Heteroatoms as well as heterocyclic scaffolds are frequently present as the common cores in a plethora of active pharmaceuticals natural products. Statistically, more than 85% of all biologically active compounds are heterocycles or comprise a heterocycle and most frequently, nitrogen heterocycles as a backbone in their complex structures. These facts disclose and emphasize the vital role of heterocycles in modern drug design and drug discovery. In this review, we try to present a comprehensive overview of top prescribed drugs containing nitrogen heterocycles, describing their pharmacological properties, medical applications and their selected synthetic pathways. It is worth mentioning that the reported examples are actually limited to current top selling drugs, being or containing N-heterocycles and their synthetic information has been extracted from both scientific journals and the wider patent literature.

/pdf/prescribed-drugs-containing-nitrogen-heterocycles-an-31vxbjpp0q.pdf

Prescribed drugs containing nitrogen heterocycles: an overview

Transdermal patches are now widely used as cosmetic, topical and transdermal delivery systems. These patches represent a key outcome from the growth in skin science, technology and expertise developed through trial and error, clinical observation and evidence-based studies that date back to the first existing human records. This review begins with the earliest topical therapies and traces topical delivery to the present-day transdermal patches, describing along the way the initial trials, devices and drug delivery systems that underpin current transdermal patches and their actives. This is followed by consideration of the evolution in the various patch designs and their limitations as well as requirements for actives to be used for transdermal delivery. The properties of and issues associated with the use of currently marketed products, such as variability, safety and regulatory aspects, are then described. The review concludes by examining future prospects for transdermal patches and drug delivery systems, such as the combination of active delivery systems with patches, minimally invasive microneedle patches and cutaneous solutions, including metered-dose systems.

https://bpspubs.onlinelibrary.wiley.com/doi/epdf/10.1111/bph.13059

Transdermal patches: history, development and pharmacology

Imidazole and benzimidazole rings are the most important nitrogen-containing heterocycles, which are widely explored and utilized by the pharmaceutical industry for drug discovery. Due to their special structural features and electron-rich environment, imidazole- and benzimidazole-containing drugs bind to a variety of therapeutic targets, thereby exhibiting a broad spectrum of bioactivities. Numerous imidazole- and benzimidazole-based drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potential. Due to their enormous medicinal value, the research and development of imidazole- and benzimidazole-containing drugs is an increasingly active and attractive topic of medicinal chemistry. This review enlightens the landscape of the discovery and development of imidazole- and benzimidazole-based drugs with an emphasis on structure activity relationship features (SAR), medicinal chemistry, and their mechanism of action. Furthermore, the present review also provides the recent advances in the development of imidazole- and benzimidazole-based drugs along with new perspectives. We hope that this paper will open up new opportunities for researchers to design future generation novel and potent imidazole- and benzimidazole-containing drugs.

Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions

Therapeutic system in the form of a skin patch that administers clonidine transdermally in an initial priming dose of 10 to 300 mcg/cm 2 of skin that brings the concentration of clonidine in the blood to a level sufficient to elicit alpha-adrenergic stimulation without intolerable side effects, followed by a substantially constant continuous dosage in the range of 0.1 to 100 mcg/hr that maintains said level. The system is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-clonidine reservoir lamina that is the source of the clonidine for the continuous constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-clonidine contact adhesive layer that is the source of the clonidine for the priming dose and the means by which the system is attached to the skin.

Therapeutic system for administering clonidine transdermally

A Negishi cross-coupling of alkylpyridinium salts and alkylzinc halides has been developed. This is the first example of alkyl–alkyl bond formation via cross-coupling of an alkyl amine derivative w...

/pdf/harnessing-alkylpyridinium-salts-as-electrophiles-in-12hiu93u67.pdf

Harnessing Alkylpyridinium Salts as Electrophiles in Deaminative Alkyl–Alkyl Cross-Couplings

Development of a RIA for clonidine and its comparison with the reference methods.

2-(phenyl-amino)-1, 3-diazacyclopentene-(2) substitution products

The compounds are 1-phenoxy-2-hydroxy-3-alkylamino-propanes and non-toxic acid addition salts thereof, useful as beta -adrenolytics and hypotensives in warm-blooded animals.

1-phenoxy-2-hydroxy-3-sec. alkylamino-propanes

Compounds of the formula ##EQU1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, and R 1 is hydrogen or methyl, And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anticonvulsives and antiarrhythmics in warmblooded animals.

1-(2',6'-Dimethyl-phenoxy)-2-amino-alkanes and salts thereof

Compounds of the formula ##STR1## wherein R 1 and R 2 , which may be identical to or different from each other, are each hydrogen, chlorine, bromine or alkyl of 1 to 3 carbon atoms, R 3 is hydrogen, furfuryl, hydroxyethyl, β-hydroxy-phenethyl, monochlorophenyl-ethyl, dichlorophenyl-ethyl, N-ethyl-piperidyl or --A--NR 6 R 7 , where A is alkylene of 1 to 5 carbon atoms, and R 6 and R 7 are alkyl of 1 to 2 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, morpholino, piperazino or N'-dimethylphenyl-piperazino, R 4 is hydrogen or, together with R 3 and the nitrogen to which they are attached, forms a heterocycle selected from the group consisting of piperidino, morpholino, dimethyl-morpholino or N'-methyl-piperazino, R 5 is hydrogen, alkyl of 1 to 3 carbon atoms, hydroxy-ethyl, diethylamino-ethyl or furfuryl, Provided, however, that R 1 and R 2 are other than both hydrogen or both alkyl at the same time and that R 3 and R 5 are other than both hydrogen at the same time, or a non-toxic, pharmacologically acceptable acid addition salt thereof; the compounds as well as the salt are useful as hypotensives, platelet aggregation inhibitors and antiarrhythmics.

2-Amino-4-phenyl-2-imidazolines and salts thereof

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