- Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: A first round of lead optimization
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Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly patients, and is characterized by progressive loss of articular cartilage. Among the various matrix metalloproteinases (MMPs), MMP-13 is specifically expresse
- La Pietra, Valeria,Marinelli, Luciana,Cosconati, Sandro,Di Leva, Francesco Saverio,Nuti, Elisa,Santamaria, Salvatore,Pugliesi, Isabella,Morelli, Matteo,Casalini, Francesca,Rossello, Armando,La Motta, Concettina,Taliani, Sabrina,Visse, Robert,Nagase, Hideaki,Da Settimo, Federico,Novellino, Ettore
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experimental part
p. 143 - 152
(2012/03/09)
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- Efficient, stereoselective approach to the synthesis of 3-(1-Phenyl-2-(Z-styrylsulfonyl)-1H-imidazol-4-yl)-2H-chromen-2-ones
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Reaction of phenyl acetylene with 3-(1-aryl-2-mercapto-4-imidazolyl)-2H-1- benzopyran-2-ones (4) in the presence of sodium hydroxide in absolute ethanol led to the formation of 3-(1-phenyl-2-(Z-styrylthio)-1H-imidazol-4-yl)-2H- chromen-2-ones (6) in excel
- Guravaiah, Nalajam,Rao, Vedula Rajeswar
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p. 1167 - 1174
(2011/05/06)
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- Synthesis of 3-(1-aryl-2-mercapto-imidazolyl)-2H-1-benzopyran-2-one derivatives
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Reaction of 3-(2-bromoacetyl) coumarins with various substituted aromatic primary amines resulted in the formation of 3-(2-anilino acetyl) coumarins 1 which on subsequent reaction with potassium thiocyanate furnishes corresponding 3-(1-aryl-2-mercapto-imi
- Kumar, Ravi V.,Rao, V. Rajeswar
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p. 415 - 418
(2007/10/03)
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- α,β-UNSATURATED KETONES AND ANILIDES OF THE COUMARIN SERIES IN THE SYNTHESIS OF ISOXAZOLE, IMIDAZOLE, AND PYRAZOLE DERIVATIVES
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Coumarin-containing unsaturated ketones react with bromine to give dibromides, which form derivatives of isoxazoles and pyrazoles via reaction with hydroxylamine hydrochloride or phenylhydrazine.A method for preparing coumarin-containing imidazoles from the corresponding anilides was elaborated.
- Skripskaya, O. V.,Yagodinets, P. I.,Chernyuk, I. N.
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p. 1625 - 1627
(2007/10/03)
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- 3-α-Bromacetyl-coumarines as Synthones for Heterocyclic Substituted Coumarines
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3-α-Bromacetyl-coumarines 2 react easily and in high yields with thiourea and thioamide derivatives 3 and 5, resp., to 4-coumar-3'-yl-thiazoles 4 and 6, resp., as well as with N,N-disubstituted thioamides 11 and N,N,N',N'-tetraalkylthiourea 12 to 5-coumar-3'-yl-oxathioliumsalts 13 and 14, respectively.In a two-step reaction 2 can be transformed by reaction with aniline 17 to 4-coumar-3'-yl-imidazoles 21 and 5-coumar-3'-yl-oxazoliumsalts 22, resp., via aminoketone intermediates 18.
- Czerney, P.,Hartmann, H.
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p. 551 - 560
(2007/10/02)
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