HL 752: A potent and long-acting antispasmodic agent

HL 752: A potent and long-acting antispasmodic agent

Ester analogues of methyl-2-(4-(2-piperidinoethoxy)benzoyl)-benzoate hydrochloride (pitofenone) ( 2) were prepared with an aim to find a more potent and metabolically stable antispasmodic compound. The compounds were evaluated for their in vitro and in vivo antispasmodic activity, and stability to i...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry Vol. 5; no. 7; pp. 1381 - 1387
Main Authors: Bal-Tembe, Swati, Bhedi, Dilip N., Mishra, Anil K., Rajagopalan, Ramanujam, Ghate, Anil V., Subbarayan, Palakodety, Punekar, Narayan S., Kulkarni, Anjali V.
Format: Journal Article
Language:English
Published: England Elsevier Ltd 01-07-1997
Subjects:
Animals
Benzoates - chemical synthesis
Benzoates - metabolism
Benzoates - pharmacology
Benzophenones - chemical synthesis
Benzophenones - metabolism
Benzophenones - pharmacology
Dogs
Drug Stability
Esters - metabolism
Esters - pharmacology
Female
Guinea Pigs
Hydrolysis
Ileum - drug effects
In Vitro Techniques
Male
Parasympatholytics - chemical synthesis
Parasympatholytics - metabolism
Parasympatholytics - pharmacology
Piperidines - chemical synthesis
Piperidines - metabolism
Piperidines - pharmacology
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Summary:Ester analogues of methyl-2-(4-(2-piperidinoethoxy)benzoyl)-benzoate hydrochloride (pitofenone) ( 2) were prepared with an aim to find a more potent and metabolically stable antispasmodic compound. The compounds were evaluated for their in vitro and in vivo antispasmodic activity, and stability to in vitro enzymatic hydrolysis. Of the compounds synthesised, HL 752 ( 21) showed the most potent and long-lasting antispasmodic activity and was selected as the candidate for clinical development. From a series of ester analogues, the most potent and long-acting antispasmodic compound, HL 752 (R = isopropyl), was chosen for development.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(97)00067-9