Munikrishnappa C.S.,Rallis India Ltd |
Munikrishnappa C.S.,CMJ University |
Puranik S.B.,CMJ University |
Prasad Y.R.,Andhra University
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2016
A novel series of 4,5-dihydropyrazole derivatives (2a-d, 3, 4a-d and 5a-h) were synthesized by the reacting acetophenones and 5-(2,3-dichlorophenyl)furan-2-carbaldehyde. All the newly synthesized compounds were characterized using elemental analysis and spectral data (IR, 1H NMR, 13C NMR and LC-MS) analysis. All the synthesized derivatives were screened for antimicrobial potential against selected gram-positive, gram-negative bacteria, yeasts, moulds and in vitro cytotoxic activity against tumor cell lines by using Mosmann's method. Doxorubicin and cisplatin was utilized as positive control to validate biological evaluation. Antimicrobial study revealed fluorinated compounds 5a, 5b, 5d and 5f exhibited enhanced inhibition compared to other designed derivatives. Among the fluorinated derivatives, Compound 5b demonstrated significant activity against tested gram-positive and gram-negative bacteria and fungal species. The invitro anticancer screening of synthesized series illustrate that all the designed compounds were active, in particular tri flouro substituted Schiff base 5b exhibited excellent anticancer activity IC50 0.32 to 0.95 μm against tested cell lines in comparison to standard drugs Cisplatin and Doxorubicin.
Munikrishnappa C.S.,Rallis India Ltd |
Prasad Y.R.,Andhra University
European Journal of Medicinal Chemistry | Year: 2016
A novel series of 5-bromo-pyrimidine derivatives (5a-l, 6a-h, 9a-m and 10a-d) were synthesized through multi step reactions starting from 5-bromo-2,4-dichloro pyrimidine. The newly synthesized compounds were characterized using elemental analysis and spectral data (IR, 1H NMR, 13C NMR and LC-MS) analysis. The titled compounds were evaluated for their in vitro cytotoxic activity against tumor cell lines panel consisted of HCT116 (human colon cancer cell line), A549 (human lung cancer cell line), K562 (human chronic myeloid leukemia cell line), U937 (human acute monocytic myeloid leukemia cell line), and L02 (human normal cell line) by using MTT assay Mosmann's method. As most of the compounds are highly potent against K562 cells, all the synthesized compounds were evaluated for Bcr/Abl tyrosine kinase inhibitory activity by using well-established ADP-Glo assay method. Dasatinib was utilized as positive control to validate in both biological evaluations. The biological activity revealed that the compounds 5c, 5e, 6g, 9e, 9f and 10c were potent Bcr/Abl kinase inhibitors among the titled compounds. Thus these compounds may be promising lead compounds to be developed as an alternative for current Dasatinib therapy. © 2016 Elsevier Masson SAS.
PubMed | Rallis India Ltd and Andhra University
Type: | Journal: European journal of medicinal chemistry | Year: 2016
A novel series of 5-bromo-pyrimidine derivatives (5a-l, 6a-h, 9a-m and 10a-d) were synthesized through multi step reactions starting from 5-bromo-2,4-dichloro pyrimidine. The newly synthesized compounds were characterized using elemental analysis and spectral data (IR, (1)H NMR, (13)C NMR and LC-MS) analysis. The titled compounds were evaluated for their invitro cytotoxic activity against tumor cell lines panel consisted of HCT116 (human colon cancer cell line), A549 (human lung cancer cell line), K562 (human chronic myeloid leukemia cell line), U937 (human acute monocytic myeloid leukemia cell line), and L02 (human normal cell line) by using MTT assay Mosmanns method. As most of the compounds are highly potent against K562cells, all the synthesized compounds were evaluated for Bcr/Abl tyrosine kinase inhibitory activity by using well-established ADP-Glo assay method. Dasatinib was utilized as positive control to validate in both biological evaluations. The biological activity revealed that the compounds 5c, 5e, 6g, 9e, 9f and 10c were potent Bcr/Abl kinase inhibitors among the titled compounds. Thus these compounds may be promising lead compounds to be developed as an alternative for current Dasatinib therapy.
News Article | November 24, 2016
This report gives an in-depth analysis of crop protection industry in India. Crop protection is the science and practice of managing plant diseases, weeds and other pests (both vertebrate and invertebrate) that damage agricultural crops and forestry. Agricultural crops include field crops (maize, wheat, rice, etc.), vegetable crops (potatoes, cabbages, etc.) and fruits. The crops in field are exposed to many factors. Insects, birds, rodents, bacteria, etc may damage the crop plants. Crop protection encompasses Pesticide-based approaches such as herbicides, insecticides and fungicides. While farmers have been doing pest management since the onset of agricultural production, the discovery of the pesticidal properties of synthetic chemicals in the middle of the 20th century has transformed agriculture. Dichloro-Diphenyl-Trichloroethane (DDT) is perhaps the best known chemical pesticide. DDT was discovered as an insecticide in 1939 and was used extensively in agriculture, and for public health program. Subsequently, other insecticides, herbicides, and fungicides were developed. Their large-scale use started in farming in industrialized countries, resulting in large increases in production and/or cost savings on labor. The first Green Revolution, which began in the 1960s, made high yielding crop varieties available to developing countries, especially in Asia. Exploitation of the production potential of these varieties stimulated the use of fertilizer and pesticides. This dynamic led to large increases in food production in many countries but also to growing pesticide use. India is the fourth largest producer of agrochemicals globally, after United States, Japan and China. The Crop protection industry is a significant industry for the Indian economy. The Indian crop protection market grew with a CAGR of 4.46% between 2010 to 2015 India’s pesticides consumption is one of the lowest in the world with per hectare consumption of just 0.60 Kg compared to UK (5 Kg/ha) and Japan (12 Kg/ha). In India, paddy accounts for the maximum share of pesticide consumption, around 29%, followed by cotton 19%. Indian population is increasing and the per capita size of land decreasing, the use of pesticides in India has to improve further. Besides increasing in domestic consumption, the exports by the Indian Crop protection Industry can be doubled in the in coming years if proper strategies and sophisticated technologies are adopted by the industry. The Indian market will slowly see increased penetration of crop protection products, which will lead to higher yields. The industry is seeing various strategic alliances between the major players regarding research and development to come up with new molecules, as the cost is huge joining hands enables the market players to remain cost competitive. The competition will be slowly intensified, as the increasing awareness will generate the demand. Key Product Type • Insecticide • Herbicide • Fungicide • Bio-pesticide • Others 1. Executive Summary 2. Global Crop Protection Market Outlook 2.1. Market Size By Value 2.2. Market Size By Volume 2.2.1. Overall Market 2.2.2. Herbicides Market 2.2.3. Fungicides Market 2.2.4. Insecticides Market 2.2.5. By Region 188.8.131.52. Europe Crop Protection Market 184.108.40.206. Asia Crop Protection Market 220.127.116.11. Latin America Crop Protection Market 18.104.22.168. North America Crop Protection Market 2.3. Market Share 2.3.1. By Region 2.3.2. By Product Type 2.3.3. By Crop 3. India Crop Protection Market Outlook 3.1. Market Size By Value 3.2. Market Size By Volume 3.2.1. Overall Market 3.2.2. Insecticide Market 3.2.3. Herbicide Market 3.2.4. Fungicide Market 3.2.5. Bio-pesticide Market 3.3. Market Share 3.3.1. By Company 3.3.2. By State 3.3.3. By Product Type 3.3.4. By Crop 3.4. Production 4. India Economic Snapshot 5. Market Penetration 6. Raw Material 7. Manufacturing Process 8. Policy & Regulatory Landscape 9. PEST Analysis 10. Trade Dynamics 10.1. Import 10.2. Export 11. Channel Partner Analysis 12. India Crop Protection Market Dynamics 12.1. Key Drivers 12.2. Key Challenges 13. Market Trends & Developments 13.1. Increased Demand for Food Safety and Quality 13.2. Mounting Cost of Research & Development 13.3. Adoption of Genetically Modified Crops and Bio Pesticides 13.4. Companies Shifting Focus from Agrochemical to Agriculture 13.5. Integrated Pest Management for Enhancing Yields 13.6. Leading Players Working Towards Brand Building 14. Competitive Landscape 14.1. Porters Five Forces 14.2. Company Profiles 14.2.1. Bayer CropScience Ltd. 14.2.2. PI Industries Ltd. 14.2.3. Dhanuka Agritech Ltd. 14.2.4. Mosanto India Ltd. 14.2.5. Rallis India Ltd. 14.2.6. UPL Limited, India 14.2.7. Syngenta 14.2.8. Insecticides India Ltd. 14.2.9. E.I.DuPont India Private Limited 14.2.10. BASF India Limited 15. Strategic Recommendations 16. Disclaimer
Hosmani R.S.,Syngenta |
Nayak S.P.,Mangalore University |
Kumar Y.,Rallis India Ltd
Quality Assurance and Safety of Crops and Foods | Year: 2012
Introduction: Kresoxim-methyl is a broad spectrum fungicide used for controlling sheath blight and blast in paddy, also downy and powdery mildew diseases in grapes. Objectives: A supervised field trial consisting of two experiments viz. soil application and foliar application was conducted in order to study the uptake, distribution, translocation and metabolism of kresoxim-methyl in paddy, treated at the rates of 250 and 500 g a.i. ha-1. Methods: Depending on the crop growth and stage (40, 60, 80 and 110 days after transplanting), different plant parts like foliage, shoot, roots, panicles, straw and grain, along with soil, were sampled and analysed using liquid chromatography tandem mass spectrometry for parent compound kresoxim-methyl and its metabolites. Results: The results of the study revealed that there was little translocation of residues of kresoxim-methyl and its acid metabolite to various plants parts, i.e. foliage, roots, soil, shoot and panicle, and very little to straw and grains. Conclusion: The major route of metabolism was hydrolysis with formation of acid metabolite. © 2012 Blackwell Publishing Ltd.
Dey D.,Indian Institute of Science |
Mohan T.P.,Rallis India Ltd. |
Vishalakshi B.,Mangalore University |
Chopra D.,Indian Institute of Science
Crystal Growth and Design | Year: 2014
A comprehensive analysis of the crystal packing and the energetic features of a series of four biologically active molecules belonging to the family of substituted 4-(benzylideneamino)-3-(4-fluoro-3-phenoxyphenyl)-1H-1,2,4-triazole-5-(4 H )-thione derivatives have been performed based on the molecular conformation and the supramolecular packing. This involves the formation of a short centrosymmetric R2 2(8) N-H⋯S supramolecular synthon in the solid state, including the presence of C-H⋯S, C-H⋯O, C-H⋯N, C-H⋯F, C-H⋯Cl, C-F⋯F-C, C-Cl⋯Cl-C, and C-H⋯π intermolecular interactions along with π-π stacking to evaluate the role of noncovalent interactions in the crystal. The presence of such synthons has a substantial contribution toward the interaction energy (-18 to -20 kcal/mol) as obtained from the PIXEL calculation, wherein the Coulombic and polarization contribution are more significant than the dispersion contribution. The geometrical characteristics of such synthons favor short distance, and the population of related molecules having these geometries is rare as has been obtained from the Cambridge Structural Database (CSD). Furthermore, their interaction energies have been compared with those present in our molecules in the solid state. The topological characteristics of the N-H⋯S supramolecular synthon, in addition to related weak interactions, C-H⋯N, C-H⋯Cl, C-F⋯F-C, and C-Cl⋯Cl-C, have been estimated using the quantum theory of atoms in molecules (QTAIM). In addition, an analysis of the Hirshfeld surface and associated fingerprint plots of these four molecules also have provided a platform for the evaluation of the contribution of different atom⋯atom contacts, which contribute toward the packing of the molecules in solids. (Figure Presented). © 2014 American Chemical Society.
Shukla R.,Indian Institute of Science |
Mohan T.P.,Rallis India Ltd |
Vishalakshi B.,Mangalore University |
Chopra D.,Indian Institute of Science
CrystEngComm | Year: 2014
In the present study, we have synthesized and characterized two biologically active 1,2,4-triazole derivatives, a fluoro derivative, namely (E)-3-(4-fluoro-3-phenoxyphenyl)-4-((4-fluorobenzylidene)amino) -1-(morpholinomethyl)-1H-1,2,4-triazole-5(4H)-thione (TRZ-1), and a chloro derivative, namely (E)-4-((4-chlorobenzylidene)amino)-3-(4-fluoro-3- phenoxyphenyl)-1-(morpholinomethyl)-1H-1,2,4-triazole-5(4H)-thione (TRZ-2), via single crystal and powder X-ray diffraction. The chloro derivative crystallizes in an anhydrous form (TRZ-2A) and a solvated one (TRZ-2B) due to the presence of a toluene molecule in the crystal. This solvatomorphic behavior has been studied in detail using different thermal techniques, namely DSC and TGA, combined with hot stage microscopy (HSM). All of the three crystal structures show the presence of different intermolecular interactions of the type C-H⋯O, C-H⋯SC, C-H⋯π, C-H⋯X (X = -F, -Cl), π⋯π and lp⋯π interactions. The fingerprints for all these interactions were evaluated using Hirshfeld surfaces. The nature and energetics associated with these interactions were characterized using PIXEL and supported by ab initio quantum mechanical calculations using TURBOMOLE. In addition, the calculations performed on the evaluation of the electrostatic potential provide deeper insights into the nature of lp⋯π interactions. This journal is © The Royal Society of Chemistry.
Gajbhiye V.T.,Indian Agricultural Research Institute |
Gupta S.,Indian Agricultural Research Institute |
Mukherjee I.,Indian Agricultural Research Institute |
Singh S.B.,Indian Agricultural Research Institute |
And 3 more authors.
Bulletin of Environmental Contamination and Toxicology | Year: 2011
Persistence of azoxystrobin was studied in/on grapes when applied @ 150 g ai ha -1 (recommended dose) and 300 g ai ha -1 (double the recommended dose) in three grapes growing states of India, namely Karnataka, Maharashtra and Tamil Nadu, in the year 2006-2007. A total of five sprays were given at an interval of about 15 days. Grapes and soil samples were collected after 5th spray, extracted and analysed by gas chromatography using electron capture detector. Half life of azoxystrobin on grapes varied from 5.4 to 11.2 days. Residues of azoxystrobin were much below the prescribed MRL (0.5 mg kg -1) after 21 days. The dissipation of azoxystrobin in soil followed first order rate kinetics with an average half life of 8.1 days at the recommended dose of application. © 2010 The Author(s).
Bio-efficacy and phytotoxicity of new fungicide formulation: TAQAT 75% WP (Captan 70% + hexaconazole 5%) RIL 004/F1 75% WP against downy mildew and powdery mildew diseases on grapes in northern Karnataka
Jamadar M.M.,University of Agricultural Sciences, Dharwad |
Mallikarjunappa S.,Rallis India Ltd. |
Kendappa G.N.,Rallis India Ltd.
Pestology | Year: 2013
A new Rallis India Ltd. fungicide formulation: TAQAT 75% WP (RIL-004/F1 75% WP) a combination product of captan 70% + hexaconazole 5% was evaluated for its bio-efficacy and phytotoxicity against downy mildew and powdery mildew of grapes for two seasons at Horticulture Research Station, (Tidagundi) Bijapur during 2008-09 and 2009-10. The results indicated the superiority of combination product: captan 70% + hexaconazole 5% at 2.0 g/1 in management of both downy mildew and powdery mildew reducing the disease by more than 74.9 and 62.7 per cent respectively vis-à-vis other chemical formulations without any phytotoxic effects.
RALLIS INDIA Ltd | Date: 2013-04-12
The present disclosure provides process for preparation of azimsulfuron or its salts, isomers, and other derivatives thereof. The process involves treating a compound of formula I, with aqueous acetic acid or formic acid and chlorine gas or sodium hypochlorite in presence of hydrochloric acid in chlorinated solvents such as dichloromethane, 1,2-dichloroethane or with aqueous acetic acid and N-chlorosuccinimide or hydrogen peroxide in presence of hydrochloric acid in aqueous cyclic ether such as tetrahydrofuran, 1,4-dioxane to obtain 1-methyl-4-(2-methyl-2H-tetrazol-5-yl)-1H-pyrazole-5-sulfonyl chloride; converting the sulfonyl chloride to a sulfonamide and treating the sulfonamide with a phenyl(4,6-dimethoxypyrimidin-2-yl) carbamate to obtain azimsulfuron or its salts, isomers, and other derivatives thereof.