Synthesis and bronchodilatory activity of four new derivatives of deoxyvasicine.
As part of a continuing effort aimed at the development of efficacious antihistaminic and bronchodilator agents for the treatment of asthma and related respiratory diseases, a series of novel trisubstituted deoxyvasicine derivatives was designed and synthesized. Bronchodilatory activity of pure samples of ligands 17a-d, and DL-8-chlorovasicine hydrochloride is investigated and compared with isoprenaline and aminophylline. These studies confirm the activity of ligands 17a-d and the potentiating effect of 17c on aminophylline.
Ojo
B
B
Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0540, USA.
Findsen
L A
LA
Igarashi
N
N
Kong
B
B
Chowdhury
B K
BK
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000628:Aminophylline / Q000494:pharmacology; D000818:Animals; D001986:Bronchial Spasm / Q000517:prevention & control*; D001993:Bronchodilator Agents / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D011799:Quinazolines; D013329:Structure-Activity Relationship; D014132:Trachea / Q000187:drug effects
D000470:Alkaloids; D001993:Bronchodilator Agents; D011799:Quinazolines; D000628:Aminophylline; C048835:3-deoxyvasicine; D007545:Isoproterenol