(Benzoylphenyl)piperidines: a new class of immunomodulators

A series of (benzoylphenyl)piperidines has been synthesized and evaluated for activity as immunomodulators. Several of these compounds show good activity in primary screening on the basis of the lymphocytes mitogenic response to Con A, PHA, and PWM. A chloro group in position 4 of the benzoyl moiety...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1991-05, Vol.34 (5), p.1545-1552
Main Authors: Bellamy, Francois D, Chazan, Jean B, Dodey, Pierre, Dutartre, Patrick, Ou, Khan, Pascal, Marc, Robin, Jacques
Format: Article
Language:English
Subjects:
Adjuvants, Immunologic - chemical synthesis
Adjuvants, Immunologic - pharmacology
Animals
Cell Division - drug effects
Chemical Phenomena
Chemistry
Exact sciences and technology
Lymphocyte Activation - drug effects
Mice
Mice, Inbred DBA
Mice, Nude
Mitogens - antagonists & inhibitors
Noncondensed benzenic compounds
Organic chemistry
Piperidines - chemical synthesis
Piperidines - pharmacology
Preparations and properties
Structure-Activity Relationship
T-Lymphocytes - drug effects
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Summary:A series of (benzoylphenyl)piperidines has been synthesized and evaluated for activity as immunomodulators. Several of these compounds show good activity in primary screening on the basis of the lymphocytes mitogenic response to Con A, PHA, and PWM. A chloro group in position 4 of the benzoyl moiety as well as an amino group (or a carbamate derivative) para to the piperidine nucleus seems to be essential for activity. The depicted compounds may be considered as the first examples of a new series of immunomodulators.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00109a004