Bioactive small molecules are organic compounds that have a low molecular weight (900 daltons). Most pharmaceutical drugs are small molecules. Larger structures such as nucleic acids, proteins, and many polysaccharides are not small molecules.
WF 3681 was isolated from Chaetomella sp. as a novel inhibitor of aldose reductase by researchers at Fujisawa Co. Japan in 1987, exhibiting an IC50 of 2.5 x 10-7 M. WF 3681 does not significantly reduce accumulation of sorbitol in rat sciatic nerves of...
WEB 2086 (apafant) is a potent and selective platelet activating (PAF) antagonist. WEB 2086 has high affinity for guinea pig peritoneal macrophage PAF receptors, dissociating slowly. WEB 2086 at 10-8 to 10-6 mol/L strongly and...
Securinine is a tetracyclic alkaloid isolated from the roots of Securinega suffruticosa with an unusual structure in which the piperidine ring has a skewed boat form and the diene is not coplanar. Securinine inhibits [3H]GABA binding to rat brain...
Indole-3-carboxaldehyde is an endogenous metabolite of plants and is produced in humans by the metabolism of L-tryptophan in Lactobacillus and other gastrointestinal bacteria. Indole-3-carboxaldehyde is an immunomodulator, acting as an agonist of the...
hemi-Oxanthromicin is the monomer of (±)-oxanthromicin, first isolated from a soil-derived Streptomyces sp. by Capon and co-workers in 2014. Unlike its co-metabolites, oxanthromicin and spiro-oxanthromicin, hemi-oxanthromicin does not inhibit...
Fumitremorgin B is a tremorgenic mycotoxin isolated from Aspergillus fumigatus. Fumitremorgin B is active against a range of phytopathogenic fungi including Botrytis cinerea, Alternaria solani and alternata at 6.25 µg/mL. Fumitremorgen B has potent...
Circumdatin A, produced by Aspergillus sp., was first reported in 1999 by Rahbaek and colleagues, University of Copenhagen, Denmark. The structure of circumdatin A was revised as a unique oxepine in 2008 using X-ray crystallography. Lack of availability...
Cinnabarinic acid is an endogenous kynurenine metabolite formed from oxidative dimerization of 3-hydroxyanthranilic acid and transamination of 3-hydroxykynurenine. Cinnabarinic acid activates glutamate receptors by interacting with residues of the...
Simvastatin acid is the active β-hydroxy acid metabolite of simvastatin formed in vivo. Simvastatin acid is a potent inhibitor of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase, an essential enzyme involved in the in vivo synthesis of...
Beauveriolides are 13-membered cyclodepsipeptides isolated from Beauveria sp. Beauveriolide III inhibits acyl-CoA:cholesterol acyltransferase (ACAT) to block the synthesis of cholesteryl ester, leading to a reduction of lipid droplets in macrophages...
Beauveriolides are 13-membered cyclodepsipeptides isolated from Beauveria sp.. Beauveriolides I and III inhibit macrophage acyl-CoA:cholesterol acyltransferase (ACAT) activity to block the synthesis of cholesteryl ester, leading to a reduction of lipid...
Anagyrine is a teratogenic quinolizidine alkaloid found in Lupinus sp. which undergoes metabolism to a piperidine that causes crooked calf syndrome. Anagyrine, but not lupanine or sparteine, directly desensitize nicotinic acetylcholine receptors (nAChR)...