The flavonoid phlorizin was isolated from the bark of apple trees and shown to cause glucosuria. Phlorizin is an inhibitor of sodium glucose cotransporters (SGLT1 and SGLT2). With phlorizin as lead compound, specific inhibitors of SGLT2 were developed in the last decade and some of them have been approved for treatment mainly of type 2 diabetes. Inhibition of SGLT2 eliminates excess glucose via the urine. In recent times, the dual SGLT1/SGLT2 inhibitory activity of phlorizin has served as a model for the development and testing of new drugs exhibiting both activities.

Xemilofiban [SC 54684, SC 54684A (HCl), xemlofiban], an orally active antiplatelet agent, is a glycoprotein IIb/IIIa receptor antagonist. This drug was in a phase III clinical trial in the US and Europe for the treatment of thrombosis in patients with unstable angina pectoris and acute myocardial infarction undergoing angioplasty. Because of insufficient evidence of efficacy and concerns about safety over this long of a period of treatment, these trials didn’t get the market approval. In Japan, Sankyo discontinued the development of xemilofiban for thrombosis at phase II following Searle's decision to drop the project.

Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Tulobuterol is a long-acting beta2-adrenergic receptor agonist. Tulobuterol has almost no effects on blood pressure and heart rate and is highly selective for the tracheal muscle. It is indicated to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, bronchitis, chronic obstructive pulmonary disease (COPD) and emphysema. Serious side effects detected were: tremor, palpitations and serum potassium level decrease.

Efonidipine is a 1,4-dihydropyridine derivative for the treatment of hypertension and angina. Efonidipine exerts its antihypertensive and antianginal effects through blocking L- and T-type calcium channels.

Subarachnoid haemorrhage (SAH) following cerebral aneurysm rupture or trauma can result in the induction of secondary ischaemic brain damage via a decrease in microvascular perfusion, a disruption of the blood-brain barrier and consequent vasogenic oedema, and the delayed spasm of the major cerebral arteries (i.e. vasospasm). It is increasingly apparent that oxygen radical-induced, iron-catalyzed lipid peroxidation (LP) within the subarachnoid blood and vascular wall plays a key role in the occurrence of these secondary events. Tirilazad mesylate, is a nonglucocorticoid, 21-aminosteroid, is a potent cytoprotective inhibitor of LP that works by a combination of radical scavenging and membrane stabilizing properties. It has been demonstrated to attenuate the acute and delayed vascular consequences of SAH and to protect the brain against ischaemic insults. Tirilazad mesylate has been proposed to treat acute ischaemic stroke. When tested on animal models, tirilazad protects brain tissue, and reduces brain damage. However, the drug fails to treat, and even worsens a stroke when studied on a human being.

Diamminedichlorodihydroxyplatinum IV is the platinum-based antineoplasticis agent. Oxaliplatin is cis, cis, trans- isomer of Diamminedichlorodihydroxyplatinum IV. Oxaliplatin show high stability and therefore can be utilized orally for outpatient care. Although oxoplatin is capable of binding directly to DNA after prolonged incubation, platinum(IV) agents are considered to be largely inert prodrugs that are converted to highly cytotoxic platinum(II) compounds by reducing substances, enzymes, or microenvironmental conditions. Reaction of oxoplatin with 0.1 M hydrogen chloride mimicking gastric acid yields cis-diammine-tetrachlorido-platinum(IV) (DATCP[IV]), which exhibits two-fold increased activity. The oxoplatin metabolite DATCP(IV) constitutes a potent cytotoxic derivative that may be produced by gastric acid or acidic areas prevailing in larger solid tumors, depending on the respective pharmaceutical formulation of oxoplatin.

Nitroblue Tetrazolium (NBT) is a chromogenic substrate that, like other tetrazolium compounds, can be reduced to produce a colored formazan derivative. Conventionally, a semi-quantitative microscopic NBT assay is used to determine the production of superoxide anion (O2(-)) in various phagocytic cells. This microscopic assay is conducted by counting the cells containing blue NBT formazan deposits, which are formed by reduction of the membrane permeable, water-soluble, yellow-colored, nitroblue tetrazolium (Y-NBT) by O2(-). NBT test, the oldest and most recognized diagnostic test for chronic granulomatous disease (CGD), relies on light microscopy to provide a mostly qualitative determination of phagocyte NADPH oxidase activity: production of blue reduced NBT formazan in normal cells but not in those from patients with CGD. NBT can also be used as a chromogenic activity stain for oxidoreductases in gels or solutions. More commonly NBT is often paired with 5-bromo-4-chloro-3-inolyl phosphate (PCIB) for the colorimetric detection of alkaline phosphatase activity. Alkaline phosphate converts PCIB to a product that reduces NBT to its formazan derivative, resulting in a black-purple precipitate.

Prolonium is a quartenary amine derivative. Prolonium iodide has been given by injection as a source of iodine as part of the treatment of thyroid storm and for the pre-operative management of hyperthyroidism. It is marketed in Italy for veterinary use for the treatment of infectious granulomas, in the various forms of actinomycosis actinobacillosis of the tongue, larynx, pharynx, skin and subcutaneous connective tissue.

Chlorbenzoxamine is an antimuscarinic agent used for the treatment of peptic ulcer disease and other functional gastrointestinal disorders. Chlorbenzoxamine, a structural analog of hydroxyzine, produces a unique antagonism of gastric ulceration induced in rats and dogs by various procedures. This effect is not accompanied by a significant gastric secretory depression or a reduction in gastric acid concentration. Chlorbenzoxamine does not show anticholinergic or antihistaminic activity in vitro but does produce a nonspecific depression of isolated smooth muscle. The antiulcer effect of chlorbenzoxamine in rats is abolished by hypophysectomy suggesting a central or endocrine mechanism of action.