- Optimization strategy of single-digit nanomolar cross-class inhibitors of mammalian and protozoa cysteine proteases
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Cysteine proteases (CPs) are involved in a myriad of actions that include not only protein degradation, but also play an essential biological role in infectious and systemic diseases such as cancer. CPs also act as biomarkers and can be reached by active-
- Cianni, Lorenzo,Rocho, Fernanda dos Reis,Rosini, Fabiana,Bonatto, Vinícius,Ribeiro, Jean F.R.,Lameira, Jer?nimo,Leit?o, Andrei,Shamim, Anwar,Montanari, Carlos A.
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- Synthesis of: N -unsubstituted cycloalkylimines containing a 4 to 8-membered ring
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Primary cycloalkylimines with a 4 to 8-membered ring were synthesized by dehydrocyanation of the corresponding α-aminonitriles on solid potassium hydroxide via a vacuum gas-solid reaction. Imine-enamine tautomerism has been demonstrated at room temperature for the most kinetically stable derivatives.
- Guillemin, Jean-Claude,Nasraoui, Wafa,Gazzeh, Houda
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p. 5647 - 5650
(2019/05/21)
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- Method for easily and conveniently synthesizing 1-amino-1-nitrile-cyclopropane
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The invention discloses a method for easily and conveniently synthesizing 1-amino-1-nitrile-cyclopropane. According to the method, 2,4-bromobutyronitrile is utilized as a starting material and reactswith phthalimide potassium under the base catalysis to generate phthalimide cyclopropanecarbonitrile, and then hydrazinolysis is carried out in ethanol to obtain the 1-amino-1-nitrile-cyclopropane. The method disclosed by the invention has the advantages of mild reaction conditions, relatively high yield, low cost and suitability for industrialized application.
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Paragraph 0010; 0014; 0015; 0016
(2018/03/28)
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- Design, synthesis and antibacterial activity studies of novel quinoline carboxamide derivatives
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A series of novel quinoline-6-carboxamides and 2-chloroquinoline-4- carboxamides were synthesized by the reaction of their analogous carboxylic acids with various amine derivatives in the presence of base TEA and protecting agent BOP at room temperature.
- Shivaraj, Yellappa,Naveen, Malenahalli H.,Vijayakumar, Giriyapura R.,Kumar, Doyijode B. Aruna
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p. 241 - 245
(2013/07/25)
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- Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
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A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
- Guay, Daniel,Beaulieu, Christian,Jagadeeswar Reddy,Zamboni, Robert,Methot, Nathalie,Rubin, Joel,Ethier, Diane,David Percival
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scheme or table
p. 5392 - 5396
(2010/05/02)
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