13141-32-7Relevant academic research and scientific papers
Evaluation of anti-depressant effects of phthalazinone-based triple-acting small molecules against 5-HT2A, 5-HT2C, and the serotonin transporter
Kim, Jihye,Cha, Eunji,Park, Woo Kyu,Lee, Hye Yeon,Lim, Sang Min,Kim, Hak Joong,Pae, Ae Nim
, (2020)
Development of highly effective, safe, and fast-acting anti-depressants is urgently required for the treatment of major depressive disorder. It has been suggested that targeting 5-HT2A and 5-HT2C in addition to inhibition of serotonin reuptake may be beneficial in generating anti-depressant agents with better pharmacology and less adverse effects. We have developed phthalazinone-based compounds that potently bind to 5-HT2A, 5-HT2C, and the serotonin transporter. The representative compounds 11j and 11l displayed strong binding affinities against these targets, and showed favorable toxicity profiles as determined by hERG binding and CYP inhibition assays. Furthermore, these compounds presented promising anti-depressant effects comparable to fluoxetine and also synergistic effects with fluoxetine in forced swimming test, which implicates these compounds can be developed to help the treatment of major depressive disorder.
METHODS AND COMPOSITIONS FOR INHIBITING CNKSR1
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Paragraph 0154, (2014/07/07)
Embodiments include compositions and methods of inhibiting CNKSR1 and methods of identifying inhibitors of CNKSR1.
COMPOUNDS AND METHODS FOR TREATING MAMMALIAN GASTROINTESTINAL MICROBIAL INFECTIONS
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Page/Page column 158, (2014/03/22)
Disclosed are compounds and pharmaceutically acceptable salts thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound selectively inhibits a parasitic IMPDH versus a host IMPDH. Also disclosed are pharmaceutical compositions comprising one or more compounds of the invention. Related methods of treating various parasitic and bacterial infections in mammals are disclosed. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
Synthesis and antimycobacterial evaluation of novel phthalazin-4- ylacetamides against log- and starved phase cultures: Research article
Sriram, Dharmarajan,Yogeeswari, Perumal,Senthilkumar, Palaniappan,Sangaraju, Dewakar,Nelli, Rohit,Banerjee, Debjani,Bhat, Pritesh,Manjashetty, Thimmappa H.
experimental part, p. 381 - 391 (2010/12/19)
Twenty four novel 2-[3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1- phthalazinyl]acetic acid amides were synthesized from phthalic anhydride and were subjected to in vitro and in vivo evaluation against log- and starved phase of mycobacterial species and
1,2-DIHYDRO-1-OXOPHTHALAZINYL DERIVATIVES HAVING BIOLOGICAL ACTIVITY ON SEROTONIN RECEPTORS 5-HT2A AND 5-HT2C, AND PREPARATION THEREOF
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Page/Page column 19-20, (2008/12/07)
The present invention relates to a novel 1,2-dihydro-1-oxophthalazinyl piperazine compound having biological activity as serotonin receptor antagonist, a preparation method of the compound and a pharmaceutical composition for the treatment and prevention of central nervous system diseases comprising the compound.
