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Synthesis of Triazoloquinoxalines as Antitubercular Agents
Sekhar, Kondapalli Venkata Gowri Chandra,Rao, Vajja Sambasiva,Kumar, Dalip Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, $^{13}C$ NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.
Pharmacophore Hypothesis for Atypical Antipsychotics
Sekhar, Kondapalli Venkata Gowri Chandra,Vyas, Devambhatla Ravi Kumar,Nagesh, Hunsur Nagendra,Rao, Vajja Sambasiva Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.9
A three-dimensional pharmacophore hypothesis was developed for atypical antipsychotics in order to map common structural features of highly active compounds by using HipHop in CATALYST program. The pharmacophore hypotheses were generated using 12 compounds as training set and validated using 11 compounds as test set. The most predictive hypothesis (Hypo1) comprises five features viz. two hydrophobic regions, two hydrogen bond acceptor lipid and one aromatic ring. In the absence of information like crystallized structure of 5-$HT_{2A}$ receptor and binding mode of antipsychotics with 5-$HT_{2A}$ receptor, this hypothesis will serve as a potentially valuable tool in the design of novel atypical antipsychotics acting primarily at 5-$HT_{2A}$ and $D_2$ receptors.
Sekhar, Kondapalli Venkata Gowri Chandra,Rao, Vajja Sambasiva,Reddy, Aravalli Satish,Sunandini, Ravada,Satuluri, V S A Kumar Korean Chemical Society 2010 Bulletin of the Korean Chemical Society Vol.31 No.5
A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3-yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, $^1H$ NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.
Kondapalli Venkata Gowri Chandra Sekhar,Vajja Sambasiva Rao,Aravalli Satish Reddy,Ravada Sunandini,V S A Kumar Satuluri 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.5
A simple and efficient method has been developed for conversion of arenecarbaldehyde-3-methylquinoxalin-2-ylhydrazones to 3-(2-methylquinoxalin-3-yl)-2-(substitutedphenyl)thiazolidin-4-ones in good yields using microwave irradiation technique on silica as solid support under solvent free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, 1H NMR, and mass spectroscopy. All the synthesized thiazolidinones were investigated for their antimicrobial and antifungal activities. The results of the biological activities revealed that the compounds 3b, 3d, 3f and 3h exhibited excellent antibacterial activities while 3d and 3h exhibited good antifungal activity.
Synthesis of Triazoloquinoxalines as Antitubercular Agents
Kondapalli Venkata Gowri Chandra Sekhar,Vajja Sambasiva Rao,Dalip Kumar 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
1,2,4-Triazoles and quinoxalines were found to display various pharmacological activities. Hence a series of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines were synthesized. Due to various advantages of organic reactions under solvent-free conditions these compounds were developed using iodobenzene diacetate under solvent-free conditions. The synthesized compounds were characterized by elemental microanalysis, infrared spectroscopy, 1^H NMR, 13^C NMR and HRMS. All the synthesized compounds were investigated for their antitubercular activity and 5g was found to the most active compound.
Pharmacophore Hypothesis for Atypical Antipsychotics
Kondapalli Venkata Gowri Chandra Sekhar,Devambhatla Ravi Kumar Vyas,Hunsur Nagendra Nagesh,Vajja Sambasiva Rao 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.9
A three-dimensional pharmacophore hypothesis was developed for atypical antipsychotics in order to map common structural features of highly active compounds by using HipHop in CATALYST program. The pharmacophore hypotheses were generated using 12 compounds as training set and validated using 11 compounds as test set. The most predictive hypothesis (Hypo1) comprises five features viz. two hydrophobic regions, two hydrogen bond acceptor lipid and one aromatic ring. In the absence of information like crystallized structure of 5-HT2A receptor and binding mode of antipsychotics with 5-HT2A receptor, this hypothesis will serve as a potentially valuable tool in the design of novel atypical antipsychotics acting primarily at 5-HT2A and D2 receptors.