2-(substituted phenyl)-3-chloro-4-oxoazetidin-1-yl] amino}-2-oxoethyl) phenyl] pyridine-4-carboxamide derivatives were designed, prepared, and screened for their antimycobacterial activities. The hydrazone derivatives were first synthesized via conventional and microwave methods, and then the β-lactam ring could be constructed via a [2+2] ketenimine cycloaddition. The structure of all synthesized compounds was characterized by FTIR, 1H NMR, 13C NMR, and Mass spectroscopy techniques. All the newly synthesized derivatives were found to be effective in inhibiting M. tuberculosis H37RV strain infection at concentrations of 12.5, 25.0, and 50.0 µg/mL using the MABA method. Amongst, the compound (6e) was found to be good potent antitubercular activity at 12.5 mg/mL concentration in comparison with the rest of the compounds using the standard therapeutic agent Streptomycin. Molecular dynamics simulation studies and Molecular docking studies have been performed against mycobacterial InhA enzyme to gain an insight into the possible mechanistic action in search of good potent antitubercular candidates.

Design, Synthesis, and Fungicidal Activity of Macrolactones and Macrolactams with a Sulfonamide Side Chain

2008 ◽  
Vol 56 (15) ◽  
pp. 6547-6553 ◽  
Author(s):  
Wei-Juan Zhu ◽  
Peng Wu ◽  
Xiao-Mei Liang ◽  
Yan-Hong Dong ◽  
Jian-Jun Zhang ◽  
...  
Keyword(s):  
Fungicidal Activity ◽  
Side Chain ◽  
Design Synthesis

scholarly journals Design Synthesis and Biological Evaluation of NovelN-Nitro Acid Amide Derivatives as Lead Compounds of Herbicide

2016 ◽  
Vol 2016 ◽  
pp. 1-6
Author(s):  
Xiaojuan Qi ◽  
Wenjie Tang ◽  
Shan Gao ◽  
Min Gao ◽  
Changshui Chen ◽  
...  
Keyword(s):  
Acid Amide ◽  
Biological Evaluation ◽  
Herbicidal Activity ◽  
Acetohydroxyacid Synthase ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Amide Derivatives ◽  
Sorghum Sudanense ◽  
Synthesis And Biological Evaluation

A series ofN-nitro acid amide derivatives compounds were synthesized based on the active site of target acetohydroxyacid synthase (AHAS, EC: 2.2.1.6) enzyme. All the structures of newly prepared compounds were thoroughly characterized by satisfied IR and1H NMR spectra. The IC50values against AHAS enzyme and EC50values for herbicidal activity againstAmaranthus mangostanus L.andSorghum sudanenseof all synthesized target compounds were determined. The compoundsII-10,II-21, andII-22with IC50values of 7.09 mg/L, 9.07 mg/L, and 9.11 mg/L and the compoundsII-8andII-22with EC50values of 9.87 mg/L and 19.88 mg/L against root ofAmaranthus mangostanus L.andSorghum sudanensewere illustrated, respectively. Meanwhile, the possible reasons for the lower activity of compounds were analyzed by molecular docking prediction.

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