title: HL 752: a potent and long-acting antispasmodic agent.
abstract: 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.
authors.affiliation: Research Centre, Hoechst Marion Roussel Limited, L.B.S. Marg, Mulund, Bombay, India.
authors.forename: S
authors.initials: S
authors.lastname: Bal-Tembe
authors.forename: D N
authors.initials: DN
authors.lastname: Bhedi
authors.forename: A K
authors.initials: AK
authors.lastname: Mishra
authors.forename: R
authors.initials: R
authors.lastname: Rajagopalan
authors.forename: A V
authors.initials: AV
authors.lastname: Ghate
authors.forename: P
authors.initials: P
authors.lastname: Subbarayan
authors.forename: N S
authors.initials: NS
authors.lastname: Punekar
authors.forename: A V
authors.initials: AV
authors.lastname: Kulkarni
mesh_terms: D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001577:Benzophenones / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D004285:Dogs; D004355:Drug Stability; D004952:Esters / Q000378:metabolism / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006868:Hydrolysis; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D010276:Parasympatholytics / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D001565:Benzoates; D001577:Benzophenones; D004952:Esters; D010276:Parasympatholytics; D010880:Piperidines; C108655:HL 752; C015454:pitofenone