- AMINO ALCOHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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The present invention belongs to the field of medicine, and specifically discloses an amino alcohol derivative represented by Formula I, a pharmaceutically acceptable salt, solvate, polymorph or prodrug thereof. In addition, the present invention also discloses a pharmaceutical composition comprising the above substances, and a use of the substance in the preparation of a medicament for the prevention and treatment of an immune inflammatory disease, or a disease or condition associated with immunological competence such as multiple sclerosis, ALS, CIDP, systemic lupus erythematosus, rheumatoid arthritis, ulcerative colitis, psoriasis, polymyositis, etc.
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Paragraph 0219; 0220
(2021/11/13)
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- Utilization of ultrasonic as an approach of green chemistry for synthesis of hydrazones and bishydrazones as potential antimicrobial agents
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Hydrazides 3,4, Hydrazones 6a-c, bishydrazones 8a,b, N-hydroxy-N'- arylpropanehydrazonamide 9a,b and 1-(piperidin-1-yl)-N2-arylamidrazones 10a,b were prepared under ultrasonic waves as an approach for green chemistry. a notable good yield and short reaction time were afforded under ultrasonic waves.The structures of compounds were confirmed in terms of spectroscopic and elemental analyses. The invitro antimicrobial activity of the prepared compounds were evaluated. most of compounds exhibited an excellent growth inhibition such as compounds 2, 3 and 8b against gram positive bacteria, while 2, 3, 8b, 9a, 10a and 10b against gram negative bacteria. all of tested compounds have excellent or good antifungal activity except 3.
- Younis, Ahmed,Awad, Ghada E. A.
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p. 599 - 610
(2020/05/28)
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- Synthesis, chemical characterization and antimicrobial activity of new acylhydrazones derived from carbohydrates
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A new series of glycosylated acylhydrazones was synthesized and all the chemical structures were confirmed by High Resolution Mass Spectrometry (HRMS), 1H and 13C Nuclear Magnetic Resonance (1H-NMR; 13C-NMR) and Fourier Transform Infrared (FTIR) spectroscopy methods. The mass accuracy between the calculated and found values observed in HRMS analyses were near or lower than 5 ppm, which are acceptable for proposing a molecular formula using this technique. All of the synthesized compounds were screened for their antibacterial, antifungal and antiviral activities. Five compounds (12, 13, 14, 16 and 19) exerted a modest antifungal activity against the strains evaluated. Derivative 14 showed fungicidal activity against Candida glabrata at 173.8 μM and saccharide unit contributed to the increase of the antifungal potential against this strain. New chemical manipulation of derivative 14 can make it possible to obtain new potentially antimicrobial agents.
- Guilherme, Fernanda Dias,Simonetti, Julia évelin,Folquitto, Lais Regina Santos,Reis, Adriana Cotta Cardoso,Oliver, Josidel Concei??o,Dias, Amanda Latércia Tranches,Dias, Danielle Ferreira,Carvalho, Diogo Teixeira,Brand?o, Geraldo Célio,Souza, Thiago Belarmino de
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p. 349 - 356
(2019/03/04)
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- SAR Studies on Aromatic Acylhydrazone-Based Inhibitors of Fungal Sphingolipid Synthesis as Next-Generation Antifungal Agents
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Recently, the fungal sphingolipid glucosylceramide (GlcCer) synthesis has emerged as a highly promising new target for drug discovery of next-generation antifungal agents, and we found two aromatic acylhydrazones as effective inhibitors of GlcCer synthesis based on HTP screening. In the present work, we have designed libraries of new aromatic acylhydrazones, evaluated their antifungal activities (MIC80 and time-kill profile) against C. neoformans, and performed an extensive SAR study, which led to the identification of five promising lead compounds, exhibiting excellent fungicidal activities with very large selectivity index. Moreover, two compounds demonstrated broad spectrum antifungal activity against six other clinically relevant fungal strains. These five lead compounds were examined for their synergism/cooperativity with five clinical drugs against seven fungal strains, and very encouraging results were obtained; e.g., the combination of all five lead compounds with voriconazole exhibited either synergistic or additive effect to all seven fungal strains.
- Del Poeta, Maurizio,Haranahalli, Krupanandan,Lazzarini, Cristina,Mallamo, John,McCarthy, J. Brian,Ojima, Iwao,Pathiranage, Senuri,Sun, Yi,Zambito, Julia
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- Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists
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Herein we report the design and synthesis of a series of simple phenol amide ERRγ agonists based on a hydrazone lead molecule. Our structure activity relationship studies in this series revealed the phenol portion of the molecule to be required for activity. Attempts to replace the hydrazone with more suitable chemotypes led to a simple amide as a viable alternative. Differential hydrogen-deuterium exchange experiments were used to help understand the structural basis for binding to ERRγ and aid in the development of more potent ligands.
- Lin, Hua,Doebelin, Christelle,Patouret, Rémi,Garcia-Ordonez, Ruben D.,Ra Chang, Mi,Dharmarajan, Venkatasubramanian,Bayona, Claudia Ruiz,Cameron, Michael D.,Griffin, Patrick R.,Kamenecka, Theodore M.
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p. 1313 - 1319
(2018/03/21)
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- 1,2,4-Triazole and 1,3,4-oxadiazole analogues: Synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities
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1,2,4-Triazole and 1,3,4-oxadiazole analogues are of interest due to their potential activity against microbial and malarial infections. In search of suitable antimicrobial and antimalarial compounds, we report here the synthesis, characterization and biological activities of 1,2,4-triazole and 1,3,4-oxadiazole analogues (SS 1-SS 10). The molecules were characterized by IR, mass, 1H NMR, 13C NMR and elemental analysis. The in vitro antimicrobial activity was investigated against pathogenic strains, the results were explained with the help of DFT and PM6 molecular orbital calculations. In vitro cytotoxicity and genotoxicity of the molecules were studied against S. pombe cells. In vitro antimalarial activity was studied. The active compounds were further evaluated for enzyme inhibition efficacy against the receptor Pf-DHFR computationally as well as in vitro to prove their candidature as lead dihydrofolate reductase inhibitors.
- Thakkar, Sampark S.,Thakor, Parth,Doshi, Hiren,Ray, Arabinda
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p. 4064 - 4075
(2017/07/05)
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- Synthesis of sulfonylhydrazone- and acylhydrazone-substituted 8-ethoxy-3-nitro-2h-chromenes as potent antiproliferative and apoptosis inducing agents
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3-Nitro-2H-chromenes have recently been identified as a novel class of potent antitumor agents. In view of the favorable effects shown by sulfonylhydrazones and acylhydrazones, we designed and synthesized a series of sulfonylhydrazone- and acylhydrazone-substituted 8-ethoxy-3-nitro-2H-chromene derivatives, and evaluated their cell growth inhibition activities against A549, KG-1, A2780, and K562 cells. All the tested compounds exhibited more potent antiproliferative activity than BENC-511 against KG-1 cells. These compounds displayed IC50 values in the nanomolar range against A2780 cells. Compound 7d showed prominent cytotoxicity against K562 cells with an IC 50 of 0.11 μM, which was comparable to that of BENC-511. Compound 7d arrested K562 cells at the G1 phase at high concentrations and induced apoptosis in K562 cells. Furthermore, 7d increased the levels of cleaved caspase-3, decreased the expression of bcl-2 and induced the cleavage of poly(ADP-ribose) polymerase in K562 cells. Thus, this study provides the development of a series of novel compounds as effective antitumor agents with apoptotic death ability.
- Zhang, Datong,Ma, Yuntong,Liu, Yu,Liu, Zhao-Peng
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p. 576 - 588
(2014/08/18)
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- Synthesis of 2,5-disubstituted 1,3,4-oxadiazoles as potential antimicrobial, anticancer and anti-HIV agents
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Several 2-(N-substituted carboxamidomethylthio)-5-(4-acetylaminophenyl)-l,3,4-oxadiazoles 4 a-s have been synthesized and tested for their antibacterial, antitubercular, anticancer and anti-HIV activities. The structures of these compounds have been estab
- Shah,Shah,Bhatt,Desai,Trivedi,Undavia
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p. 180 - 182
(2007/10/03)
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