Developing Global Leaders for Research, Regulation, and Stewardship of Crop Protection Chemistry in the 21st Century

To provide sufficient food and fiber to the increasing global population, the technologies associated with crop protection are growing ever more sophisticated but, at the same time, societal expectations for the safe use of crop protection chemistry tools are also increasing. The goal of this perspective is to highlight the key issues that face future leaders in crop protection, based on presentations made during a symposium titled “Developing Global Leaders for Research, Regulation and Stewardship of Crop Protection Chemistry in the 21st Century”, held in conjunction with the IUPAC 13th International Congress of Pesticide Chemistry in San Francisco, CA, USA, during August 2014. The presentations highlighted the fact that leaders in crop protection must have a good basic scientific training and understand new and evolving technologies, are aware of the needs of both developed and developing countries, and have good communication skills. Concern is expressed over the apparent lack of resources to meet these needs, and ideas are put forward to remedy these deficiencies.Keywords: sustainable agriculture, developing regions, training leaders, smart systems, stewardship, women in agriculture, crop protection, universities, nanopesticides, communications, GM crop

Essential oil composition, antifungal, and seedling growth inhibitory effects of zerumbone from <i>Zingiber zerumbet</i> Smith

<p>The composition of the essential oil isolated from the rhizomes of <i>Zingiber zerumbet</i> Smith was determined using GC and GC–MS. Zerumbone (74.82%), humulene (6.02%), and β-copaen-4α-ol (4.32%) were identified as major compounds. <i>E</i>-Bisabol-11-ol (4.32%), <i>E</i>-bisabol-11-ol (0.92%), β-sinensal (0.57%), and α-himachalene oxide (0.19) were reported for the first time in its oil. Zerumbone was further isolated from the crude mixture of oil and identified by FTIR, NMR (¹H, ¹³C, DEPT, HXCO, and HMBC), and mass (EI-MS) spectral data. Zerumbone showed promising antifungal activity against three phytopathogenic fungi, namely <i>Rhizoctonia solani</i> (EC₅₀, 39.6 ppm), <i>Sclerotium rolfsii</i> (EC₅₀, 59.3 ppm), and <i>Macrophomina phaseolina</i> (EC₅₀, 147.4 ppm) compared with hexaconazole (EC₅₀, 18.3, 13.4, and 4.5 ppm, respectively). Zerumbone has also shown concentration-dependent affect on seedling growth of <i>Phalaris minor</i> Retz., compared with control and <i>Triticum aestivum</i> L. (wheat). Zerumbone strongly suppressed the root and shoot growth of <i>P. minor</i> seedling at 1000 ppm compared with control and wheat. It exhibited no or less effect on the germination of seeds of <i>T. aestivum</i>.</p

Not Available

Not AvailableA new microwave method (MM) has been developed for the synthesis of a series of 16 substituted ferrocenyl chalcones using acetylferrocene (1) with different aldehydes (2a-2p) and comparing it with conventional method (CM). The synthesized compounds were characterized by various spectroscopic techniques viz IR, HR-MS, 1H NMR, and 13C NMR. The time required for completion of reaction in MM varied from 1 to 5min as compared to CM which required 10–40 h. All the synthesized compounds were screened for antifungal activity against Sclerotium rolfsii and Alternaria solani. In vitro fungicidal activity revealed that compound 3o (ED50 = 23.24mg L−1) was found to be most active against S. rolfsii. But in case of A. solani, compound 3c (ED50 = 29.9mg L−1) showed highest activity. The nematicidal activity revealed that the compound 3b was more potent with LC50 values of 10.67, 7.30, and 4.55 ppm at 24, 48, and 72 h, respectively. 2D-Quantitative Structural Activity Relationship (2D-QSAR) analysis of these ferrocenyl chalcones was carried out by developing three different models namely Partial Least Squares (PLS, Model 1), Multiple Linear Regression (MLR, Model 2) and Principal Component Regression (PCR, Model 3). Statistical significance and predictive ability of these models were assessed by internal and external validation and also verified by leave one-out cross-validation. QSAR study revealed that MLR for S. rolfsii (r2 = 0.999, q2 = 0.996), PLS for A. solani (r2 = 0.934, q2 = 0.749) and PCR for M. incognita (r2 = 0.878, q2 = 0.772) were the best model. The physico-chemical parameters were calculated using VLife MDS 4.6 software. QSAR study could be employed for structure optimization to achieve better activity.Not Availabl

Not Available

Not AvailableThe present study reports, bioefficacy evaluation of effective compounds against Meloidogyne incognita and Sclerotium rolfsii in pot cultured tomato. The identified five most effective compounds, i.e. (2E)-1-(4-Methylphenyl)-3-ferrocenyl-prop-2-en-1-one (6g), (2E)-1-(4-Methoxyphenyl)-3-ferrocenyl-prop-2-en-1-one (6h), (2E)-1-(3-Bromophenyl)-3-ferrocenyl-prop-2-en-1-one (6j), (2E)-1-(2,4-Dichlorophenyl)-3-ferrocenyl-prop-2-en-1-one (6k) and (2E)-1-(3,5-Dichloro-2-hydroxyphenyl)-3-ferrocenyl-prop-2-en-1-one (6p) along with Carbofuran 3G as positive control were tested at 20, 40 and 80 ppm by soil drenching and root dipping methods. The study revealed that all plant growth parameters were positively influenced by these compounds. The presence of an electron releasing group positively influenced the efficacy, and the activity was highest in compounds 6g and 6h at 80 ppm. Based on in vitro results against S. rolfsii, (2E)-1-Ferrocenyl-3-(4-bromophenyl)-prop-2-en-1-one (3b), (2E)-1-Ferrocenyl-3-(2,6-dichlorophenyl)-prop-2-en-1-one (3o) and (2E)-1-(5-Chloro-2-hydroxyphenyl)-3-ferrocenyl-prop-2-en-1-one (6o) along with Tebuconazole 25.9% EC and Hexaconazole 5% SC as positive control were evaluated. The shoot length was found to be highest (24.50 cm) in plants treated with 3b followed by 3o and 6o at 1000 ppm. The percent disease incidence was significantly decreased as compared to control. The percent disease incidence was found to be minimum in plants treated with 3b at 1000 ppm. However, root dipping was not as effective as soil drenching. Therefore, ferrocenyl chalcone derivatives proved to be of great fungicidal and nematicidal potential opening new opportunities for expanding their effectiveness as new pest control agents.Not Availabl

Synthetic, biocatalytic acetylation and anti-tuberculosis activity evaluation studies on (±) -4-alkyl-3,4-dihydro-3-ω-hydroxyalkyl-2<i>H</i>-1 ,3-benzoxazines^¶

1958-1969Five novel (±)-4-alkyl-3,4-dihydro-3-ω-hydroxyalkyl-2H-1,3-benzoxazines have been synthesized by Mannich-type condensation of N-ω-hydroxyalkyl, N-[1-(2-hydroxypheny l)ethyl/propyl]amine and formaldehyde in 55 to 60% yields. Porcine pancreatic lipase in tetrahydrofuran catalyses the acetylation of these benzoxazines in an enantioselective fashion. This perhaps is the first report of the resolution of benzoxazines involving the primary alcoholic group situated far away from the asymmetric center as a remote handle for chiral recognition by porcine pancreatic lipase. The activity of 4-alkyl-3,4-dihydro-3-ω hydroxyalkyl -2H-1,3-benzoxazines and their precursors, i. e. secondary amines and corresponding Schiffs bases have been evaluated for the inhibition of Mycobacterium tuberculosis.</i

The root endophyte fungus Piriformospora indica leads to early flowering, higher biomass and altered secondary metabolites of the medicinal plant, Coleus forskohlii

This study was undertaken to investigate the influence of plant probiotic fungus Piriformospora indica on the medicinal plant C. forskohlii. Interaction of the C. forskohlii with the root endophyte P. indica under field conditions, results in an overall increase in aerial biomass, chlorophyll contents and phosphorus acquisition. The fungus also promoted inflorescence development, consequently the amount of p-cymene in the inflorescence increased. Growth of the root thickness was reduced in P. indica treated plants as they became fibrous, but developed more lateral roots. Because of the smaller root biomass, the content of forskolin was decreased. The symbiotic interaction of C. forskohlii with P. indica under field conditions promoted biomass production of the aerial parts of the plant including flower development. The plant aerial parts are important source of metabolites for medicinal application. Therefore we suggest that the use of the root endophyte fungus P. indica in sustainable agriculture will enhance the medicinally important chemical production

Synthesis, characterization and in vitro anti-invasive activity screening of polyphenolic and heterocyclic compounds

Invasion is the hallmark of malignant tumors, and is responsible for the bad prognosis of the untreated cancer patients. The search for anti-invasive treatments led us to screen compounds of different classes for their effect in an assay for invasion. Thirty-nine new compounds synthesized in the present study along with 56 already reported compounds belonging mainly to the classes of lactones, pyrazoles, isoxazoles, coumarins, desoxybenzoins, aromatic ketones, chalcones, chromans, isoflavanones have been tested against organotypic confronting cultures of invasive human MCF-7/6 mammary carcinoma cells with embryonic chick heart fragments in vitro. Three of them (a pyrazole derivative, an isoxazolylcoumarin and a prenylated desoxybenzoin) inhibited invasion at concentrations as low as 1 muM; instead of occupying and replacing the heart tissue within 8 days, the MCF-7/6 cells grew around the heart fragments and left it intact, when treated with these compounds. At the anti-invasive concentration of 1 muM, the three compounds did not affect the growth of the MCF-7/6 cells, as shown in the sulforhodamine B assay. Aggregate formation on agar was not stimulated by any of the three anti-invasive compounds, making an effect on the E-cadherin/catenin complex improbable. This is an invasion suppressor that can be activated in MCF-7/6 cells by a number of other molecules. Our data indicate that some polyphenolic and heterocyclic compounds are anti-invasive without being cytotoxic for the cancer cells. (C) 2003 Elsevier Science Ltd. All rights reserved