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Shailesh Kumar Atma P. Dwivedi Vivek Kr. Kashyap A.K. Saxena A.K. Dwivedi Ranjana Srivastava Devi P. Sahu 《Bioorganic & medicinal chemistry letters》2013,23(8):2404-2407
Synthesis of a library of novel trans 6-methoxy-1,1-dimethyl-2-phenyl-3-aryl-2,3-dihydro-1H-inden-4-yloxy alkyl amines and their antimycobacterial activity against drug sensitive and multidrug resistant strains of Mycobacterium tuberculosis have been reported. All the new compounds in the series exhibited MIC between 1.56 and 6.25 μg/ml. Two compounds 1i and 1j with low MIC and low cytotoxicity showed significant reduction in CFU in infected mouse macrophages at 1× MIC concentration. The compound 1i inhibited the growth of M. tuberculosis in mice at 100 mg/kg dose with 1.35 log10 reduction of CFU in lungs tissue and was active against non-replicating Mycobacterium tuberculosis under anaerobic condition. 相似文献
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Julia I. Gavrilyuk Ulrich Wuellner Syed Salahuddin Rajib K. Goswami Subhash C. Sinha Carlos F. Barbas 《Bioorganic & medicinal chemistry letters》2009,19(14):3716-3720
Irreversible chemical programming of monoclonal aldolase antibody (mAb) 38C2 has been accomplished with β-lactam equipped mono- and bifunctional targeting modules, including a cyclic-RGD peptide linked to either the peptide (d-Lys6)-LHRH or another cyclic RGD unit and a small-molecule integrin inhibitor SCS-873 conjugated to (d-Lys6)LHRH. We also prepared monofunctional targeting modules containing either cyclic RGD or (d-Lys6)-LHRH peptides. Binding of the chemically programmed antibodies to integrin receptors α(v)β(3) and α(v)β(5) and to the luteinizing hormone releasing hormone receptor were evaluated. The bifunctional and bivalent c-RGD/LHRH and SCS-783/LHRH, the monofunctional and tetravalent c-RGD/c-RGD, and the monofunctional bivalent c-RGD chemically programmed antibodies bound specifically to the isolated integrin receptor proteins as well as to integrins expressed on human melanoma M-21 cells. c-RGD/LHRH, SCS-783/LHRH, and LHRH chemically programmed antibodies bound specifically to the LHRH receptors expressed on human ovarian cancer cells. This approach provides an efficient, versatile, and economically viable route to high-valency therapeutic antibodies that target defined combinations of specific receptors. Additionally, this approach should be applicable to chemically programmed vaccines. 相似文献
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A K Srivastava C Pandey K P Dwivedi V K Singh 《Indian journal of biochemistry & biophysics》1989,26(3):199-200
QSAR studies have been performed on the homologues of 3-triazines, using molecular connectivity index and van der Waal volume as structural parameters. The regression analysis has shown good correlation between antitumour activity and the two structural parameters. 相似文献
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Subhash C. Sharma M.D. 《International journal of biometeorology》1986,30(1):27-32
Platelet counts were estimated at sea level in 50 lowlanders. They were divided at random in two groups (A and B) of 25 each. Group A went up by train/road transport to 3658 m, while group B reached the same height after 8 days of acclimatisation enroute. Platelet counts were estimated serially in both groups at high altitude. Symptoms of high altitude exposure were also recorded. No significant change in the counts was noted in either group and none became Symptomatic. All were brought back to sea level by air and deinduction studies carried out on days 1 and 4 of return. The importance of these findings in the light of our existing knowledge is discussed. 相似文献
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Subhash Padhye Takeshi Kambara David N. Hendrickson Govindjee 《Photosynthesis research》1986,9(1-2):103-112
The recent model of Kambara and Govindjee for water oxidation [Kambara T. and Govindjee (1985) Proc. Natl. Acad. Sci. U.S.A., 82:6119–6123] has been extended in this paper by examining all the data in order to identify the most likely candidate for the redox-active ligand (RAL), suggested to operate between the water oxidizing complex (WOC) and Z, the electron donor to the reaction center P680. We have concluded that a very suitable candidate for RAL is the imidazole moiety of a histidine residue. The electrochemical data available on imidazole derivatives play heavily in this identification of RAL. Thus, we suggest that histidine might play the role of an electron mediator between the WOC and Z. A model of S-states in terms of their plausible chemical identity is presented here.Abbreviations J
electronic spin of ion
- P680
reaction center chlorophyll
- RAL
Redox active ligand
- Sn
state of the oxygen-evolving system
- WOC
water oxidation complex
- Z
electron donor to P680
Dedicated to Prof. L.N.M. Duysens on the occasion of his retirement 相似文献
10.
Subhash C. Gupta Catherine Potrikus Reese J. Woodland Hastings 《Archives of microbiology》1986,143(4):325-329
A recombinant plasmid which carried a 5 kb fragment of Vibrio harveyi DNA containing the luxA and luxB genes was mobilized from Escherichia coli into luminescence-deficient mutants of V. harveyi. The cloned genes complemented a temperature sensitive luciferase mutation, but failed to complement lesions in two different aldehyde deficient mutants. Expression of the cloned genes was not subject to autoinduction in either E. coli or in V. harveyi. 相似文献