- A method for esterification reaction rate prediction of aliphatic monocarboxylic acids with primary alcohols in 1,4-dioxane based on two parametrical taft equation
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Esterification reaction rates of aliphatic monocarboxylic acids with primary alcohols in 1,4-dioxane as inert solvent were investigated. Acids were esterified with 1-propanol and alcohols with acetic acid as model reactants at a constant temperature of 60°C, at a fixed ionic strength and pH in a batch reactor with a constant volume. For evaluation of reaction rates, an exact kinetic equation for the equilibrium reaction was applied. Under these conditions and for low reactants, concentrations reaction rate depends only on the structure of reactants and, therefore, can be predicted by a correlation equation with two Taft coefficients (inductive and steric effects). From these equations, it is possible to estimate the esterification reaction rate constant for other acid-alcohol pairs. This methodology may also be suitable for other kinetic systems measured under comparable experimental conditions.
- Vojtko, Jan,Tomcik, Peter
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p. 189 - 196
(2014/02/14)
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- Aryloxyacetic esters structurally related to α-Asarone as potential antifungal agents
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A series of aryloxyacetic ester analogues 8-13 was synthesized based on the potential pharmacophores of the antifungal agents α-Asarone (1) and 2-5. Their antifungal activity was tested in vitro for their growth inhibitory activities against pathogenic fungi. The in vitro antifungal evaluation of these alkyl and aryl esters shows that derivatives 10 displayed the highest antifungal and fungicidal activities against Cryptococcus neoformans and C. gattii. These results support the idea that the phenoxyacetic frame is a potent pharmacophore for the design of potential antifungal drugs. Graphical Abstract: [Figure not available: see fulltext.]
- Jimenez, Fabiola,Cruz, Maria Del Carmen,Zuniga, Clara,Martinez, Maria A.,Chamorro, German,Diaz, Francisco,Tamariz, Joaquin
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experimental part
p. 33 - 57
(2010/10/20)
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- Heterocyclic compouds
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A compound of the general formula wherein: n is 0 or 1; M1 is an amino group; Q is an aromatic heterocyclic group containing a basic nitrogen atom; M2 is an imino group; L is a template group; and A is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group; and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.
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- Heterocyclic derivatives
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Compounds of formula I STR1 and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R13, M2, X1, Z1, Z1a, X2 and A1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.
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- Heterocyclic derivatives
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Compounds of formula I STR1 and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R13, M2, X1, Z1, Z1a, X2 and A1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.
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