Aptuit Laurus Private Ltd

Hyderabad, India

Aptuit Laurus Private Ltd

Hyderabad, India
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Ravindran J.,University of Texas M. D. Anderson Cancer Center | Subbaraju G.V.,Aptuit Laurus Private Ltd | Ramani M.V.,Aptuit Laurus Private Ltd | Sung B.,University of Texas M. D. Anderson Cancer Center | Aggarwal B.B.,University of Texas M. D. Anderson Cancer Center
Biochemical Pharmacology | Year: 2010

Curcumin, a component of turmeric (Curcuma longa), exhibits anti-inflammatory and anti-proliferative activities through the generation of reactive oxygen species (ROS). Curcumin (diferuloylmethane) contains two hydroxyl, two methoxy and two phenyl groups but how these groups contribute to its activity is poorly understood. We synthesized analogues that varied in inclusion of these groups and compared their activity. We found that bisdemethylcurcumin (BDC) was more potent than curcumin as an anti-inflammatory agent as indicated by suppression of TNF-induced NF-κB activation, more potent as an anti-proliferative agent, and more potent in inducing ROS. Hispolon, which lacks one aromatic unit in relation to curcumin, also exhibited enhanced anti-inflammatory and anti-proliferative activities. When synthetic curcumin (Cur-S) was compared with bisdemethylcurcumin (BDC), hispolon, hispolon methyl ether (HME), dehydroxy hispolon (DH), hydroxy hispolon (HH), methoxy hispolon methyl ether (MHME), and methoxy hispolon (MH), we found that following order of anti-inflammatory activity: BDC=Hispolon>HME>HH>Cur-S>MHME>MH>DH; for anti-proliferative: Hispolon>BDC>MHME>Cur-S>MH>HME=HH>DH; and for prooxidant: BDC>Cur-S=MHME>HH>MH+HME>DH (254-1414 mean fluorescence intensity). Thus, dehydroxy hispolon was least potent for all three activities. Overall the results indicate that the substitution of a hydroxyl group for a methoxy group at the meta positions of the phenyl rings in curcumin significantly enhanced the anti-inflammatory activity, and the removal of phenyl ring at the 7th position of the heptadiene back bone and addition of hydroxyl group significantly increased the anti-proliferative activity of curcumin. © 2010 Elsevier Inc.


Khan M.,Aptuit Laurus Private Ltd | Jayasree K.,Aptuit Laurus Private Ltd | Reddy K.V.S.R.K.,Aptuit Laurus Private Ltd | Dubey P.K.,Jawaharlal Nehru University
Journal of Pharmaceutical and Biomedical Analysis | Year: 2012

A simple and rapid capillary zone electrophoretic method was developed for determining dimethyl sulfate a possible human carcinogen and mutagen and chloroacetyl chloride a potential genotoxic agent at trace levels in pharmaceutical drug substances by indirect photometric detection. A systematic screening of various anionic probes was performed to obtain the best separation conditions and sensitivity. High sensitivities with low quantification and detection levels were achieved for dimethylsulfate and chloroacetyl chloride using a background electrolyte (BGE) containing 5. mM pyridine dicarboxylic acid as the probe ion. The method is specific, precise and accurate for the two genotoxins. The optimized method was validated for specificity, precision, linearity, accuracy and stability in solution. Calibration curves were linear (R> 0.999) for both dimethylsulfate and chloroacetyl chloride in the range LOQ - 300% of nominal concentrations. The CE method was effectively implemented for estimating dimethylsulfate and chloroacetyl chloride in two different active pharmaceutical ingredients (APIs). © 2011 Elsevier B.V.


Harikrishna M.,Aptuit Laurus Private Ltd | Mohan H.R.,Aptuit Laurus Private Ltd | Dubey P.K.,University of Hyderabad | Shankar M.,Aptuit Laurus Private Ltd | Subbaraju G.V.,Aptuit Laurus Private Ltd
Synthetic Communications | Year: 2012

A general synthetic approach has been developed for the synthesis of a key intermediate (6) that can be elaborated into several ophthalmic prostaglandins and their derivatives. Using these strategy, we have obtained (±)-bimatoprost (1) and its analog, (±)-homobimatoprost (5). Copyright © Taylor & Francis Group, LLC.


Sunil Kumar I.V.,Aptuit Laurus Private Ltd | Anjaneyulu G.S.R.,Aptuit Laurus Private Ltd | Hima Bindu V.,Jawaharlal Nehru Technological University
Beilstein Journal of Organic Chemistry | Year: 2011

Sertindole (1), an atypical anti-psychotic drug is used for the treatment of schizophrenia. During the laboratory optimization and later during its bulk synthesis the formation of various impurities was observed. The impurities formed were monitored and their structures were tentatively assigned on the basis of their fragmentation patterns in LC-MS. Most of the impurities were synthesized and their assigned constitutions confirmed by co-injection in HPLC. We describe herein the formation, synthesis and characterization of these impurities. Our study will be of immense help to others to obtain chemically pure sertindole. © 2011 Sunil Kumar et al; licensee Beilstein-Institut.


Kumar I.V.S.,Aptuit Laurus Private Ltd | Ramanjaneyulu G.S.,Aptuit Laurus Private Ltd | Bindu V.H.,Jawaharlal Nehru Technological University
Letters in Organic Chemistry | Year: 2011

Synthesis of Sildenafil by the O-alkylation of 5-[2-hydroxy-5-(4- methylpiperazin-1-ylsulphonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H- pyrazolo-[4,3-d]pyrimidin-7-one 8 proved difficult because concomitant alkylation of the pyrimidine moity also occurred. The selective O-alkylation was carried by DCC assisted decarboxilative etherification of the carbonate 9. © 2011 Bentham Science Publishers.


Nageswari A.,Jawaharlal Nehru University | Nageswari A.,Aptuit Laurus Private Ltd | Krishna Reddy K.V.S.R.,Aptuit Laurus Private Ltd | Mukkanti K.,Jawaharlal Nehru University
Chromatographia | Year: 2012

Formaldehyde has been highlighted as potential genotoxic impurity (GTI). Trace-level quantification of GTIs in drug substances requires sensitive, precise and accurate analytical methodologies for their estimation in drug substances and control. Analysis and estimation of formaldehyde is very challenging due to its properties namely volatility, high polarity, low molecular weight and over and above the absence of chromophore. This article presents a validated HPLC-UV method which is sensitive to quantification of formaldehyde in active pharmaceutical ingredient. As formaldehyde does not possess chromophore, the developed HPLC method involves derivatization with 2,4-dinitrophenylhydrazine. Using this method, the detection and quantitation limits achieved are 0.5 and 1.5 ppm, respectively. The calibration curve of formaldehyde was linear over the concentration range of 1.5-20 ppm. The method was found to be sensitive, precise and accurate and the proposed method has been successfully applied to estimate formaldehyde content in scale-up batches of bulk drug. © 2012 Springer-Verlag.


Patent
Aptuit Laurus Private Ltd | Date: 2012-11-26

The present invention provides a process for the preparation of tenofovir. The present invention also provides a process for the preparation of tenofovir disoproxil or a salt thereof and its pharmaceutical composition using the tenofovir of the present invention.


Nageswari A.,Aptuit Laurus Private Ltd | Nageswari A.,Jawaharlal Nehru University | Reddy K.V.S.R.K.,Aptuit Laurus Private Ltd | Mukkanti K.,Jawaharlal Nehru University
Journal of Pharmaceutical and Biomedical Analysis | Year: 2012

A simple, precise, accurate stability-indicating gradient reverse phase ultra-performance liquid chromatographic (RP-UPLC) method was developed for quantitative determination of purity of Imatinib Mesylate (IMM) drug substance and drug products in the presence of its process related impurities, and degradation products. The proposed RP-UPLC method utilizes Acquity UPLC BEH 50-mm, 2.1mm and 1.7μm C-18 column at 30°C, with a gradient program of 9.0min at a flow rate of 0.3mL/min. The compounds of interest were monitored at 237nm. Resolution for Imatinib and eight related components was found to be greater than 1.5 for any pair of components. The correlation coefficients (r 2>0.9990) obtained indicate clear correlations between the concentrations and their peak areas for the investigated compounds. RSD obtained for the repeatability and intermediate precision experiments, was less than 5.0%. Accuracy of the method was further ascertained by performing recovery studies through spiking experiments. The drug substance was subjected to hydrolytic, oxidative, photolytic and thermal stress conditions as per ICH. The developed method was validated according to the current ICH guidelines for specificity, limit of detection, limit of quantitation, linearity, accuracy, precision, ruggedness and robustness. The method is also suitable for the assay determination of IMM in pharmaceutical dosage forms. © 2012 Elsevier B.V.


Khan M.,Aptuit Laurus Private Ltd | Reddy C.N.K.,Aptuit Laurus Private Ltd | Ravindra G.,Aptuit Laurus Private Ltd | Reddy K.V.S.R.K.,Aptuit Laurus Private Ltd | Dubey P.K.,Jawaharlal Nehru University
Journal of Pharmaceutical and Biomedical Analysis | Year: 2012

A series of novel 6-fluoro1,4-dihydro-4-oxo-3-quinoline carboxylic acid dimers were synthesized as potential antibacterial agents from commercially available substituted fluorobenzoic acids. A stability indicating HPLC method was developed to determine these novel fluoroquinolone dimers using a systematic method development approach. Samples were subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation; and analyzed to demonstrate the specificity and stability indicating ability of the developed method. The precision for all four fluoroquinolone dimers was within 2.0% RSD. Calibration curves were linear (LOQ, 150%), with regression coefficients >0.99 for all dimers. The method was conveniently applied for determining purity and assay of these four novel fluoroquinolone dimers. © 2011 Elsevier B.V.


The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.

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