Sanathnagar, India
Sanathnagar, India

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Bhujanga Rao A.K.S.,Natco Research Center
Asian Journal of Pharmaceutical and Clinical Research | Year: 2012

A series of N-substituted-5-methyl-1-(4-methylphenyl)-1H-1,2,3-triazole-4-carboxamide derivatives were synthesized by treating 5-methyl-1-(4-methylphenyl)-1H-1,2,3-triazole-4-carboxylic acid with thionyl chloride followed by reaction with various amines. IR, 1H NMR spectra and mass spectral data are confirming the synthesis of N-substituted-5-methyl-1-(4-methylphenyl)-1H-1, 2, 3-triazole-4-carboxamide derivatives.


Kishore M.,College and Research center | Jayaprakash M.,Natco Research Center | Vijayabhaskarareddy T.,Dr Reddys Laboratories
International Journal of ChemTech Research | Year: 2011

Rapid, simple and sensitive spectrophotometric methods are presented for the determination of Capecitabine. The methods are based on their oxidation and precipitation reactions. In both methods the reactions can be monitored spectrophotometrically by measuring the absorbance of the produced complexes at 520 and 560 nm. The proposed methods have permitted the quantification of Capecitabine over linearity in the range of 10-120 mg/ml and its percentage recovery was found to be 99.65-99.93 %.


Parvataneni D.M.,Natco Research Center | Devraj R.,Natco Research Center | Mangamoori L.N.,Jawaharlal Nehru Technological University
Journal of Microencapsulation | Year: 2013

Surfactants are routinely included in tablets during wet or dry granulations or along with directly compressible vehicles to improve wetting, disintegration and dissolution. Besides this micellar solubilization can improve permeability of poorly soluble drugs via gastrointestinal tract membranes thereby enhancing oral bioavailability. Microparticle-entrapped micelles (MEM) technology is a novel method of incorporating surfactants in tablets for improving in vitro and in vivo performance of poorly water-soluble drugs. Valsartan (VAL) was solubilized in cremophor EL micelles at cloud point temperature; lactose was dissolved in micellar dispersion and the dispersion was directly spray-dried to obtain solid product, which was subsequently converted into tablets using suitable excipients. VAL tablets produced by applying MEM technology improved dissolution performance of valsartan tablets. These tablets exhibited superior dissolution rate over controls and marketed tablets in all media employed irrespective of pH conditions and composition. © 2013 Informa UK Ltd.


Kompella A.,Natco Research Center | Adibhatla B.R.K.,Natco Research Center | Muddasani P.R.,Natco Research Center | Rachakonda S.,Natco Research Center | And 2 more authors.
Organic Process Research and Development | Year: 2012

An efficient, economic process has been developed for the production of imatinib with 99.99% purity and 50% overall yield from four steps. Formation and control of all possible impurities is described. The synthesis comprises the condensation of N-(5-amino-2-methylphenyl)-4-(3-pyridinyl)-2-pyrimidineamine with 4-(4-methylpiperazinomethyl)benzoyl chloride in isopropyl alcohol solvent in the presence of potassium carbonate to yield imatinib base. © 2012 American Chemical Society.


Ravikumar K.,Indian Institute of Chemical Technology | Sridhar B.,Indian Institute of Chemical Technology | Bhujanga Rao A.K.S.,Natco Research Center | Pulla Reddy M.,Natco Research Center
Acta Crystallographica Section C: Crystal Structure Communications | Year: 2011

Sorafenib, a drug that targets malignant cancer cells and cuts off the blood supply feeding the tumour, has been crystallized as the free base, 4-(4-{3-[4-chloro-3-(trifluoromethyl)phen-yl]ureido}phenoxy)-N-methylpyridine-2- carboxamide, C21H16ClF3N4O 3, (I), and as a tosyl-ate salt, 4-(4-{3-[4-chloro-3-(trifluoro-meth- yl)phen-yl]ureido}phen-oxy)-2-(N-methylcarbamoyl)pyridinium 4- methylbenzenesulfonate, C21H17ClF3N 4O3 +·C7H7O 3S-, (II). In both structures, the sorafenib mol-ecule is in an extended conformation. The pyridine-2-carboxamide group exhibits a syn conformation of the N atoms in (I), whereas an almost anti orientation is present in (II). In both crystal structures, the two terminal groups, viz. pyridine-2-carboxamide and the trifluorophenyl ring, are oriented differently to the conformations found in enzyme-bound sorafenib. The sorafenib molecules in (I) are linked into zigzag chains by N - H⋯O hydrogen bonds, whereas in (II) the presence of the additional tosyl-ate anion results in the formation of chains of fused hydrogen-bonded rings. This study reveals the variations in the solid-state conformation of the sorafenib mol-ecule in different crystalline environments. © 2011 International Union of Crystallography.


Amala K.,Natco Research Center | Rao A.K.S.B.,Natco Research Center | Gorantla B.,Illinois College | Gondi C.S.,Illinois College | Rao J.S.,Illinois College
International Journal of Oncology | Year: 2013

Imatinib mesylate is the first tyrosine kinase inhibitor developed and approved for the treatment of chronic myeloid leukemia (CML). In the past few years development of resistance towards imatinib mesylate has been reported. To overcome this problem a series of phenyl amino pyrimidine derivatives have been designed, prepared and evaluated for anti-proliferative activity against the BCR-ABL-positive leukemia cell line K562. Among these phenyl amino pyrimidine derivatives, NRC-AN-019 has been found to be a promising new lead compound for the therapy of imatinib mesylate-resistant chronic myeloid leukemia. In this communication, we describe the design, preparation and preclinical studies of NRC-AN-019.


PubMed | Natco Research Center
Type: Journal Article | Journal: International journal of oncology | Year: 2012

Imatinib mesylate is the first tyrosine kinase inhibitor developed and approved for the treatment of chronic myeloid leukemia (CML). In the past few years development of resistance towards imatinib mesylate has been reported. To overcome this problem a series of phenyl amino pyrimidine derivatives have been designed, prepared and evaluated for anti-proliferative activity against the BCRABLpositive leukemia cell line K562. Among these phenyl amino pyrimidine derivatives, NRCAN019 has been found to be a promising new lead compound for the therapy of imatinib mesylate-resistant chronic myeloid leukemia. In this communication, we describe the design, preparation and preclinical studies of NRCAN019.


PubMed | Natco Research Center
Type: Journal Article | Journal: Pakistan journal of biological sciences : PJBS | Year: 2013

In this study of the recovery and purification of rapamycin from the culture broth of an actinomycetes strain MTCC 5681, we investigated various factors such as biomass separation, suitable solvents for extraction, normal phase and flash chromatographic conditions and selective precipitation to obtain rapamycin in substantially pure form of the product. Adsorption chromatography particularly with normal phase and flash chromatography, in combination with centrifugal decantation is found to be the most suitable for separation as well as purification of rapamycin. Centrifugal decantation technique is likely to emerge as an efficient, industrially scalable, high yielding and economical process for biomass separation. The purity of rapamycin obtained through the method described was 99.4% which has not been reported so far.


PubMed | Natco Research Center
Type: Journal Article | Journal: Indian journal of pharmaceutical sciences | Year: 2012

A new strategy for the synthesis of curcuminoids is described involving the reaction of acetylacetone difluroboronite with an aromatic aldehyde in the presence of n-butylamine as catalyst. The new intermediate products, curcuminoid difluroboronites, of symmetrically substituted curcuminoids like curcumin and bisdemethoxycurcumin are stable, can be isolated and hydrolysed with aq. methanol at pH 5.8 to get the curcuminoids of high purity. The method is applicable for unsymmetrical curcuminoids like demethoxycurcumin also with some modification involving column chromatography. The intermediate curcuminoid difluroboronites, as also the natural -diketone pongamol difluroboronite, prepared for the first time were characterized on the basis of physical and chemical properties and spectroscopic data. The advantage of using borontrifluoride to protect the enol group in acetylacetone over the generally used boric oxide is brought out. The importance of conducting biological activity studies using pure curcuminoids is explained.


PubMed | Natco Research Center
Type: Journal Article | Journal: Preparative biochemistry & biotechnology | Year: 2013

The purpose of this investigation is to enhance the production of the immunosuppressant drug rapamycin by subjecting the strain CBS 773.23 to ultraviolet (UV) and N-methyl-N-nitro-N-nitroso guanidine (NTG) mutations. Among all the mutants tested, MTCC 5681 (NRC-CM03/SH) obtained by NTG mutagenesis of strain CBS 773.72 showed the highest activity, 210mg/L. The effect of different factors including medium composition, pH, temperature, and intensity of mixing on rapamycin production was studied. Based on the study, the optimal concentrations of soluble starch and dry yeast granules were found to be 50g/L and 1.5g/L, respectively. Furthermore, optimal values for pH, temperature, and shaking speed were found to be 6.0, 28C, and 220rpm, respectively. The production of rapamycin increased 1.6-fold, to 360mg/L, in shake-flask culture using the optimal combination of factors observed compared with basal cultivation medium using MTCC 5681 mutant strain.

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