The Experts below are selected from a list of 15834 Experts worldwide ranked by ideXlab platform
Kelly Chibale - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, biological evaluation and mechanistic studies of totarol Amino Alcohol derivatives as potential antimalarial agents.
Bioorganic & medicinal chemistry, 2011Co-Authors: Claire Tacon, Eric M. Guantai, Pete Smith, Kelly ChibaleAbstract:Herein we report on the semisynthesis and biological evaluation of β-Amino Alcohol derivatives of the natural product totarol and other simple aromatic systems. All β-Amino Alcohol derivatives of totarol exhibited higher antiplasmodial activity than totarol [IC(50): 11.69 μM (K1, chloroquine and multi-drug resistant strain), and 11.78 μM (D10, chloroquine sensitive strain)]-12e was the most active [IC(50): 0.63 μM (K1), and 0.61 μM (D10)]. The phenyl and naphthyl β-Amino Alcohol derivatives were much less active than their corresponding totarol equivalents. The majority of the β-Amino Alcohol derivatives of totarol were more active against K1 than the D10 strains of Plasmodium falciparum, a trend similar to the inverse relationship observed with the established aryl-Amino Alcohol antimalarial mefloquine. Selected compounds were shown to affect erythrocyte morphology, inhibit erythrocyte invasion and trigger CQ accumulation.
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comparison of the antiplasmodial and falcipain 2 inhibitory activity of β Amino Alcohol thiolactone chalcone and isatin chalcone hybrids
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Renate H Hans, Kelly ChibaleAbstract:: The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member beta-Amino Alcohol triazole library showed that the thiolactone-chalcones, with IC(50)s ranging from 0.68 to 6.08 microM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC(50)s of 14.9 microM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity.
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Comparison of the antiplasmodial and falcipain-2 inhibitory activity of β-Amino Alcohol thiolactone-chalcone and isatin-chalcone hybrids.
Bioorganic & medicinal chemistry letters, 2010Co-Authors: Renate H Hans, Jiri Gut, Philip J. Rosenthal, Kelly ChibaleAbstract:Abstract The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member β-Amino Alcohol triazole library showed that the thiolactone-chalcones, with IC 50 s ranging from 0.68 to 6.08 μM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC 50 s of 14.9 μM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity.
Akkattu T. Biju - One of the best experts on this subject based on the ideXlab platform.
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employing carboxylic acids in aryne multicomponent coupling triggered by aziridines azetidines
ChemInform, 2016Co-Authors: Tony Roy, Sachin Suresh Bhojgude, Manikandan Thangaraj, Trinadh Kaicharla, Bikash Garai, Akkattu T. BijuAbstract:The aryne multicomponent coupling involving carboxylic acids initiated by aziridines as nucleophiles affords N-aryl β-Amino Alcohol derivatives while the application of azetidines as nucleophilic triggers furnishes N-aryl γ-Amino Alcohol derivatives.
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employing carboxylic acids in aryne multicomponent coupling triggered by aziridines azetidines
Organic chemistry frontiers, 2016Co-Authors: Tony Roy, Sachin Suresh Bhojgude, Manikandan Thangaraj, Trinadh Kaicharla, Bikash Garai, Akkattu T. BijuAbstract:The transition-metal-free aryne multicomponent coupling (MCC) involving carboxylic acids initiated by aziridines/azetidines has been reported. The use of aziridines as nucleophiles afforded N-aryl β-Amino Alcohol derivatives and the application of azetidines as nucleophilic triggers furnished N-aryl γ-Amino Alcohol derivatives in moderate to good yields. These reactions proceed under mild conditions and result in the formation of a new carbon–nitrogen bond and a new carbon–oxygen bond. The utility of carboxylic acids in aryne MCCs has been demonstrated, and the synthetic potential of phenols as acid surrogates in the present aryne MCCs has been realized.
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synthesis of n aryl β Amino Alcohols by trifluoroacetic acid promoted multicomponent coupling of aziridines arynes and water
Journal of Organic Chemistry, 2015Co-Authors: Tony Roy, Dnyaneshwar R Baviskar, Akkattu T. BijuAbstract:A transition-metal-free, three-component coupling involving N-substituted aziridines, arynes, and water promoted by trifluoroacetic acid (TFA) has been reported. The reaction furnished medicinally important N-aryl β-Amino Alcohol derivatives in moderate to good yields. In addition, the use of azetidines in this reaction afforded N-aryl γ-Amino Alcohol derivatives.
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Synthesis of N‑Aryl β‑Amino Alcohols by Trifluoroacetic Acid Promoted Multicomponent Coupling of Aziridines, Arynes, and Water
2015Co-Authors: Tony Roy, Dnyaneshwar R Baviskar, Akkattu T. BijuAbstract:A transition-metal-free, three-component coupling involving N-substituted aziridines, arynes, and water promoted by trifluoroacetic acid (TFA) has been reported. The reaction furnished medicinally important N-aryl β-Amino Alcohol derivatives in moderate to good yields. In addition, the use of azetidines in this reaction afforded N-aryl γ-Amino Alcohol derivatives
M Muthukrishnan - One of the best experts on this subject based on the ideXlab platform.
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synthesis and antitubercular activity of Amino Alcohol fused spirochromone conjugates
ChemInform, 2013Co-Authors: Mohammad Mujahid, R G Gonnade, Perumal Yogeeswari, Dharmarajan Sriram, M MuthukrishnanAbstract:All the title compounds (VII) (21 examples) are screened for their in vitro antimycobacterial activity against Mycobacterium tuberculosis (virulent strain H37Rv).
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synthesis and antitubercular activity of Amino Alcohol fused spirochromone conjugates
Bioorganic & Medicinal Chemistry Letters, 2013Co-Authors: Mohammad Mujahid, R G Gonnade, Perumal Yogeeswari, Dharmarajan Sriram, M MuthukrishnanAbstract:Abstract A series of 21 new Amino Alcohol fused spirochromone conjugates have been synthesized, characterized with analytical data and evaluated their antimycobacterial activity against Mycobacterium tuberculosis (virulent strain H37Rv) in vitro. Some of the compounds exerted significant inhibition, in particular, compound 4f found to be the most potent derivative exhibiting MIC = 3.13 μg/mL.
Daniel G Anderson - One of the best experts on this subject based on the ideXlab platform.
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bioinspired alkenyl Amino Alcohol ionizable lipid materials for highly potent in vivo mrna delivery
Advanced Materials, 2016Co-Authors: Owen S Fenton, Robert Langer, Kevin J Kauffman, Rebecca L Mcclellan, Eric A Appel, Robert J Dorkin, Mark W Tibbitt, Michael W Heartlein, Frank Derosa, Daniel G AndersonAbstract:Thousands of human diseases could be treated by selectively controlling the expression of specific proteins in vivo. A new series of alkenyl Amino Alcohol (AAA) ionizable lipid nanoparticles (LNPs) capable of delivering human mRNA with unprecedented levels of in vivo efficacy is demonstrated. This study highlights the importance of utilizing synthesis tools in tandem with biological inspiration to understand and improve nucleic acid delivery in vivo.
Renate H Hans - One of the best experts on this subject based on the ideXlab platform.
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comparison of the antiplasmodial and falcipain 2 inhibitory activity of β Amino Alcohol thiolactone chalcone and isatin chalcone hybrids
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Renate H Hans, Kelly ChibaleAbstract:: The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member beta-Amino Alcohol triazole library showed that the thiolactone-chalcones, with IC(50)s ranging from 0.68 to 6.08 microM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC(50)s of 14.9 microM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity.
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Comparison of the antiplasmodial and falcipain-2 inhibitory activity of β-Amino Alcohol thiolactone-chalcone and isatin-chalcone hybrids.
Bioorganic & medicinal chemistry letters, 2010Co-Authors: Renate H Hans, Jiri Gut, Philip J. Rosenthal, Kelly ChibaleAbstract:Abstract The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member β-Amino Alcohol triazole library showed that the thiolactone-chalcones, with IC 50 s ranging from 0.68 to 6.08 μM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC 50 s of 14.9 μM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity.