6 research outputs found

    Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives

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    The cyclooxygenase-2 (COX-2) enzyme is an important target for drug discovery and development of novel anti-inflammatory agents. Selective COX-2 inhibitors have the advantage of reduced side-effects, which result from COX-1 inhibition that is usually observed with nonselective COX inhibitors. In this study, the design and synthesis of a new series of 7-methoxy indolizines as bioisostere indomethacin analogues (5a–e) were carried out and evaluated for COX-2 enzyme inhibition. All the compounds showed activity in micromolar ranges, and the compound diethyl 3-(4-cyanobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5a) emerged as a promising COX-2 inhibitor with an IC50 of 5.84 µM, as compared to indomethacin (IC50 = 6.84 µM). The molecular modeling study of indolizines indicated that hydrophobic interactions were the major contribution to COX-2 inhibition. The title compound diethyl 3-(4-bromobenzoyl)-7-methoxyindolizine-1,2-dicarboxylate (5c) was subjected for single-crystal X-ray studies, Hirshfeld surface analysis, and energy framework calculations. The X-ray diffraction analysis showed that the molecule (5c) crystallizes in the monoclinic crystal system with space group P 21/n with a = 12.0497(6)Å, b = 17.8324(10)Å, c = 19.6052(11)Å, α = 90.000°, β = 100.372(1)°, γ = 90.000°, and V = 4143.8(4)Å3. In addition, with the help of Crystal Explorer software program using the B3LYP/6-31G(d, p) basis set, the theoretical calculation of the interaction and graphical representation of energy value was measured in the form of the energy framework in terms of coulombic, dispersion, and total energy

    Measurement of the Ωc0\Omega_c^0 lifetime at Belle II

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    We report on a measurement of the Ωc0\Omega_c^0 lifetime using Ωc0→Ω−π+\Omega_c^0 \to \Omega^-\pi^+ decays reconstructed in e+e−→ccˉe^+e^-\to c\bar{c} data collected by the Belle II experiment and corresponding to 207 fb−1207~{\rm fb^{-1}} of integrated luminosity. The result, τ(Ωc0)=243±48(stat)±11(syst) fs\rm\tau(\Omega_c^0)=243\pm48( stat)\pm11(syst)~fs, agrees with recent measurements indicating that the Ωc0\Omega_c^0 is not the shortest-lived weakly decaying charmed baryon

    Measurement of the Ωc0\Omega_c^0 lifetime at Belle II

    No full text
    We report on a measurement of the Ωc0\Omega_c^0 lifetime using Ωc0→Ω−π+\Omega_c^0 \to \Omega^-\pi^+ decays reconstructed in e+e−→ccˉe^+e^-\to c\bar{c} data collected by the Belle II experiment and corresponding to 207 fb−1207~{\rm fb^{-1}} of integrated luminosity. The result, τ(Ωc0)=243±48(stat)±11(syst) fs\rm\tau(\Omega_c^0)=243\pm48( stat)\pm11(syst)~fs, agrees with recent measurements indicating that the Ωc0\Omega_c^0 is not the shortest-lived weakly decaying charmed baryon
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