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Chinese Chemical Letters 2014年第5期25卷 732-736页

作者： Satish Gaddam Harshavardhan Reddy Kasireddy Karnakar Konkala Ramesh Katla Nageswar Yadavalli Venkata Durga CSIR-medicinal chemistry and Pharmacology division Indian Institute of Chemical Technology

A simple and practical method for the synthesis of N-substituted-2-aminobenzothiazoles via a crosscoupling reaction of 2-iodo anilines with isothiocyanates is envisaged using nano copper oxide as a recyclable catalyst and Cs2CO3as a base in PEG-400,as a bio-degradable,reusable,inexpensive and nontoxic reaction medium,under ligand-free *** present tandem process underlines environmental acceptability to access a wide range of N-substituted-2-aminobenzothiazoles in good to excellent yields.

关键词： 2-Aminobenzothiazoles 2-Iodoanilines Isothiocyanates CuO nanoparticles Recyclability PEG-400

Structural features of substituted triazole-linked chalcone derivatives as antimalarial activities against D_(10) strains of Plasmodium falciparum: A QSAR approach

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Journal of Central South University 2015年第10期22卷 3738-3744页

作者： Mukesh C.Sharma division of Drug Design & medicinal chemistry Research Lab School of Pharmacy Devi Ahilya University Takshila Campus

A quantitative structure–activity relationship(QSAR) was performed to analyze antimalarial activities against the D10 strains of Plasmodium falciparum of triazole-linked chalcone and dienone hybrid derivatives using partial least squares regression coupled with stepwise forward–backward variable selection method. QSAR analyses were performed on the available IC50 D10 strains of Plasmodium falciparum data based on theoretical molecular descriptors. The QSAR model developed gave good predictive correlation coefficient(r2) of 0.8994, significant cross validated correlation coefficient(q2) of 0.7689, r2 for external test set)(2predr of 0.8256, coefficient of correlation of predicted data set)(2sepred,r of 0.3276. The model shows that antimalarial activity is greatly affected by donor and electron-withdrawing substituents. The study implicates that chalcone and dienone rings should have strong donor and electron-withdrawing substituents as they increase the activity of chalcone. Results show that the predictive ability of the model is satisfactory, and it can be used for designing similar group of antimalarial compounds. The findings derived from this analysis along with other molecular modeling studies will be helpful in designing of the new potent antimalarial activity of clinical utility.

关键词： quantitative structure–activity relationship(QSAR) chalcone antimalarial Plasmodium falciparum stepwise forward–backward partial least squares

Facile synthesis of benzimidazole bearing 2-pyridone derivatives as potential antimicrobial agents

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Chinese Chemical Letters 2014年第2期25卷 305-307页

作者： N.C.Desai N.R.Shihory G.M.Kotadiya division of medicinal chemistry Department of Chemistry(UGC NON-SAP & DST-FIST Sponsored)M.K.Bhavnagar University

A series of benzimidazole bearing 2-pyridones 5a-k were synthesized and assessed in vitro for their activity as antimicrobial agents using the conventional broth dilution method. The results of the antimicrobial study revealed that compounds 5b, 5c, Sj and 5k exhibited substantial antibacterial activity while compound 5d emerged as amore potent antifungal agent compared to the standard drugs chloramphenicol and ketoconazole, respectively. It was observed that the presence of inductively electron withdrawing groups remarkably enhance the antibacterial activity of the newly synthesized compounds. Cytotoxicity studies suggested that none of the tested compounds exhibited any significant cytotoxic effects.

关键词： Benzimidazole 2-Pyridone Antimicrobial activity Cytotoxicity

Synthesis, Crystal Structure and Antibacterial Activity of 1-((2-Chloroquinolin-3-yl)-methyl)-pyridin-2(1H)-one

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Chinese Journal of Structural chemistry 2010年第11期29卷 1612-1617页

作者： S. Mohana Roopan Venkatesha R. Hathwar F. Nawaz Khan Atul Kumar Kushwaha Organic & medicinal chemistry Research Laboratory Organic Chemistry Division School of Advanced Sciences VIT University Solid State and Structural chemistry Unit Indian Institute of Science

On the basis of the interesting structures and biological activities exhibited by several heterocyclic systems possessing the pyridone nucleus such as mappcine and camptothecin, we have planed to design the synthesis, crystal studies and antibacterial activity of the new 1-（（2- chloroquinolin-3yl）-methyl）-pyridine-2（1H）-one building block. An X-ray analysis has provided valuable insight into the effect of steric factors on the three-dimensional shape of this compound which serves as a useful advanced intermediate in the synthesis of these biologically active molecules. A multistep synthesis of camptothecin （5） has been designed by retrosynthetic analysis as part of an ongoing program on lead anticancer drug.

关键词： crystal structure 1-((2-chloroquinolin-3yl)-pyridine-2(1H)-one

Potential anti-tubercular agents:Hexahydro-3-phenyl indazol-2-yl(pyridin-4-yl)methanones from anti-tubercular drug isoniazid and bis(substituted-benzylidene)cycloalkanones

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Chinese Chemical Letters 2015年第5期26卷 567-571页

作者： Ayyakannu Arumugam Napoleon Fazlur-Rahman Nawaz Khan Euh Duck Jeong Eun Hyuk Chung Organic and medicinal chemistry Research Laboratory Organic Chemistry DivisionSchool of Advanced SciencesVIT-University Korea Basic Science Institute Busan Center

A series of indazol-2-yl（pyridin-4-yl）methanones, 4 were acquired from 2,6-bisbenzylidene cyclohex- anones, 3 and anti-tubercular drug （isoniazid）, and their anti-tubercular impacts were screened. Among the test compounds used against Mycobacterium tuberculosis H37 Ra cell line in the microplate alamar blue assay, the compounds 4g-j revealed moderate anti-tubercular activity with MIC 12.5 μg/mL, comparable to standard drugs （streptomycin, MIC, 6.25 μg/mL, pyrazinamide, isoniazid and ciprofloxacin with MICs of 3.125 μg/mL）.

关键词： Benzylidene cyclohexanones Hexahydro-3-phenyl indazol-2-yl (pyridin- 4-yl)methanones lsoniazid Anti-tubercular activity

Comparison of conventional and supported liquid extraction methods for the determination of sitagliptin and simvastatin in rat plasma by LC-ESI-MS/MS

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Journal of Pharmaceutical Analysis 2015年第3期5卷 161-168页

作者： B.Ramesh N.Manjula S.R.Bijargi V.U.M.Sarma P.Sita Devi Natural Products chemistry division Indian Institute of Chemical Technology medicinal chemistry & Pharmacology division Indian Institute of Chemical Technology

Three extraction methods were compared for their efficiency to analyze sitagliptin and simvastatin in rat plasma by LC-MS/MS, including （1） liquid-liquid extraction （LLE）, （2） solid phase extraction （SPE） and （3） supported liquid extraction （SLE）. Comparison of recoveries of analytes with different extraction methods revealed that SLE was the best extraction method. The detection was facilitated with ion trap-mass spectrometer by multiple reactions monitoring （MRM） in a positive ion mode with ESI. The transitions monitored were m./z 441.1→325.2 for simvastatin, 408.2→235.1 for sitagliptin and 278.1→260.1 for the IS. The lower limit of quantification （LLOQ） was 0.2 ng/mL for sitagliptin and 0.1 ng/mL for simvastatin. The effective SLE offers enhanced chromatographic selectivity, thus facilitating the potential utility of the method for routine analysis of biological samples along with pharmacokinetic studies.

关键词： Rat plasma Simvastatin Sita#'ptin Supported liquid extraction

Autochthonous halotolerant plant growth-promoting rhizobacteria promote bacoside A yield of Bacopa monnieri(L.)Nash and phytoextraction of salt-affected soil

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Pedosphere 2020年第5期30卷 671-683页

作者： Umesh PANKAJ Durgesh Narain SINGH Pooja MISHRA Pooja GAUR C.S.Vivek BABU Karuna SHANKER Rajesh Kumar VERMA Department of Soil Science CSIR-Central Institute of Medicinal and Aromatic PlantsLucknow 226015(India) division of Biotechnology CSIR-Central Institute of Medicinal and Aromatic PlantsLucknow 226015(India) division of Microbial Technology CSIR-Central Institute o f Medicinal and Aromatic PlantsLucknow 226015(India) Analytical chemistry Department CSIR-Central Institute o f Medicinal and Aromatic PlantsLucknow 226015(India) Research Centre CSIR-Central Institute of Medicinal and Aromatic PlantsBangalore 560065(India)

Phytoremediation is a promising approach for reclamation of salt-affected *** is the most commonly used process,which exploits plants to absorb,immobilize,and accumulate salt in their *** this study,halotolerant plant growth-promoting rhizobacteria(PGPR)were isolated from the rhizosphere of wild grasses growing naturally in salt-affected areas of Lucknow,Uttar Pradesh(India)and were tested for their efficacies of salt-tolerance and plant growth-promoting(PGP)*** on 16S rRNA sequences,the most efficient halotolerant isolates possessing PGP traits were identified as Pseudomonas plecoglossicida(KM 233646),Acinetobacter calcoaceticus(KM 233647),Bacillus flexus(KM 233648),and Bacillus safensis(KM 233652).Application of these isolates as bio-inoculants significantly(Pmedicinal plant,Bacopa monnieri(L.)Nash,grown on natural salt-affected *** phytoremediation of salt-affected soil was evident by the substantial increase in shoot Na^+:K^+ratio of bio-inoculant-treated *** compared to un-inoculated control plants,the soil physico-chemical properties of bio-inoculant-treated plants were *** shoot and root biomass(fresh and dry weights),soil enzymes,and soil nutrient parameters showed significant positive correlations with the shoot Na+:K+***,the halotolerant PGPR screened in this study could be useful for the reclamation of saline soils concomitant with improved plant growth and bacoside A yield.

关键词： bio-inoculant phytoremediation plant productivity soil physico-chemical property soil salinity

Exploring the benefits of biochar over other organic amendments for reducing of metal toxicity in Withania somnifera

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Biochar 2019年第3期1卷 293-307页

作者： Nidhi Nigam Vineet Yadav Puja Khare Raghuvendra Pratap Singh Paurabi Das Karuna Shanker Ram Suresh Sharma Agronomy and Soil Science division CSIR-Central Institute of Medicinal and Aromatic PlantsP.O.-CIMAPNear Kukrail Picnic SpotLucknow 226015India Analytical chemistry division CSIR-Central Institute of Medicinal and Aromatic PlantsLucknow 226015India Technology and Business Development division CSIR-Central Institute of Medicinal and Aromatic PlantsLucknow 226015India

Biochar is considered as a good metal sequester and ameliorates the metal toxicity and uptake in ***,its effec-tiveness over other organic amendments is not well *** aim of this study is to compare the biochar amendments alleviating the levels of Pb and Cd in Withania somnifera *** with other organic *** manure,vermicom-post,and biochar were applied in the field spiked with highly available Pb and *** bioavailability and accumulation,plant growth and plant physiology,antioxidant enzymes and metabolite content of *** along with soil properties were evaluated in all *** indicates that the application of organic manures significantly alleviated the metal levels(33-72%)in the plant in comparison with *** herbage yield was significantly higher(33-69%)under different organic manures as compared to the metal *** metabolite contents and antioxidant enzymes were higher in metal treatments in comparison with *** manures were not only able to restrain the Pb and Cd in soil but also enhanced the soil microbial *** indicate that biochar amendments were more promising than farmyard manure and vermicompost due to the presence of more stable carbon in biochar and more alleviation in metal *** addition,net profit in the cultivation of *** was higher for biochar amendments(50%higher)compared to *** study recommended that biochar could be a better option for commercial and safer production of ***.

关键词： Toxic metals Withania somnifera Biochar Phytotoxicity

Assay method for quality control and stability studies of a new antimalarial agent (CDRI 99/411)

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Journal of Pharmaceutical Analysis 2013年第5期3卷 335-340页

作者： Kiran Khandelwal Shakti Deep Pachauri Sofa Zaidi Pankaj Dwivedi Ashok Kumar Sharma Chandan Singh Anil Kumar Dwivedi division of Pharmaceutics CSIR-Central Drug Research Institute division of medicinal and Process chemistry CSIR-Central Drug Research Institute

CDRI compound no. 99/411 is a potent 1,2,4-trioxane antimalarial candidate drug under development at our Institute. An HPLC method for determination of CDRI 99/411 with its starting material and intermediates has been developed and validated for in process quality control and stability studies. The analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection （LOD） and lower limit of quantification （LLOQ） were determined according to International Conference on Harmonization ICH Q2（R1） guidelines. HPLC separation was achieved on a RP-select B Lichrosphere~ column （250 mm x 4 ram, 5 lam, Merck） using water containing 0.1% glacial acetic acid and acetonitrile as the mobile phase in a gradient elution. The eluents were monitored by a photo diode array detector at 245 and 275 nm. Based on signal to noise ratio of 3 and 10 the LOD of CDRI 99/411 was 0.55 μg/mL, while the LLOQ was 1.05 μg/mL. The calibration curves were linear in the range of 1.05- 68 μg/mL. Precision of the method was determined by inter- and intra-assay variations within the acceptable range.

关键词： HPLC Trioxane Process quality control Stability

VARIATION OF PHYSICO-CHEMICAL PROPERTIES OF RADIATION CROSSLINKED RUBBER WITH STORAGE TIME

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Chinese Journal of Polymer Science 2005年第5期23卷 497-501页

作者： N.C.Dafader M.E.Haque F.Akhtar Nuclear and Radiation chemistry division

The effect of storage on physico-chemical properties of non-irradiated natural rubber and radiation vulcanized natural rubber （RVNR） were evaluated. The rubber films were stored under two different conditions, namely in open air and sealed polyethylene bags. The antioxidant, tris（nonylated phenyl） phosphite （TNPP） was used for preventing degradation of RVNR films. Gel content, cross-link density, tensile strength at break and 500% elongation of rubber films were measured. The results show that the retention （%） of tensile properties of rubber films with TNPP is higher than that of rubber films without antioxidants. The rubber films stored in polyethylene bags also show better retention of tensile properties than those of rubber films stored in open air.

关键词： Storage Radiation Tensile Properties Antioxidant.