1171919-00-8Relevant articles and documents
Synthesis, crystal structure, molecular docking and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine derivatives
Jose, Gilish,Kumara, T. H. Suresha,Nagendrappa, Gopalpur,Sowmya,Jasinski, Jerry P.,Millikan, Sean P.,More, Sunil S.,Janardhan, Bhavya,Harish,Chandrika
, p. 85 - 95 (2015)
New antibacterial agents, pyrrolo[3,2-c]pyridine derivatives have been designed and synthesized. The structural considerations of the designed molecules were further supported by the docking study with GlcN-6-P synthase. The chemical structures of the new compounds were characterized by NMR, mass spectral analysis and elemental analysis. Single crystals of two compounds, C13H15N2Cl [6a] and C21H24N3OCl, CH4O [7c] were obtained allowing for structural analysis. [C13H15N2Cl] monoclinic, P21/c, a = 9.9763(6) A?, b = 9.6777(6) A?, c = 13.3002(9) A?, β = 106.459(7)°, V = 1231.47(14) A?3, Z = 4, T = 173(2) K, μ(Cu Kα) = 2.522 mm-1, Dcalc = 1.266 g/mm3, 7124 reflections, 2404 unique (Rint = 0.0381), R1 = 0.0420 (I > 2σ(I)) and wR2 = 0.1254 (all data). [C21H24N3OCl, CH4O] triclinic, P-1, a = 10.1478(7) A?, b = 12.0945(8) A?, c = 18.3244(10) A?, α = 104.369(5)°, β = 90.766(5)°, γ = 99.235(6)°, V = 2147.1(2) A?3, Z = 4, T = 173(2) K, μ(Cu Kα) = 1.744 mm-1, Dcalc = 1.243 g/mm3, 14238 reflections, 8297 unique (Rint = 0.0330), R1 = 0.0578 (I > 2σ(I)) and wR2 = 0.1773 (all data). The in vitro antimicrobial activities of the compounds were conducted against various Gram-negative, Gram-positive bacteria and fungi. Amongst the tested compounds 7e displayed promising antibacterial activity against Gram-positive bacteria Bacillus flexus compared to antibiotic Amoxicillin.
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects
Papillon, Julien P. N.,Lou, Changgang,Singh, Alok K.,Adams, Christopher M.,Ksander, Gary M.,Beil, Michael E.,Chen, Wei,Leung-Chu, Jennifer,Fu, Fumin,Gan, Lu,Hu, Chii-Whei,Jeng, Arco Y.,Lasala, Daniel,Liang, Guiqing,Rigel, Dean F.,Russell, Kerry S.,Vest, John A.,Watson, Catherine
, p. 9382 - 9394 (2015/12/23)
Human clinical studies conducted with LCI699 established aldosterone synthase (CYP11B2) inhibition as a promising novel mechanism to lower arterial blood pressure. However, LCI699's low CYP11B1/CYP11B2 selectivity resulted in blunting of adrenocorticotropic hormone-stimulated cortisol secretion. This property of LCI699 prompted its development in Cushing's disease, but limited more extensive clinical studies in hypertensive populations, and provided an impetus for the search for cortisol-sparing CYP11B2 inhibitors. This paper summarizes the discovery, pharmacokinetics, and pharmacodynamic data in preclinical species and human subjects of the selective CYP11B2 inhibitor 8.
Palladium-catalyzed synthesis of 2,3-disubstituted 5-azaindoles via heteroannulation reaction and of 2-substituted 5-azaindoles through domino sila-Sonogashira/5-endo cyclization
Livecchi, Marion,Calvet, Geraldine,Schmidt, Frederic
experimental part, p. 5006 - 5016 (2012/07/03)
A general and efficient procedure for the synthesis of 2,3-disubstituted 5-azaindoles through the palladium-catalyzed heteroannulation of 4-acetamido-3-iodopyridines and diaryl-, dialkyl-, or arylalkylalkynes is described along with a study of the reactio
