- 1-Phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives as non-imidazole histamine H3-antagonists
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In this study, a series of 1-phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl] piperazine derivatives has been prepared and in vitro tested as H 3-receptor antagonists (electrically evoked contraction of the guinea pig jejunum). All compounds inve
- Staszewski, Marek,Walczynski, Krzysztof
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p. 1287 - 1304
(2013/04/10)
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- New azoles with potent antifungal activity: Design, synthesis and molecular docking
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In response to the urgent need for novel antifungal agents with improved activity and broader spectrum, computer modeling was used to rational design novel antifungal azoles. On the basis of the active site of lanosterol 14α-demethylase from Candida albicans (CACYP51), a series of new azoles with substituted-phenoxypropyl piperazine side chains were rational designed and synthesized. In vitro antifungal activity assay indicates that the new azoles show good activity against most of the tested pathogenic fungi. Interestingly, the designed compounds are also active against an azole-resistant clinical strain. Compared to fluconazole and itraconazole, several compounds (such as 12i, 12j and 12n) show higher antifungal activity and broader spectrum, which are promising leads for the development of novel antifungal agents.
- Che, Xiaoying,Sheng, Chunquan,Wang, Wenya,Cao, Yongbing,Xu, Yulan,Ji, Haitao,Dong, Guoqiang,Miao, Zhenyuan,Yao, Jianzhong,Zhang, Wannian
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scheme or table
p. 4218 - 4226
(2009/12/09)
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- Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics
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Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a-n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity.
- Gao, Feng-Li,Wang, Xin,Zhang, Hong-Mei,Cheng, Tie-Ming,Li, Run-Tao
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p. 1535 - 1537
(2007/10/03)
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- N,N-SUBSTITUTED CYCLIC AMINE DERIVATIVES
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N,N-substituted cyclic amine derivatives represented by general formula (VIII) or pharmacologically acceptable salts thereof: wherein A represents aryl, etc.; E represents -CO- or -CHOH-; G represents oxygen, etc.; J represents optionally substituted aryl; R1 represents lower alkyl, etc.; Alk represents linear or branched lower alkylene; n, v, w, x and y independently represent each 0 or 1; and p represents 2 or 3. These compounds or salts thereof are efficacious in treating diseases against which calcium antagonism is efficacious. These diseases include cerebrovascular disorder at the acute stage, cerebral stroke, cerebral infarction, head injury, cerebral nerve cell death, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, brain circulatory disturbance, brain function disturbance, pain, convulsion, schizophrenia, hemicrania, epilepsy, circular psychosis, nerve degeneration diseases, brain ischemia, AIDS, complex dementia, edema, anxiety and diabetic nephropathy.
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- 2-(substituted-1-piperazinyl)[1,2,4]triazolo[1,5-a]pyrimidines
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This disclosure describes novel 2-(4-substituted-1-piperazinyl)[1,2,4]triazolo[1,5-a]pyrimidines useful as hypotensive agents.
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- Pyrazolylpiperazines
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This disclosure describes novel pyrazolylpiperazines useful as hypotensive agents in mammals and as intermediates for the preparation of certain pyrazolo[1,5-a]pryrimidines.
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