- Synthesis of novel polyfunctionally substituted thieno[2,3-c]pyridazines
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4-Cyano-5,6-dimethylpyridazin-3-(2H)-thione 3b was used as a key intermediate for the synthesis of novel polysubstituted thieno[2,3-c] pyridazines.
- Gaber, Abd El-Aal M.,El-Gaby, Mohamed S. A.,Kamal El-Dean, Adel M.,Eyada, Hassan A.,Al-Kamali, Ahmed S. N.
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- Synthesis and Preliminary Evaluation of 11C-Labeled VU0467485/AZ13713945 and Its Analogues for Imaging Muscarinic Acetylcholine Receptor Subtype 4
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Muscarinic acetylcholine receptors (mAChRs) have five distinct subunits (M1–M5) and are involved in the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. Attributed to the promising clinical efficacy of xanomeline, an M1/M4-preferring agonist, in patients of schizophrenia and Alzheimer's disease, M1- or M4-selective mAChR modulators have been developed that target the topographically distinct allosteric sites. Herein we report the synthesis and preliminary evaluation of 11C-labeled positron emission tomography (PET) ligands based on a validated M4R positive allosteric modulator VU0467485 (AZ13713945) to facilitate drug discovery. [11C]VU0467485 and two other ligands were prepared in high radiochemical yields (>30 %, decay-corrected) with high radiochemical purity (>99 %) and high molar activity (>74 GBq μmol?1). In vitro autoradiography studies indicated that these three ligands possess moderate-to-high in vitro specific binding to M4R. Nevertheless, further physiochemical property optimization is necessary to overcome the challenges associated with limited brain permeability.
- Deng, Xiaoyun,Hatori, Akiko,Chen, Zhen,Kumata, Katsushi,Shao, Tuo,Zhang, Xiaofei,Yamasaki, Tomoteru,Hu, Kuan,Yu, Qingzhen,Ma, Longle,Wang, Gangqiang,Wang, Lu,Shao, Yihan,Josephson, Lee,Sun, Shaofa,Zhang, Ming-Rong,Liang, Steven
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supporting information
p. 303 - 309
(2019/01/04)
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- CCSO nano catalyzed solid phase synthesis of 3-oxo-5,6-disubstituted-2,3-dihydropyridazine-4-carbonitrile
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Co-doped Ce0.94Ca0.05Sr0.01O1.94 (CCSO) nano particles have been successfully synthesized by an auto-combustion method and were characterized by XRD, TEM and AFM analyses. The catalytic activity of the nano-catalyst is evaluated by the synthesis of substituted pyridazines from substituted benzil and cyano acetylhydrazide, which have great biological and pharmaceutical interest. Thus, a highly economically efficient one-pot solvent free synthesis of pyridazine was developed, which is promoted by the CCSO nano catalyst. The benefits of the reaction are its very short time (2-4 min) and high yields (90-95%). The method offers a highly convergent, inexpensive, and functionality-tolerable procedure for rapid access to important pyridazine compounds in good yields. This journal is
- Singh, Praveen,Kumar, Ranjeet,Yadav, Brijesh Kumar,Khanna, Ranjana S.,Tewari, Ashish Kumar
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p. 51239 - 51243
(2014/12/11)
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- Synthesis and reactions of some new thieno[2,3-c]pyridazine derivatives
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The alkylation of 4-cyano-5,6-dimethylpyridazin-3(2H)-thione 3 with some halo compounds gave the S-alkylated products 4a-c, which upon treatment with ethanolic sodium ethoxide afforded the cyclized thienopyridazines 5a-c as products. Pyridazothienotriazin
- Al-Kamali, Ahmed S. N.
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body text
p. 1812 - 1824
(2010/02/28)
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- Novel synthesis of thieno[2,3-c]pyridazine and pyrimido[4′,5′: 4,5]thieno[2,3-c]pyridazine derivatives
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Novel series of thieno[2,3-c]pyridazines and pyrimido[4′,5′:4, 5] thieno-[2,3-c]pyridazines have been synthesized from the readily accessible 4-cyano-5,6-dimethylpyridazin-3(2H)-thione 3b. Copyright Taylor & Francis Inc.
- El-Dean, A. M. Kamal,El-Gaby,Gaber,Eyada,Al-Kamali
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p. 413 - 424
(2007/10/03)
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