The present invention relates to the compound (E,Z)-ajoene of formula (1) for use in treatment of bacterial infections. Another aspect of the present invention is a composition comprising (E,Z)-ajoene of formula (1) and at least one antibiotic. Yet another aspect of the invention relates to a method for manufacturing (E,Z) ajoene of formula (1) wherein the conformation of the internal CC bond can be either E or Z or a mixture thereof, said method comprising reacting allicin of formula (3) with an acid in the presence of a solvent to provide (E,Z ajoene) of formula (1) as defined above. Yet another aspect of the invention is (E,Z)-ajoene of formula 1 obtainable by the method described above.

The present invention relates to the compound (E,Z)-ajoene of formula (1) for use in treatment of bacterial infections. Another aspect of the present invention is a composition comprising (E,Z)-ajoene of formula (1) and at least one antibiotic. Yet another aspect of the invention relates to a method for manufacturing (E,Z) ajoene of formula (1) wherein the conformation of the internal CC bond can be either E or Z or a mixture thereof, said method comprising reacting allicin of formula (3) with an acid in the presence of a solvent to provide (E,Z ajoene) of formula (1) as defined above. Yet another aspect of the invention is (E,Z)-ajoene of formula 1 obtainable by the method described above.

Provided is a method for producing a polythiol compound, including reacting 2-mercaptoethanol with an epihalohydrin, wherein the reaction is carried out in the presence of a halide selected from the group consisting of a 2,3-dihalogeno-1-propanol and an allyl halide, and an amount of the halide in the reaction is more than 0.50% by mass and 10.00% by mass or less with respect to the total amount of the halide and the epihalohydrin. Also provided are a method for producing a curable composition, including producing a polythiol compound by the abovementioned production method, and a method for producing a cured product, including producing a curable composition by the abovementioned production method.

Provided is a method for producing a polythiol compound, including reacting 2-mercaptoethanol with an epihalohydrin, wherein the reaction is carried out in the presence of a halide selected from the group consisting of a 2,3-dihalogeno-1-propanol and an allyl halide, and an amount of the halide in the reaction is more than 0.50% by mass and 10.00% by mass or less with respect to the total amount of the halide and the epihalohydrin. Also provided are a method for producing a curable composition, including producing a polythiol compound by the abovementioned production method, and a method for producing a cured product, including producing a curable composition by the abovementioned production method.

The present invention relates to a process for producing ajoene from allicin via a polymeric substrate, comprising the steps of heating allicin or an allicin solution at a predetermined temperature range such that at least a portion of the allicin is converted to ajoene to form an ajoene solution; and separating the ajoene from the ajoene solution; wherein at least one of the heating or separating steps is conducted via a polymeric substrate. The process for producing ajoene from allicin via a polymeric substrate further comprises a step of retaining the allicin or the allicin solution on the polymeric substrate before the heating step is conducted within or out of the polymeric substrate. The present invention also relates to ajoene or a composition comprising ajoene obtained by the process thereof.

The present invention relates to a process for producing ajoene from allicin via a polymeric substrate, comprising the steps of heating allicin or an allicin solution at a predetermined temperature range such that at least a portion of the allicin is converted to ajoene to form an ajoene solution; and separating the ajoene from the ajoene solution; wherein at least one of the heating or separating steps is conducted via a polymeric substrate. The process for producing ajoene from allicin via a polymeric substrate further comprises a step of retaining the allicin or the allicin solution on the polymeric substrate before the heating step is conducted within or out of the polymeric substrate. The present invention also relates to ajoene or a composition comprising ajoene obtained by the process thereof.

The present invention relates to a process for producing ajoene from allicin via a polymeric substrate, comprising the steps of heating allicin or an allicin solution at a predetermined temperature range such that at least a portion of the allicin is converted to ajoene to form an ajoene solution; and separating the ajoene from the ajoene solution; wherein at least one of the heating or separating steps is conducted via a polymeric substrate. The process for producing ajoene from allicin via a polymeric substrate further comprises a step of retaining the allicin or the allicin solution on the polymeric substrate before the heating step is conducted within or out of the polymeric substrate. The present invention also relates to ajoene or a composition comprising ajoene obtained by the process thereof.

The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).

##STR00001##

The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).

##STR00001##

Herein is described a method to rapidly screen a large chemical space for a compound that binds to a target protein through an iterative fragment assembly approach that can be performed at low reagent cost and without requiring purification of the assembled product. The method employs a library of test ligands each of which comprise a bait molecule, which is known from prior art or prior screening to have some intrinsic affinity for the target protein, and a test moiety.