23976-28-5Relevant academic research and scientific papers
Erythromycin A ketolide antibiotic derivative as well as preparation method and application thereof
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, (2020/05/08)
The invention discloses a series of erythromycin A ketolide antibiotics containing an aminoquinoline ring as shown in a formula I, a preparation method and application thereof, side chain intermediates of all compounds and a synthesis method. The key points are as follows: the compound shown in the formula I has the efficacy of broad-spectrum antibiotics, and has outstanding antibacterial activityon sensitive and drug-resistant gram-positive bacteria and gram-negative bacteria; particularly, the antibacterial activity of strains such as vancomycin-resistant enterococcus faecalis, enterococcusfaecium, erythromycin-resistant pneumonia streptococcus, streptococcus pyogenes, pneumonia klebsiella, shigella flexneri and the like is obviously superior to that of control drugs telithromycin. Thecompound provided by the invention can be used as a broad-spectrum antibiotic, and has antibacterial and antiviral activities for inhibiting gram-positive bacteria and gram-negative bacteria.
A Borrowing Hydrogen Strategy for Dehydrative Coupling of Aminoisoquinolines with Benzyl Alcohols in Water
Hikawa, Hidemasa,Tan, Rie,Tazawa, Aoi,Kikkawa, Shoko,Azumaya, Isao
supporting information, p. 539 - 547 (2020/01/02)
We report a borrowing hydrogen strategy for a palladium-catalyzed dehydrative coupling of aminoisoquinolines with benzylic alcohols in water. This cascade reaction using the π-benzylpalladium system can be achieved in an atom-economic process without the
An Efficient and Selective Nickel-Catalyzed Direct N-Alkylation of Anilines with Alcohols
Vellakkaran, Mari,Singh, Khushboo,Banerjee, Debasis
, p. 8152 - 8158 (2017/12/08)
Herein, we developed an efficient and selective nickel-catalyzed monoalkylation of various primary alcohols with aryl and heteroaryl amines together with diols and amino alcohol derivatives. Notably, the catalytic protocol consisting of an earth-abundant and non-precious NiBr2/L1 system enables the transformations in the presence of hydroxyl, alkene, nitrile, and nitro functionalities. As a highlight, we have demonstrated the alkylation of diamine, intramolecular cyclization to N-heterocycles, and functionalization of complex vitamin E, an (±)-α-tocopherol derivative. Preliminary mechanistic studies revealed the participation of a benzylic C-H bond in the rate-determining step.
Erythromycin A ketolide antibiotic derivatives containing quinoline substituent group, and preparation methods and applications thereof
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, (2016/10/08)
The invention discloses a series of erythromycin A ketolide antibiotic derivatives containing quinoline substituent group, represented by a formula I. The invention also provides preparation methods and applications of the derivatives, and side-chain inte
Design, synthesis and antimycotic activity of (N-heteroaryl)arylmethanamines
Ballistreri, Alberto,Bottino, Alessandra,Musumarra, Giuseppe,Fioravanti, Rossella,Biava, Mariangela,Porretta, Giulio Cesare,Simonetti, Nicola,Villa, Adelaide
, p. 61 - 65 (2007/10/03)
The design, synthesis and antimycotic activities or 18 (N-heteroaryl)arylmethanamines are reported. The MIC against Candida strains of the most active amine, 3-(p-methylbenzylamino)quinoline, is comparable to that of pyrrolnitrin.
Research on antibacterial and antifungal agents. XI. Synthesis and antimicrobial activity of N-heteroaryl benzylamines and their schiff bases
Fioravanti,Biava,Porretta,Landolfi,Simonetti,Villa,Conte,Porta-Puglia
, p. 123 - 132 (2007/10/02)
The synthesis and antimicrobial activity of new N-heteroaryl benzylamines and their Schiff bases are reported. Antifungal data were compared with those obtained with miconazole, ketoconazole, enilconazole and imazalil sulfate, which showed that some of the tested compounds possessed moderate activity against strains of Candida albicans, Candida Sp and good activity against isolates of plant pathogenic fungi. In contrast the synthesized compounds showed poor antibacterial activity, except for 3j which exhibited abetter activity than nalidixic acid used as positive control. The results obtained are discussed on the basis of structure-activity relationships.
ELECTRON IMPACT MASS SPECTRA OF para-SUBSTITUTED N-HETEROARYL BENZYLAMINES
Fioravanti, Rossella,Biava, Mariangela,Poretta, Giulio Cesare,Foti, Salvatore,Masumarra, Giuseppe,Saletti, Rosaria
, p. 367 - 378 (2007/10/02)
The 70 eV electron impact mass spectra of some para-substituted N-heteroaryl benzylamines, synthesized through the corresponding Schiff bases, are reported.Typical fragmentation patterns are discussed with the aid of mass analyzed ion kinetic energy spectra and exact mass measurements.The compounds are relatively stable under electron impact, the molecular ion being the base peak or the second most intense ion in the spectra.The dominating breakdown process is the benzylic cleavage, that gives rise to the base peak in some of the investigated compounds and to the second intense peak in others.
SYNTHESIS OF 2,3-FUSED QUINOLINES FROM 3-SUBSTITUTED QUINOLINE 1-OXIDES. PART III. INTRAMOLECULAR CYCLIZATION OF QUINOLINE 1-OXIDES BEARING ACTIVE METHYLENE GROUPS AT THE 3-POSITION IN THE PRESENCE OF ACETIC ANHYDRIDE
Miura, Yutaka,Fujimura, Yasuo,Takaku, Sakae,Hamana, Masamoto
, p. 693 - 699 (2007/10/02)
3-N-Alkylcyanoacetamidoquinoline 1-oxides (3a and 3c) react with Ac2O at room temperature in chloroform to afford 1-alkyl-3-cyano-4H-pyrroloquinolin-2-ones (4a and 4c).The cyclization of 3-N-alkylethoxycarbonylacetamidoquinoline 1-oxides (3b and 3d) occurs upon heating with Ac2O at 60 deg C. 3-(3,3-Dicyanopropoxy)quinoline 1-oxide (5) also cyclizes to the pyranoquinoline (6) when treated with Ac2O at room temperature in chloroform-DMF.
