Bioorganic & medicinal chemistry, 2008-06, Vol.16 (11), p.5974-5981
2008
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Details
- Autor(en) / Beteiligte
- Titel
- Benzanilides with spasmolytic activity: Chemistry, pharmacology, and SAR
- Ist Teil von
- Bioorganic & medicinal chemistry, 2008-06, Vol.16 (11), p.5974-5981
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2008
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- . The following study describes the synthesis of new benzanilide derivatives and their pharmacological investigation on smooth muscle preparations of guinea pigs. All compounds were synthesized in good yields and showed a spasmolytic activity without significant effect on vascular smooth muscles and heart muscle preparations. Moreover, further pharmacological investigations as well as in silico studies were performed to elucidate the mechanism of action. Compound 3 showed the most potent spasmolytic activity with an IC 50 of 3.25 μM.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0968-0896eISSN: 1464-3391DOI: 10.1016/j.bmc.2008.04.057Titel-ID: cdi_proquest_miscellaneous_19502904
- Format
- –
- Schlagworte
- Anilides - chemical synthesis, Anilides - pharmacology, Animals, Benzanilide, Biological and medical sciences, Digestive system, Dose-Response Relationship, Drug, Female, Guinea Pigs, Heart Atria - drug effects, Ileum - drug effects, Ileum - physiology, Inhibitory Concentration 50, Male, Medical sciences, Muscle Contraction - drug effects, Muscle Contraction - physiology, Papillary Muscles - drug effects, Papillary Muscles - physiology, Pharmacology. Drug treatments, SAR, Smooth muscle preparations, Spasmolytic activity, Stilbenes - chemistry, Stilbenes - pharmacology, Structure-Activity Relationship