Anthem Biosciences Pvt. Ltd

Bangalore, India

Anthem Biosciences Pvt. Ltd

Bangalore, India

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Eswaran S.,Anthem Biosciences Pvt. Ltd | Adhikari A.V.,National Institute of Technology Karnataka
Bioorganic and Medicinal Chemistry Letters | Year: 2010

A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis. © 2009 Elsevier Ltd. All rights reserved.


Eswaran S.,Anthem Biosciences Pvt. Ltd | Adhikari A.V.,National Institute of Technology Karnataka | Thomas K.D.,Anthem Biosciences Pvt. Ltd
European Journal of Medicinal Chemistry | Year: 2010

Four new series of quinoline derivatives were synthesized starting from 2-trifluoromethyl aniline through multi-step reactions. In the reaction sequence,substituted aniline was cyclized to 4-hydroxy quinoline 1,which was then transformed to 4-chloro-2,8-bis(trifluoromethyl)quinoline 2. The key scaffold 4-hydrazinyl-2,8-bis(trifluoromethyl)quinoline 3,obtained from the compound 2,was successfully converted to target quinoline derivatives,viz. hydrazones 4aet,ureas 5aee,thioureas 6aec and pyrazoles 7aed,in good yields. The newly synthesized title compounds were evaluated for their in vitro antibacterial activity against Escherichia coli,Staphylococcus aureus,Pseudomonas aeruginosa and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H37Rv and MDR-TB. Preliminary results indicated that most of the hydrazone derivatives demonstrated very good antibacterial and antituberculosis activities while other derivatives showed moderate activity. © 2010 Elsevier Masson SAS. All rights reserved.


Eswaran S.,Anthem Biosciences Pvt. Ltd. | Adhikari A.V.,National Institute of Technology Karnataka | Ajay Kumar R.,Rajiv Gandhi Center for Biotechnology Trivandrum
European Journal of Medicinal Chemistry | Year: 2010

A new class of fused oxazoloquinoline derivatives was synthesized starting from 2-bromo-1-phenylethanones 1a-b through multi-step reactions. The newly synthesized compounds were evaluated for their in vitro antibacterial against Escherichia coli (ATTC-25922), Staphylococcus aureus (ATTC-25923), Pseudomonas aeruginosa (ATCC-27853) and Klebsiella pneumoniae (recultured) and antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294). Preliminary results indicated that most of the compounds demonstrated very good antibacterial and antituberculosis activities which are comparable with the first line drugs. Compounds 6a, 6c, 6g, 6j, 6k and 6n emerged as the lead antitubercular agents with MIC, 1 μg/mL and 99% bacterial inhibition while eight compounds, viz., 5a, 15k, 6a, 6c, 6g, 6j, 6k and 6n were found to be more potent than INH (MIC: 1.5 μg/mL) with MIC 1 μg/mL. © 2009 Elsevier Masson SAS. All rights reserved.


Thomas K.D.,Anthem Biosciences Pvt. Ltd | Thomas K.D.,National Institute of Technology Karnataka | Adhikari A.V.,National Institute of Technology Karnataka | Chowdhury I.H.,Post Graduate Institute of Medical Education and Research | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2011

Three new series of quinoline-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines were synthesized through multi-step reactions. The required intermediate, [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1, 2,3-triazol-4-yl]methanol (2) was prepared by treating 4-azido-6-methoxy-2- methylquinoline (1) with propargyl alcohol. Three different series of compounds were synthesized from this intermediate. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 2 was confirmed by X-ray crystallographic study. Further, the title compounds were evaluated for their in vitro anti-bacterial activity against five different bacterial strains and antimycobacterial activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis (ATCC 19420) and Mycobacterium fortuitum (ATCC 19542). Title compounds, 6a, 6d, 6i, 6j, 7e, 10a and 10i were found to be active against Mycobacterium tuberculosis H37Rv strain and could be lead molecules of interest. © 2011 Elsevier Masson SAS.


Thomas K.D.,Anthem Biosciences Pvt. Ltd | Thomas K.D.,National Institute of Technology Karnataka | Adhikari A.V.,National Institute of Technology Karnataka | Shetty N.S.,Justice Ks Hegde Medical Academy
European Journal of Medicinal Chemistry | Year: 2010

A new series of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3-triazol-4-yl] methanamine derivatives were synthesized starting from 4-methoxyaniline through multi-step reactions. The title compounds 5a-y were prepared by treating the azide intermediate 4 with propargyl bromide and different alkyl/heterocyclic amines in a sequential three component synthesis. All the new compounds were characterized by spectral and elemental analyses. The newly synthesized final compounds were evaluated for their in vitro antibacterial and antifungal activities against pathogenic strains. The preliminary screening results indicated that most of the compounds demonstrated moderate to very good antibacterial and antifungal activities, comparable to the first-line drugs. Twenty five new derivatives of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3- triazol-4-yl] methanamine have been synthesized and the most effective compounds have MIC of 6.25 μg/mL, which are in comparable with present antibiotics. © 2010 Elsevier Masson SAS. All rights reserved.


Baburaj T.,Anthem Biosciences Pvt. Ltd | Thambidurai S.,Alagappa University
Tetrahedron Letters | Year: 2012

Terminal tert-butyloxycarbonyl (Boc) protected hydrazino acids, useful intermediates for modified peptides and biologically active heterocyclic derivatives, were synthesized by electrophilic amination methodology using N-Boc-O-tosyl hydroxylamine as an efficient NH-Boc transfer reagent. Also, we have demonstrated the conversion of other amino acid derivatives such as amino esters and amino alcohols into β-Boc-hydrazino derivatives using this reagent. © 2012 Elsevier Ltd. All rights reserved.


Baburaj T.,Anthem Biosciences Pvt. Ltd | Thambidurai S.,Alagappa University
Synlett | Year: 2011

β-Boc-protected aryl and alkyl hydrazines, useful intermediates for azapeptides and N-substituted pyrazoles, were synthesized by electrophylic amination methodology, using less energetic N-Boc-O-tosyl hydroxylamine as an efficient nitrogen source. Also we have demonstrated a two-step, chromatography-free synthesis of N-Boc-O-tosyl hydroxylamine. © Georg Thieme Verlag Stuttgart - New York.


Silva T.M.,University of Coimbra | Silva T.M.,Lund University | Andersson S.,Lund University | Sukumaran S.K.,Anthem Biosciences Pvt. Ltd. | And 3 more authors.
PLoS ONE | Year: 2013

Background: New strategies are needed for breast cancer treatment and one initial step is to test new chemotherapeutic drugs in breast cancer cell lines, to choose candidates for further studies towards clinical use. Methodology and Findings: The cytotoxic effects of a biogenic polyamine analogue - norspermidine - and its trinuclear Pd(II) and Pt(II) complexes - Pd3NSpd2 and Pt3NSpd2, respectively - were investigated in one immortalized normal-like and three breast cancer cell lines. The normal-like MCF-10A cells were least sensitive to the compounds, while growth inhibition and cell death was observed in the cancer cell lines. Norspermidine and its Pd(II) complex were generally shown to have stronger antiproliferative effects than the corresponding Pt(II) complex. Moreover, both norspermidine and the Pd(II) complex reduced the cellular activity of the growth-related enzyme, ornithine decarboxylase (ODC) to a lower level than the Pt(II) complex in most of the cell lines examined. Treatment with norspermidine or the Pd(II) complex reduced the number of colonies formed in a soft agar assay performed with the breast cancer cell lines, indicating that these compounds reduced the malignancy of the breast cancer cells. The effect of norspermidine or the Pd(II) complex on colony formation was much stronger than that observed for the Pt(II) complex. The results from a new mammalian genotoxicity screen together with those of a single cell gel electrophoresis assay indicated that none of the drugs were genotoxic at a 25 μM concentration. Main Conclusions: Overall, norspermidine and its Pd(II) complex were shown to have strong antiproliferative effects. In comparison, the effects obtained with the Pd(II) complex were much stronger than that of the Pt(II) complex. The results obtained in the present study demonstrate that the trinuclear Pd(II) complex of norspermidine (Pd3NSpd2) may be regarded as a potential new metal-based drug against breast cancer, coupling a significant efficiency to a low toxicity. © 2013 Silva et al.


Patent
Anthem Biosciences Pvt Ltd. | Date: 2012-04-07

The present invention relates to a novel method for high throughput detection of wide range of genotoxins in eukaryotic cells wherein the eukaryotic cell based tool combines the ability to detect a broad spectrum of genotoxic signaling events and a simple and reproducible assay technique. The present invention further comprises expression cassettes, vectors, and eukaryotic cell lines for the same.


The present invention relates to a recombinant DNA expression/secretion system in E. coli wherein the said system combines the potential of signal peptide-based translocation of recombinant proteins to the periplasmic space of E. coli with membrane brave defective mutants of E. coli to further aid secretion into the extracellular space. The present invention further relates to the expression system which furthermore includes a helper plasmid to drive the expression of translocons to facilitate improved periplasmic secretion of the over-expressed recombinant protein. In addition, this system also facilitates efficient production of specific proteins of interest in E. coli.

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