A novel guanidine compound having excellent fungicidal activity is represented by formula [I]. (In the formula, Y represents a divalent group represented by formula [II] (wherein each of R.sup.7-R.sup.9 independently represents a hydrogen atom or the like) or the like; each of X and Z independently represents an unsubstituted or substituted alkylene group or the like; each of Q.sup.1 and Q.sup.2 independently represents a single bond or the like; each of A.sup.1 and A.sup.2 independently represents an unsubstituted or substituted divalent heterocyclic compound residue or the like; and each of R.sup.1-R.sup.6 independently represents a hydrogen atom or the like.)

##STR00001##

With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against Staphylococcus aureus (MIC900.25 g/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies.

With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against Staphylococcus aureus (MIC900.25 g/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies.

Sirt5, a mitochondrial Sirtuin, has been identified herein as an efficient demalonylase and desuccinylase. Disclosed herein are assays to identify Sirt5 modulators based on this robust enzymatic activity. Sirt5-specific modulators can be used study the biological function of Sirt5 and to target Sirt5 activities in treating human diseases.

Sirt5, a mitochondrial Sirtuin, has been identified herein as an efficient demalonylase and desuccinylase. Disclosed herein are assays to identify Sirt5 modulators based on this robust enzymatic activity. Sirt5-specific modulators can be used study the biological function of Sirt5 and to target Sirt5 activities in treating human diseases.

The present disclosure encompasses compositions and methods for the treatment of precancerous skin lesions. Compositions of the invention comprise a cytotoxic agent and a thymic stromal lymphopoietin (TSLP) inducer.

The present disclosure encompasses compositions and methods for the treatment of precancerous skin lesions. Compositions of the invention comprise a cytotoxic agent and a thymic stromal lymphopoietin (TSLP) inducer.

1,5-dihydro-2,4-benzodiazepine-3-one derivatives, such as a compound represented by formula I, acts on 5-HT.sub.2A and 5-HT.sub.2C receptors. The selectivity for 5-HT.sub.2A is superior or similar to pimavanserin. The derivative is used for treating schizophrenia or Parkinson's disease, dementia-related behavioral disorders, and psychosis. The antipsychotic activity of the compound is equivalent to that of pimavanserin, the side effects of sedation and worsening of exercise are less than those of pimavanserin, and cardiotoxicity is less than that of pimavanserin. ##STR00001##