36796-53-9Relevant academic research and scientific papers
Discovery, Optimization, and Characterization of Novel Chlorcyclizine Derivatives for the Treatment of Hepatitis C Virus Infection
He, Shanshan,Xiao, Jingbo,Dulcey, Andrés E.,Lin, Billy,Rolt, Adam,Hu, Zongyi,Hu, Xin,Wang, Amy Q.,Xu, Xin,Southall, Noel,Ferrer, Marc,Zheng, Wei,Liang, T. Jake,Marugan, Juan J.
supporting information, p. 841 - 853 (2016/02/23)
Recently, we reported that chlorcyclizine (CCZ, Rac-2), an over-the-counter antihistamine piperazine drug, possesses in vitro and in vivo activity against hepatitis C virus. Here, we describe structure-activity relationship (SAR) efforts that resulted in the optimization of novel chlorcyclizine derivatives as anti-HCV agents. Several compounds exhibited EC50 values below 10 nM against HCV infection, cytotoxicity selectivity indices above 2000, and showed improved in vivo pharmacokinetic properties. The optimized molecules can serve as lead preclinical candidates for the treatment of hepatitis C virus infection and as probes to study hepatitis C virus pathogenesis and host-virus interaction.
PIPERIDINE AND PIPERAZINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS AND CANCER
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Paragraph 0334; 0335, (2015/06/11)
Disclosed are compounds of formula (I) (formula I),as antiviral agents, antineoplastic agents, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X and Y are independently CH or N, o is 0, 1 or 2, and E is absent or is (CR13 R14 )m, NH, or S, F is absent or is (CR15 R16 )n, C=O, or -SO2 -, G is absent or is (CR17 CR18 )r, H is absent or is C=O, or -SO2 - and R1, Ar1, Ar2 are as defined in the specification. These compounds are antiviral agents and are contemplated in the treatment of viral infections, for example, hepatitis C, or are antineoplastic agents.
Structure-activity studies of fentanyl
Casy,Huckstep
, p. 605 - 608 (2007/10/02)
The preparation of analogues of fentanyl with para substituents in the anilino aromatic ring, anilino nitrogen separated from phenyl by methylene or bimethylene, and phenacyl replacing propionyl as the N-acyl substituent is reported. Although all para sub
1,4-Benzodiazepine derivatives
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, (2008/06/13)
1,4-Benzodiazepine derivatives of the formula: STR1 (in which R1 is pyrrolidinyl or piperidinyl each optionally substituted by C1-3 alkyl, phenyl-C1-3 alkyl, C1-5 alkanoyl, or C2-5 alkoxycarbonyl, R2 is hydrogen, hydroxy, or acetoxy, R3 is C1-3 alkyl, phenyl-C1-3 alkyl, or phenyl optionally substituted by one or two halogens, X is hydrogen, halogen, C1-3 alkyl, C1-3 alkoxy, nitro, trifluoromethyl, or di-C1-3 alkyl-amino, and n is 1 or 2) or pharmaceutically acceptable acid addition salts thereof, which are useful as a psychotropic agent such as anti-depressant or anxiolytic agent can be prepared from several routes.
Aminohaloborane in Organic Synthesis. IX. Exclusive ortho Acylation Reaction of N-Monoaminoalkylanilines
Adachi, Makoto,Sasakura, Kazuyuki,Sugasawa, Tsutomu
, p. 1826 - 1835 (2007/10/02)
The exclusive ortho acylation reaction of aniline derivatives using boron trichloride made possible the one-step synthesis of 2-acyl-N-monoaminoalkylanilines (1) and the corresponding imines (2) from N-monoaminoalkylanilines, even in the case of compounds with a bulky substituent at the nitrogen atom.Conventional methods only give 1 via elaborate procedures.Keywords: regioselective reaction; 2-acylaniline derivative; 2-acylaniline-imine derivative; boron trichloride
