- Asymmetric synthesis of fluorinated L-tyrosine and meta-L-tyrosines
-
A convenient asymmetric synthesis of (2S)-2-amino-3-(2-fluoro-5-hydroxyphenyl) propanoic acid, (2S)-2-amino-3-(4-fluoro-3-hydroxyphenyl) propanoic acid and (2S)-2-amino-3-(2-fluoro-4-hydroxyphenyl) propanoic acid is described.Key steps include the synthes
- Monclus, Michel,Masson, Carine,Luxen, Andre
-
-
Read Online
- Nucleophilic aromatic substitution of unactivated fluoroarenes enabled by organic photoredox catalysis
-
Nucleophilic aromatic substitution (SNAr) is a classical reaction with well-known reactivity toward electron-poor fluoroarenes. However, electron-neutral and electron-rich fluoro(hetero)arenes are considerably underrepresented. Herein, we present a method for the nucleophilic defluorination of unactivated fluoroarenes enabled by cation radical-accelerated nucleophilic aromatic substitution. The use of organic photoredox catalysis renders this method operationally simple under mild conditions and is amenable to various nucleophile classes, including azoles, amines, and carboxylic acids. Select fluorinated heterocycles can be functionalized using this method. In addition, the late-stage functionalization of pharmaceuticals is also presented. Computational studies demonstrate that the site selectivity of the reaction is dictated by arene electronics.
- Nicewicz, David A.,Pistritto, Vincent A.,Schutzbach-Horton, Megan E.
-
supporting information
p. 17187 - 17194
(2020/11/02)
-
- Synthesis and Biological Evaluation of 1,2,3-triazole tethered Pyrazoline and Chalcone Derivatives
-
A series of pyrazoline derivatives and corresponding chalcone intermediates with substituents same as combretastatin-A4(CA-4) conjugated with triazole nucleus has been synthesized and evaluated for their anticancer potential. Sulphorhodamine B(SRB) assay indicated compound 12c to be the most active compound from the series with GI50 value of 6.7 μm against the human liver carcinoma cell line HepG2. Interestingly, the intermediate 11c exhibited more promising cytotoxicity demonstrating GI50 value of 1.3 μm against the prostate cancer cell line DU145. Compounds 11c and 12c caused accumulation of cells in G2/M phase and inhibited tubulin polymerization. Furthermore, these compounds reduce the mitochondrial membrane potential and activate caspases 3 and 9, thereby indicating their ability to trigger apoptosis.
- Hussaini, Syed Mohammed Ali,Yedla, Poornachandra,Babu, Korrapati Suresh,Shaik, Thokhir B.,Chityal, Ganesh Kumar,Kamal, Ahmed
-
-
- COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF
-
The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.
- -
-
Paragraph 0162; 0163
(2015/05/05)
-
- COMPOUND OF CAMPTOTHECIN AND PREPARATION AND USE THEREOF
-
The present disclosure relates to a compound of formula I, a pharmaceutical composition thereof and the use thereof as an anti-tumor drug.
- -
-
Paragraph 0218; 0219
(2015/06/24)
-
- Anti-tubercular agents. Part 8: Synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles
-
A series of 5-nitrofuran-triazole conjugates were synthesized and evaluated for their antimicrobial activity against both Gram-positive and Gram-negative bacterial strains. All the compounds exhibited promising inhibition towards Gram-positive pathogenic strains, while mild inhibitory effects were observed towards Gram-negative bacterial strains. Some of the compounds 8a, 8b, 8e, 8f, 8h are most active among the series exhibiting MIC value of 1.17 μg/ml against different bacterial strains. The bactericidal activity is found to be in accordance with the bacterial growth inhibition data. Compound 8e was found to be equipotent to the standard drug Ciprofloxacin displaying MBC value of 1.17 μg/ml against the bacterial strain Bacillus subtilis. The compounds have also demonstrated promising antibacterial activity against the resistant strain MRSA and were found to be effective inhibitors of biofilm formation. The compound 8b exhibited excellent anti-biofilm activity with IC50 value as low as 0.8 μg/ml. These conjugates were also screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain. Compound 8e showed promising antitubercular activity with MIC value of 0.25 μg/ml. Most of these compounds are less toxic to normal mammalian cells than the widely used antibacterial drug Ciprofloxacin.
- Kamal, Ahmed,Hussaini, Syed Mohammed Ali,Faazil, Shaikh,Poornachandra,Narender Reddy,Kumar, C. Ganesh,Rajput, Vikrant Singh,Rani, Chitra,Sharma, Rashmi,Khan, Inshad Ali,Jagadeesh Babu
-
p. 6842 - 6846
(2014/01/06)
-
- Piperazine derivatives
-
This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
- -
-
Page/Page column 24
(2010/02/15)
-
- Synthesis of high-specific-radioactivity 4- and 6-[18F]fluorometaraminol- PET tracers for the adrenergic nervous system of the heart
-
Fluorine-18 (t12:109.8min)-labeled analogues of metaraminol, 4-[18F]FMR ((1R,2S)-2-amino-1-(4-[18F]fluoro-3-hydroxy phenyl)-1-propanol) and 6-[18F]FMR ((1R,2S)-2-amino-1-(2-[18F]fluoro-5-hydroxyphenyl)-1-propanol), were synthesized as new positron-emission-tomography (PET) tracers for mapping cardiac adrenergic nerve terminals. Copyright
- Langer, Oliver,Dollé, Frédéric,Valette, Héric,Halldin, Christer,Vaufrey, Fran?oise,Fuseau, Chantal,Coulon, Christine,Ottaviani, Michéle,N?gren, Kjell,Bottlaender, Michel,Maziére, Bernard,Crouzel, Christian
-
p. 677 - 694
(2007/10/03)
-
- Synthesis and Dopamine Receptor Affinities of 2-(4-fluoro-3-hydroxyphenyl)ethylamine and N-Substituted Derivatives
-
The synthesis of 2-(4-fluoro-3-hydroxyphenyl)ethylamine (26) and of some N,N-dialkyl derivatives (27-30) starting from 4-fluoro-3-hydroxytoluene and their in vitro binding affinities for dopamine (DA) receptor are reported.The amine 26 can be regarded as
- Claudi, Francesco,Cardellini, Mario,Cingolani, Gian Mario,Piergentili, Alessandro,Pertuzzi, Guidubaldo,Balduini, Walter
-
p. 2408 - 2412
(2007/10/02)
-