- Discovery of novel oxazole-based macrocycles as anti-coronaviral agents targeting SARS-CoV-2 main protease
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We have discovered a family of synthetic oxazole-based macrocycles to be active against SARS-CoV-2. The synthesis, pharmacological properties, and docking studies of the compounds are reported in this study. The structure of the new macrocycles was confir
- Al-Wahaibi, Lamya H.,Mostafa, Ahmed,Mostafa, Yaser A.,Abou-Ghadir, Ola F.,Abdelazeem, Ahmed H.,Gouda, Ahmed M.,Kutkat, Omnia,Abo Shama, Noura M.,Shehata, Mahmoud,Gomaa, Hesham A.M.,Abdelrahman, Mostafa H.,Mohamed, Fatma A.M.,Gu, Xuyuan,Ali, Mohamed A.,Trembleau, Laurent,Youssif, Bahaa G.M.
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- Barbituric acid derivatives as inhibitors of TNF-alpha converting enzyme (TACE) and/or matrix metalloproteinases
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The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R4, R5, n, W, U, X, Y, Z, U
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- Synthesis of a second-generation pseudopeptide platform
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A synthetic pathway is presented to a functionalized pseudopeptide molecular platform for use in supramolecular and solution-phase combinatorial chemistry. The platform contains amino acids with quaternary asymmetric centers, the configurations of which are determined by the method of synthesis. (C) 2000 Elsevier Science Ltd.
- Haberhauer, Gebhard,Somogyi, László,Rebek Jr., Julius
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p. 5013 - 5016
(2007/10/03)
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- Synthesis and reduction of endothiodipeptides containing malonic acid derivatives
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Amides of malonic acid derivatives and protected dipeptides containing amine malonic acid have been synthesized and converted into the corresponding monothio analoga and endothiedipeptides. By reduction of the thioamides terminal protected β-carboxy amine derivatives were obtained. Reduction of endothiodipeptides containing amine malonic acid as the carboxy component resulted in protected Ψ[CH2NH] pseudodipeptides for the use as dipeptide substitutes with proteolytic resistance.
- Krumme, Dirk,Tschesche, Harald
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p. 3007 - 3018
(2007/10/03)
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- Dimethyl Aminomalonate: A Useful C-3 Unit in a Mild, Direct Synthesis of Oxazole-4-carboxylates
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N-Acyl derivatives of the title compound undergo oxidative cyclization upon treatment with N-chlorosuccinimide in DMF to form dimethyl 4,5-dihydro-5-(phenylthio)oxazole-4,4-dicarboxylates 4 which then are decarbomethoxylated with concomitant loss of thiop
- Shapiro, Rafael
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p. 5759 - 5764
(2007/10/02)
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- Total synthesis of the biphenomycins; V. Synthesis of biphenomycin A
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The total synthesis of biphenomycin A is described. Two of the five stereogenic centres were formed by enantioselective hydrogenation of the corresponding didehydroamino acids using the rhodium-DIPAMP catalyst and the two stereogenic centres of the α-amin
- Schmidt,Leitenberger,Griesser,Schmidt,Meyer
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p. 1248 - 1254
(2007/10/02)
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