- Discovery of tetrahydropyrido[4,3-d]pyrimidine derivatives for the treatment of neuropathic pain
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A series of tetrahydropyridopyrimidine derivatives were synthesized and evaluated for neurotoxicity and peripheral analgesic activity followed by assessment of antiallodynic and antihyperalgesic potential in two peripheral neuropathic pain models, the chronic constriction injury (CCI) and partial sciatic nerve ligation (PSNL). Compounds (4b and 4d) exhibiting promising efficacies in four behavioral assays of allodynia and hyperalgesia (spontaneous pain, tactile allodynia, cold allodynia and mechanical hyperalgesia) were quantified for their ED50 values (15.12-65.10 mg/kg). Studies carried out to assess the underlying mechanism revealed that the compounds suppressed the inflammatory component of the neuropathic pain and prevented oxidative and nitrosative stress.
- Sharma, Monika,Deekshith, Vanamala,Semwal, Arvind,Sriram, Dharmarajan,Yogeeswari, Perumal
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- Novel Carboline Derivatives as Potent Antifungal Lead Compounds: Design, Synthesis, and Biological Evaluation
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A series of novel antifungal carboline derivatives was designed and synthesized, which showed broad-spectrum antifungal activity. Particularly, compound C38 showed comparable in vitro antifungal activity to fluconazole without toxicity to human embryonic lung cells. It also exhibited good fungicidal activity against both fluconazole-sensitive and -resistant Candida albicans cells and had potent inhibition activity against Candida albicans biofilm formation and hyphal growth. Moreover, C38 showed good synergistic antifungal activity in combination with fluconazole (FLC) against FLC-resistant Candida species. Preliminary mechanism studies revealed that C38 might act by inhibiting the synthesis of fungal cell wall.
- Wang, Shengzheng,Wang, Yan,Liu, Wei,Liu, Na,Zhang, Yongqiang,Dong, Guoqiang,Liu, Yang,Li, Zhengang,He, Xiaomeng,Miao, Zhenyuan,Yao, Jianzhong,Li, Jian,Zhang, Wannian,Sheng, Chunquan
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p. 506 - 511
(2014/06/09)
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- An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study
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Series of hitherto unreported piperidone grafted pyridopyrimidines synthesized through ionic liquid mediated multi-component reaction. These compounds were evaluated for their inhibitory activities against AChE and BChE enzymes. All the compounds displaye
- Basiri, Alireza,Murugaiyah, Vikneswaran,Osman, Hasnah,Kumar, Raju Suresh,Kia, Yalda,Awang, Khalijah Binti,Ali, Mohamed Ashraf
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p. 221 - 229
(2013/10/01)
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- Lightening Agents and/or Dyes that Contain Aldehyde(s)
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Agents for dyeing and/or lightening keratin fibers, in particular human hair, containing, relative to the weight thereof, 0.001 to 15 wt. % of at least one aldehyde of the formula (I): wherein X represents —CH(R2)—SO2—Y—R1, —CR3R4R5, or wherein Y represents —CH(CHO)— or —CH2— or a chemical bond, and wherein each of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 independently represents —H or —CN or —F or —Cl or —Br or —I or —CHO or —NH2 or —NO2 or —CF3 or —CCl3 or —CF2CF3 or —CCl2CCl3 or an optionally substituted (C1-C6) alkyl group or a hydroxyalkyl group or a polyhydroxyalkyl group or an optionally substituted (C1-C6) alkylene group, and wherein the agent contains no oxidation dye precursors of developer and coupler type.
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- DIHYDROIMIDAZO [ 1, 5-F] PTERIDINES AS POLO-LIKE KINASE INHIBITORS
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The present invention provides PLK inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.
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Page/Page column 29
(2010/04/06)
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- N-alkylated 3,5-bis(arylidene)-4-piperidones. Synthetic approaches, x-ray structure and anticancer activity
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(Chemical Equation Presented) In a search for cytotoxic fluorescent materials a series of N-alkylated and N,N-dialkylated 3,5-bis(arylidene) piperidones was synthesized. Alkylation of 3,5-bis(arylidene)-4-piperidone afforded quaternary salts only while condensation of N-alkyl-4-piperidones with substituted benzaldehydes was a convenient route to the corresponding N-alkylated compounds. Compounds and their pharmaceutically acceptable salts demonstrated high activity against resistant human lung carcinoma cell line A549 with IC50 values in the range of 0.3-6.5 μM.
- Makarov, Michael V.,Odinets, Irina L.,Lyssenko, Konstantin A.,Rybalkina, Ekaterina Yu.,Kosilkin, Ilya V.,Antipin, Mikhail Yu.,Timofeeva, Tatiana V.
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p. 729 - 736
(2008/09/21)
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- Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
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Novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized and evaluated for their abilities to inhibit lipopolysaccharide (LPS)-stimulated production of TNF-alpha in rat whole blood. Several of these compounds exhibited potent inhibitory activity.
- Fujita, Masakazu,Seki, Taketsugu,Inada, Haruaki,Ikeda, Naoko
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p. 1607 - 1611
(2007/10/03)
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- Eclipsed Conformation of the Exocyclic N-CH2 Bond in N-Neopentylpiperidines and the Stereodynamic Consequences As Studied by Dynamic NMR Spectroscopy and Molecular Mechanics Calculations
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The dynamic stereochemistry of a range of N-neopentylpiperidines 1 with an eclipsed N-CH2-t-Bu bond is compared with that of the corresponding range of N-ethylpiperidines 2 with a gauche N-CH2Me bond. By using dynamic NMR spectroscopy, the relative importance of ring inversion, exocyclic bond rotation, and nitrogen inversion are elucidated and barriers are reported and discussed. Minor populations of the neopentyl-axial-eclipsed conformation are detected directly and identified with the help of molecular mechanics calculations. The corresponding N-alkylpyrrolidines are also reported.
- Anderson, J. Edgar,Ijeh, Anthony I.,Storch, Christine,Casarini, Daniele,Lunazzi, Lodovico
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p. 3310 - 3317
(2007/10/03)
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