- Novel benzenesulfonamide-bearing pyrazoles and 1,2,4-thiadiazoles as selective carbonic anhydrase inhibitors
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Two series comprising 20 novel benzenesulfonamides bearing thioureido-linked pyrazole 8 and amino-1,2,4-thiadiazole 10 were synthesized and assayed as human carbonic anhydrase (hCA) inhibitors against isoforms I and II as well as the tumor-associated isof
- Kumar, Rajiv,Kumar, Amit,Ram, Sita,Angeli, Andrea,Bonardi, Alessandro,Nocentini, Alessio,Gratteri, Paola,Supuran, Claudiu T.,Sharma, Pawan K.
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- A general and efficient approach to 2H-indazoles and 1H-pyrazoles through copper-catalyzed intramolecular N-N bond formation under mild conditions
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A new efficient copper-catalyzed intramolecular amination reaction has been developed to readily synthesise a wide variety of multi-substituted 2H-indazole and 1H-pyrazole derivatives from easily accessible starting materials under mild conditions. A highly selective ligand for estrogen receptor β was prepared in three steps by employing this method. The Royal Society of Chemistry 2011.
- Hu, Jiantao,Cheng, Yongfeng,Yang, Yiqing,Rao, Yu
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supporting information; experimental part
p. 10133 - 10135
(2011/10/09)
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- Synthesis and biological screening of a combinatorial library of β-chlorovinyl chalcones as anticancer, anti-inflammatory and antimicrobial agents
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A combinatorial library of β-chlorovinyl chalcones (4) were synthesized by Claisen-Schmidt condensation reaction. Catalytic reaction of substituted 3-chloro-3-phenyl-propenal (2) and 1-(2,4-dimethoxy-phenyl)-ethanone or 1-(4-methoxy-phenyl)-ethanone (3) i
- Bandgar, Babasaheb P.,Gawande, Shrikant S.
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experimental part
p. 2060 - 2065
(2010/06/12)
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- Synthesis and biological evaluation of β-chloro vinyl chalcones as inhibitors of TNF-α and IL-6 with antimicrobial activity
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A series of β-chloro vinyl chalcones have been synthesized by Claisen-Schmidt condensation. β-chloro vinyl aldehyde has been synthesized by the Vilsmayer-Hack formylation reaction. The structures of the newly synthesized compounds were confirmed by 1H NMR, IR and Mass spectral analysis. All the compounds were evaluated for their anti-inflammatory activity (against TNF-α and IL-6) and antimicrobial (antibacterial and antifungal) activity. Compounds 5a, 5d, 5e, 5g and 5i exhibited promising activity against IL-6 with 58-83% inhibition at 10 μM concentration. None of the compound was found to be cytotoxic in CCK-8 cells at 10 μM concentration. Whereas compounds 5b, 5d, 5e and 5i showed very good antibacterial activity and compounds 5a, 5b, 5e and 5i showed good antifungal activity.
- Bandgar, Babasaheb P.,Patil, Sachin A.,Korbad, Balaji L.,Nile, Shivraj H.,Khobragade, Chandrahase N.
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scheme or table
p. 2629 - 2633
(2010/07/09)
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- SYNTHESIS OF NEW 2,5-DIARYL SELENOPHENES
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A synthesis of 2,5-parasubstituted diaryl selenophenes is described. β-Aryl-β-chloro acroleins, easily prepared from substituted acetophenones and Vilsmaier-Haack reagent, are condensed with appropriate benzylbromide derivatives to give the title compound
- Prim, Damien,Joseph, Delphine,Kirsch, Gilbert
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p. 137 - 144
(2007/10/02)
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