The present technology provides a system for monitoring quorum-sensing in bacteria comprising bacteria that release at least one membrane-lytic toxin when the bacteria are at a quorum-sensing density; synthetic lipid vesicles comprising an environmentally sensitive indicator, wherein the synthetic lipid vesicles release the environmentally sensitive dye in the presence of an effective amount of the membrane-lytic toxins; and a growth medium; wherein the bacteria and synthetic lipid vesicles are in contact with the growth medium. Methods using the system and compounds discovered with the system (e.g., compounds of Formulas I and II) are also disclosed.

The present technology provides a system for monitoring quorum-sensing in bacteria comprising bacteria that release at least one membrane-lytic toxin when the bacteria are at a quorum-sensing density; synthetic lipid vesicles comprising an environmentally sensitive indicator, wherein the synthetic lipid vesicles release the environmentally sensitive dye in the presence of an effective amount of the membrane-lytic toxins; and a growth medium; wherein the bacteria and synthetic lipid vesicles are in contact with the growth medium. Methods using the system and compounds discovered with the system (e.g., compounds of Formulas I and II) are also disclosed.

Thromboxane A2 receptor antagonists, such as ifetroban, inhibit solid tumor metastasis. The formation of surface and microscopic lung metastases are inhibited. Thromboxane A2 receptor antagonists can inhibit the tumor metastasis process without affecting the growth or development of a primary tumor.

A transdermal therapeutic system containing rotigotine base in a self-adhesive layer structure. The system includes a backing layer, and a rotigotine-containing biphasic layer. The biphasic layer has an outer phase having a composition including 75% to 100% of a polymer or a polymer mixture, and an inner phase that forms dispersed deposits in the outer phase. The inner phase includes rotigotine base and a polymer mixture of at least two hydrophilic polymers. The hydrophilic polymers are selected from the group of polyvinylpyrrolidones having a K-Value of at least 80, polyvinylpyrrolidones having a K-Value of less than 80, copolymers of vinyl caprolactam, vinylacetate and ethylene glycol, copolymers of vinylpyrrolidone and vinylacetate, copolymers of ethylene and vinylacetate, polyethylene glycols, polypropylene glycols, acrylic polymers, and modified celluloses. The polymer mixture in the inner phase is present in an amount sufficient so that it forms a solid solution with the rotigotine base.

A transdermal therapeutic system containing rotigotine base in a self-adhesive layer structure. The system includes a backing layer, and a rotigotine-containing biphasic layer. The biphasic layer has an outer phase having a composition including 75% to 100% of a polymer or a polymer mixture, and an inner phase that forms dispersed deposits in the outer phase. The inner phase includes rotigotine base and a polymer mixture of at least two hydrophilic polymers. The hydrophilic polymers are selected from the group of polyvinylpyrrolidones having a K-Value of at least 80, polyvinylpyrrolidones having a K-Value of less than 80, copolymers of vinyl caprolactam, vinylacetate and ethylene glycol, copolymers of vinylpyrrolidone and vinylacetate, copolymers of ethylene and vinylacetate, polyethylene glycols, polypropylene glycols, acrylic polymers, and modified celluloses. The polymer mixture in the inner phase is present in an amount sufficient so that it forms a solid solution with the rotigotine base.

Provided are 1,4-diphenyl-1H-imidazole and 2,4-diphenylthiazole derivatives having a structure represented by Formula I, a preparation method therefor and uses thereof: ##STR00001##
wherein R.sub.1 is any one of H, OH, and OCH.sub.3, R.sub.2 is any one of H, NO.sub.2, CH.sub.3, CF.sub.3, SO.sub.2CH.sub.3, COOCH.sub.3, or CONHCH.sub.3, R.sub.3 is any one of H, NO.sub.2, OCH.sub.3, or CF.sub.3, R.sub.4 is selected from H, CF.sub.3, or Cl, R.sub.5 is any one of H, Cl, CF.sub.3, or NHCH.sub.3, and R.sub.6 is any one of OCF.sub.3, CF.sub.3, or CN; V is either C or N, W is either CH or N, X is a C atom, Y is either CH or N, and Z is either CH or S. This compound can be used in preparation of anti-inflammatory adjuvants, TLR1 or TLR2 agonists, and anti-tumor agents and for regulating the activity activation level of TLR1 and TLR2 alkaline phosphatases in vitro and in vivo.

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.