Fused pyrimidine derivatives R 0515Synthesis Leading to Novel 2,4,6-Trisubstituted Quinazoline Derivatives, Their Antibacterial and Cytotoxic Activity Against THP-1, HL-60 and A375 Cell Lines.-Twelve 2,4,6-Trisubstituted quinazoline derivatives of type (V) are prepared and screened for their antibacterial and cytotoxic effects against the title cell lines. Derivative (Vd) exhibits the highest activity against THP-1 and HL-60 cell lines, whereas (Va) and (Vb) show moderate activity. -(CHANDRIKA, P. M.; YAKAIAH, T.; NARSAIAH*, B.; SRIDHAR, V.; VENUGOPAL, G.; RAO, J. V.; KUMAR, K. P.; MURTHY, U. S. N.; RAO, A. R. R.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 48 (2009) 6, 840-847; Fluoroorg. Div., Indian Inst. Chem. Technol., Hyderabad 500 007, India; Eng.) -M. Bohle 43-171
A simple, precise and rapid HPLC method has been developed and validated for the estimation of Lovastatin and niacin simultaneously in combined dosage form. Chromatographic separation of the two drugs was performed on a Purospher BDSC8 column (150mm×4.6mmid, 5µm particlesize).The mobile phase used was a mixture of 0.1% v/v triethylamine (pH 5.0), containing 20 mM of ammonium acetate buffer: methanol (30:70% v/v).Detection was performed at 237nm and sharp peaks were obtained forniacin and Lovastatin at retention times of 3.2±0.01 min and.6.4±0.01 min respectively.The calibration curve was linear in the concentration range 100-700µg/ml for niacin 3-18µg/ml for Lovastatin; the correlation coefficients were 0.9991 and 0.9992, respectively. The optimized method showed good performance in terms of specificity, linearity, detection and quantitationlimits, precision and accuracy in accordance with the International Conference on Harmonization (ICH) Q2 (R1) guidelines.This assay was demonstrated to be applicable for routine quantitation of Lovastatin and niacin in tablet dosage form.
Some organotin(IV) and tin(II) complexes of composition R3Sn[R'COC:CON(C6H5)N:CCH3]
(where R=C4H9, R'=CH3, C3H5, p-ClC6H4; R=C6H5, R'=C6H5 and p-ClC6H4) and Sn[p-ClC6H4COC:CON(C6H5)N:CCH3]2 were screened for their toxicity against Aedes aegypti larvae. Organotin(IV) complexes were more active than tin(II) complexes.
Fused pyrimidine derivatives R 0515Synthesis of Novel 4,6-Disubstituted Quinazoline Derivatives, Their Antiinflammatory and Anticancer Activity (Cytotoxic) Against U937 Leukemia Cell Lines.-Compounds (IV) show poor to moderate antiinflammatory and promising anticancer activities. Derivative (IVc) exhibits maximum cytotoxic effects similar to the standard etoposide. -(CHANDRIKA, P. M.; YAKAIAH, T.; RAO*, A. R. R.; NARSAIAH, B.; REDDY, N. C.; SRIDHAR, V.; RAO, J. V.; Eur. J. Med. Chem. 43 (2008) 4, 846-852; Univ. Coll. Pharm. Sci., Kakatiya Univ., Warangal 506 009, India; Eng.) -R. Staver 35-147
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