- Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols
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A library of 16 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols 17–32 has been synthesized for use in biological testing against Trypanosoma cruzi, the protozoan parasite that causes Chagas disease. The 4-substituted 2-(1H-pyrrolo[3,2-c]pyridi
- Balfour, Michael N.,Franco, Caio H.,Moraes, Carolina B.,Freitas-Junior, Lucio H.,Stefani, Hélio A.
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Read Online
- Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and in Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model
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A series of 2,4-disubstituted imidazopyridines, originating from a SoftFocus Kinase library, was identified from a high throughput phenotypic screen against the human malaria parasite Plasmodium falciparum. Hit compounds showed moderate asexual blood stage activity. During lead optimization, several issues were flagged such as cross-resistance against the multidrug-resistant K1 strain, in vitro cytotoxicity, and cardiotoxicity and were addressed through structure-Activity and structure-property relationship studies. Pharmacokinetic properties were assessed in mice for compounds showing desirable in vitro activity, a selectivity window over cytotoxicity, and microsomal metabolic stability. Frontrunner compound 37 showed good exposure in mice combined with good in vitro activity against the malaria parasite, which translated into in vivo efficacy in the P. falciparum NOD-scid IL-2Rnull (NSG) mouse model. Preliminary mechanistic studies suggest inhibition of hemozoin formation as a contributing mode of action.
- Horatscheck, André,Andrijevic, Ana,Nchinda, Aloysius T.,Le Manach, Claire,Paquet, Tanya,Khonde, Lutete Peguy,Dam, Jean,Pawar, Kailash,Taylor, Dale,Lawrence, Nina,Brunschwig, Christel,Gibhard, Liezl,Njoroge, Mathew,Reader, Janette,Van Der Watt, Mari?tte,Wicht, Kathryn,De Sousa, Ana Carolina C.,Okombo, John,Maepa, Keletso,Egan, Timothy J.,Birkholtz, Lyn-Marie,Basarab, Gregory S.,Wittlin, Sergio,Fish, Paul V.,Street, Leslie J.,Duffy, James,Chibale, Kelly
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supporting information
p. 13013 - 13030
(2020/11/13)
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- Organic compound, electroluminescent device containing organic compound and applications of electroluminescent device
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The invention discloses an organic compound with a structure represented by a formula (I), wherein the LUMO energy level of the compound is reduced by linking an aza aromatic ring structure (a structure represented by a formula (II)), so that the electronic conductivity of the material is improved, and the compound is suitable for being used as an electronic material (such as an electron transportmaterial, an electron injection material, a hole blocking material and the like). According to the invention, the organic compound as an electron type material, particularly an electron transmissionmaterial, can be matched with hole type materials (such as a hole transmission material, a hole injection material and an electron blocking material), so that the transmission of electrons and holes is balanced, and the service life of a device is prolonged.
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Paragraph 0115-0117
(2020/06/17)
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- Synthesis, molecular docking, antimycobacterial and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine Mannich bases
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In this report, we describe the synthesis and biological evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases (7a-v). The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold (6a-c) with secondary amines and excess of formaldehyde solution in AcOH. The chemical structures of the compounds were characterized by 1H NMR, 13C NMR, LC/MS and elemental analysis. Single crystal X-ray diffraction has been recorded for compound 7k ([C23H29ClN4]+2, H2O). The in?vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using Agar diffusion method and Broth micro dilution method. Compounds 7e, 7f, 7r, 7t, and 7u were showed good Gram-positive antibacterial activity against S.?aureus, B. flexus, C. sporogenes and S. mutans. Furthermore, in?vitro antimycobacterial activity was evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) using MABA. Compounds 7r, 7t, and 7u were showed good antitubercular activity against Mtb (MIC ≥6.25?μg/mL). Among the tested compounds, 1-((4-chloro-2-(cyclohexylmethyl)-1H-pyrrolo[3,2-c]pyridin-3-yl)methyl)piperidine-3-carboxamide (7t) was showed excellent antimycobacterial activity against Mtb (MIC >25). Molecular docking of the active compounds against glutamate racemase (MurI) and Mtb glutamine synthetase were explained the structure-activity observed in?vitro.
- Jose, Gilish,Suresha Kumara, Tholappanavara H.,Sowmya, Haliwana B.V.,Sriram, Dharmarajan,Guru Row, Tayur N.,Hosamani, Amar A.,More, Sunil S.,Janardhan, Bhavya,Harish,Telkar, Sandeep,Ravikumar, Yalegara Siddappa
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p. 275 - 288
(2017/03/24)
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- HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS
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Disclosed are compounds of Formula (I) or salts thereof, wherein HET is a heteroaryl selected from pyrrolo[2,3 b]pyridinyl, pyrrolo[2,3 d]pyrimidinyl, pyrazolo[3,4 b]pyridinyl, pyrazolo[3,4 d]pyrimidinyl, imidazolo[4,5 b]pyridinyl, and imidazolo[4,5 d]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a nitrogen ring atom in said heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
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Page/Page column 171-172
(2017/01/09)
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- Ligand structure includes a new metal complexes
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Compounds comprising a metal complex having novel ligands are provided. In particular, the compound is an iridium complex comprising novel aza DBX ligands. The compounds may be used in organic light emitting devices, particularly as emitting dopants, providing improved efficiency, low operating voltage, and long lifetime.
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Paragraph 0318; 0319; 0320
(2016/11/24)
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- Synthesis, crystal structure, molecular docking and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine derivatives
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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.
- Jose, Gilish,Kumara, T. H. Suresha,Nagendrappa, Gopalpur,Sowmya,Jasinski, Jerry P.,Millikan, Sean P.,More, Sunil S.,Janardhan, Bhavya,Harish,Chandrika
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- PYRROLO[3,2-C]PYRIDINE COMPOUNDS AS G-PROTEIN-COUPLED RECEPTOR KINASE 5 (GRK5) MODULATORS
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The present invention relates to pyrrolo[3,2-c]pyridine compounds and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds, as well as pharmaceutical compositions containing at least one of these compounds t
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Page/Page column 78
(2015/01/16)
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- Imidazo[4,5-c]pyridine and pyrrolo[3,2-c]pyridine compounds as G-protein-coupled receptor kinase 5 (GRK5) modulators
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The present invention relates to imidazo[5,4-c]pyridine or pyrrolo[3,2-c]pyridine compounds and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds, as well as pharmaceutical compositions containing at least one of these pyridine-based bicyclic compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pyridine-based bicyclic compounds are assumed to be modulators of the GRK5 protein, thereby regulating the expression and/or release of insulin and are useful for the treatment or prophylaxis of a metabolic disease and in particular for the treatment and prophylaxis of diabetes, obesity and impaired adipogenesis.
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Paragraph 0091
(2015/01/18)
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- New polyfunctional imidazo[4,5-C]pyridine motifs: Synthesis, crystal studies, docking studies and antimicrobial evaluation
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New antimicrobial agents, imidazo[4,5-c]pyridine derivatives have been synthesized. We have developed a new synthetic protocol for the final reaction, an efficient microwave-assisted synthesis of imidazo[4,5-c]pyridines from substituted 3,4-diaminopyridin
- Jose, Gilish,Suresha Kumara,Nagendrappa, Gopalpur,Sowmya,Jasinski, Jerry P.,Millikan, Sean P.,Chandrika,More, Sunil S.,Harish
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p. 288 - 297
(2014/04/03)
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- NEW CRTH2 ANTAGONISTS
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The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Page/Page column 94
(2013/03/26)
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- New CRTh2 antagonists
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The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Paragraph 0368; 0369
(2013/03/26)
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- PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
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The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)
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Page/Page column 0625; 0631
(2014/02/15)
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- New CRTH2 Antagonists
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The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Page/Page column 63
(2012/12/13)
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- 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
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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
- Livecchi, Marion,Calvet, Geraldine,Schmidt, Frederic
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experimental part
p. 5006 - 5016
(2012/07/03)
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- PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
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The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as "PPA derivatives"), particularly 1H-pyrrolo[3,2-c]pyridine-6- amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)
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Page/Page column 67-68
(2012/10/07)
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- NOVEL AZA- HETEROCYCLES SERVING AS KINASE INHIBITORS
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The invention relates to compounds of formula (I), to their production and to their use for producing a medicament for treating diseases, particularly tumors and/or diseases in whose origin or progression kinases are involved.
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Page/Page column 81-82
(2010/11/24)
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- Potent 4-amino-5-azaindole factor VIIa inhibitors
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The 4-amino-5-azaindole as an amidino-benzimidazole replacement is described. A series of potent and selective analogs were discovered and showed desirable ex vivo efficacy as measured by PT.
- Hu, Huiyong,Kolesnikov, Aleksandr,Riggs, Jennifer R.,Wesson, Kieron E.,Stephens, Robin,Leahy, Ellen M.,Shrader, William D.,Sprengeler, Paul A.,Green, Michael J.,Sanford, Ellen,Nguyen, Margaret,Gjerstad, Erik,Cabuslay, Ronnel,Young, Wendy B.
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p. 4567 - 4570
(2007/10/03)
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