Browsing by Author "Rajendra Prasad, V.V.S."

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    Synthesis and evaluation of fexofenadine analogue for antihistaminic, anticholinergic and sedative activities
    (Chemical Publishing Co., 2007) Sathish, N.K.; Bhagavanraju, M.; Hemamalini, K.; Gopkumar, P.; Narendra, V.; Rajendra Prasad, V.V.S.
    A novel ?-[4-isopropyl phenyl]-4-(hydroxy diphenyl methyl)-1-piperidinyl)butan-1-one (II) has been synthesized by Friedel Craft's acylation and condensation reaction. The structures of the synthesized compounds were elucidated by (IR, PMR and Mass) spectral analysis. The compound synthesized was screened for anti-histaminic activity by histamine induced contractions using guinea pig ileum, anticholinergic by guinea pig tracheal chain and sedative activity. The compound exhibited significant anti-histaminic activity.
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    Synthesis, chemical characterization of novel 1,3-dimethyl acridones as cytotoxic agents, and their DNA-binding studies
    (2010) Sathish, N.K.; Gopkumar, P.; Rajendra Prasad, V.V.S.; Shanta Kumar, S.M.; Mayur, Y.C.
    A series of new 1,3-dimethyl acridone derivatives were synthesized with different alkyl side chain (propyl and butyl) substitution at N 10-position and highly basic amine groups at terminal end of alkyl side chain. All the synthesized molecules were screened for their cytotoxic activity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines. DNA binding constants (Ki) of selected compounds were determined with calf-thymus DNA. Results showed that the molecules 7, 8, 10, 11, 12, 13, 14, and 15 exhibited good cytotoxic activity with IC50 value <10 ?M. Compound 14 having (?- hydroxyethyl) piperazine butyl side chain exhibited potent cytotoxic activity against MCF-7 cell line and DNA-intercalating properties. Examination of the relationship between lipophilicity and acridone derivatives showed poor correlation. © Birkhäuser Boston 2009.