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Special Issue "Active Pharmaceutical Ingredients"


A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 January 2013)

Special Issue Editor

Guest Editor
Prof. Dr. Cody P. Coyne (Website)

Department of Basic Sciences, College of Veterinary Medicine at Wise Center, Mississippi State University, State, MS 39762-6100, USA
Phone: +662 325 1120
Interests: pharmaceutical molecular design; selectively “targeted” pharmaceutical delivery; organic chemistry synthesis schemes; alternative pharmaceutical efficacies; additive and synergistic pharmaceutical combinations; diagnostic pharmaceuticals.

Special Issue Information

Dear Colleagues,

In the field of pharmacology, the spectrum of different molecular platforms that possess biological activity that impart therapeutic and diagnostic properties has markedly expanded since the early development of sulfonamide dyes as anti-bacterial agents. Besides classical small molecular weight pharmaceuticals the range of clinically relevant therapeutics now includes hormone analogs (agonists and antagonists), monoclonal immunoglobulin (e.g. anti-HER2/neu, anti-EGFR), receptor ligands, biologically active peptides (e.g. IL-2), conjugated preparations, photodynamic agents (e.g. 5-aminolevulinic acid), gene therapies (e.g. anti-sense mRNA), diagnostic dyes (e.g. methylene blue), and diagnostic imaging agents (18F-glucose), diagnostic function/response (e.g. dexamethazone, albuterol), and herbal preparations (e.g. arnica, aloe vera, ginsing). A quality that almost invariably all molecular based modalities share in common is at least one chemically active site that is responsible for their mechanism-of-action and a biological effect that is therapeutically relevant. Rarely small molecular weight pharmaceuticals like digitoxin exert multiple mechanisms-of-action which is a property that is often more frequently be seen with large molecular weight therapeutics which contain multiple different moieties where each one has a unique chemically active or biologically active site capable of evoking their own individual mechanism-of-action and biological effect (e.g. Glembatumumab vedotin, epirubicin-[anti-HER2/neu]). This special issue of Molecules welcomes previously unpublished manuscripts covering aspects about therapeutic agents pertaining to the first-time discovery or characterization of chemically active sites related to their mechanism-of-action, biological activity, physiological effect or therapeutic properties.

Prof. Dr. Cody P. Coyne
Guest Editor

Related Special Issues in Other Journals


Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are refereed through a peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed Open Access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs).


  • mechanism-of-action
  • chemically active site or moiety
  • biologically active site or moiety

Related Special Issue

Published Papers (1 paper)

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Open AccessArticle In Vitro and in Vivo Metabolism of Verproside in Rats
Molecules 2012, 17(10), 11990-12002; doi:10.3390/molecules171011990
Received: 3 September 2012 / Revised: 28 September 2012 / Accepted: 8 October 2012 / Published: 12 October 2012
Cited by 4 | PDF Full-text (634 KB) | HTML Full-text | XML Full-text
Verproside, a catalpol derivative iridoid glycoside isolated from Pseudolysimachion rotundum var. subintegrum, is a biologically active compound with anti-inflammatory, antinociceptic, antioxidant, and anti-asthmatic properties. Twenty-one metabolites were identified in bile and urine samples obtained after intravenous administration of verproside in rats using liquid chromatography-quadrupole Orbitrap mass spectrometry. Verproside was metabolized by O-methylation, glucuronidation, sulfation, and hydrolysis to verproside glucuronides (M1 and M2), verproside sulfates (M3 and M4), picroside II (M5), M5 glucuronide (M7), M5 sulfate (M9), isovanilloylcatalpol (M6), M6 glucuronide (M8), M6 sulfate (M10), 3,4-dihydroxybenzoic acid (M11), M11 glucuronide (M12), M11 sulfates (M13 and M14), 3-methyoxy-4-hydroxybenzoic acid (M15), M15 glucuronides (M17 and M18), M15 sulfate (M20), 3-hydroxy-4-methoxybenzoic acid (M16), M16 glucuronide (M19), and M16 sulfate (M21). Incubation of verproside with rat hepatocytes resulted in thirteen metabolites (M1–M11, M13, and M14). Verproside sulfate, M4 was a major metabolite in rat hepatocytes. After intravenous administration of verproside, the drug was recovered in bile (0.77% of dose) and urine (4.48% of dose), and O-methylation of verproside to picroside II (M5) and isovanilloylcatalpol (M6) followed by glucuronidation and sulfation was identified as major metabolic pathways compared to glucuronidation and sulfation of verproside in rats. Full article
(This article belongs to the Special Issue Active Pharmaceutical Ingredients)

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