A concept of bioisosterism has attracted much attention in recent years. The success of this strategy in developing new substances which are therapeutically attractive has observed a significant growth in distinct therapeutic classes, being amply used to discover new analogs of commercially attractive therapeutic innovations, and also as a tool useful in the molecular modification.

A lead compound with a desired pharmacological activity may have undesirable characteristics that limit its bioavailability, or structural features which adversely influence its metabolism and excretion from the body. Bioisosterism represents one of the approaches used by the medicinal chemists for rational modification of lead compounds into safer and more clinically effective agents.

Continue Reading

Hydrazine Building Blocks

This issue of Enamine Product Focus represents a family of Building Blocks containing Hydrazine unit. Several aspects of utilizing the hydrazine building blocks for the design of potential drug candidates can be outlined. Despite hydrazines themselves are rarely thought as promising drug candidates, some successful examples of drugs possessing hydrazine moiety can be found, e. g. antiparkinsonic agent Carbidopa (Lodosyn®), antidepressant Phenelzine (Nardil®) or vasodilator Hydralazine (Apresoline®).

Continue Reading

Isomeric Fluoronitrobenzenesulfonyl Chlorides

The synthesis of functional organic compounds for different applications largely relies on laborious approaches involving an extensive usage of protecting groups. Nowadays chemoselective routes to the construction of complex molecules are becoming a good alternative because they shorten the length of multistep syntheses by excluding protecting groups and, as a consequence, lead to increased overall yields.

Continue Reading

Set of Carbamoylimidazoles

Substituted ureas are drawing considerable attention as pharmacologically relevant compounds. Our proprietary trifluorourethanes, reported earlier, are suitable precursors for the preparation of aryl/heteroaryl-alkyl or aryl/heteroaryl-dialkyl urea derivatives via parallel synthesis, but they are not appropriate for the preparation of ureas bearing different alkyl substituents. We report now a new set of building blocks, carbamoylimidazoles, specifically designed for the synthesis of ureas with multiple alkyl groups.

Continue Reading

Fluorine-Substituted Building Blocks

The number of commercial pharmaceutical compounds which contain at least one fluorine substituent noticeably increased since 1950th, when the first fluorine-containing drugs were introduced. At present, about 20% of the commercial drug substances are fluorine-substituted organic compounds. As the prominent examples, top-selling anti-depressant Fluoxetine (Prozac), the cholesterol-lowering drug Atorvastatin (Lipitor), the antibacterial Ciprofloxacin (Ciprobay) could be named.

Continue Reading


Contact us

Send a message