1.
J Med Chem
; 18(5): 447-53, 1975 May.
Article
in English
| MEDLINE
| ID: mdl-239232
ABSTRACT
On treatment of N-substituted isatoic anhydrides with 2-methylmercaptoimidazolines, 10-substituted imidazo[2,1-b]quinazolin-5(10H)-ones are obtained. Several members of this class exhibited pronounced broncholytic activity. The structure-activity relationships (based on results obtained in the guinea pig histamine aerosol test) of these nonsympathomimetic bronchodilators are discussed. In addition, the detailed pharmacological evaluation of two analogs found to be five to ten times more active than theophyline as bronchodilators without having central nervous system or cardiovascular side effects is described.
Subject(s)
Bronchodilator Agents/chemical synthesis , Quinazolines/chemical synthesis , Animals , Bronchodilator Agents/pharmacology , Dogs , Female , Guinea Pigs , Hemodynamics/drug effects , Histamine/pharmacology , Histamine H1 Antagonists/pharmacology , Imidazoles/chemical synthesis , Imidazoles/pharmacology , In Vitro Techniques , Isoproterenol/pharmacology , Lethal Dose 50 , Male , Mice , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Ovalbumin , Passive Cutaneous Anaphylaxis/drug effects , Quinazolines/pharmacology , Structure-Activity Relationship , Theophylline/pharmacology , Trachea/drug effects
2.
J Med Chem
; 17(6): 636-9, 1974 Jun.
Article
in English
| MEDLINE
| ID: mdl-4829943
Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Pyrimidinones/chemical synthesis , Animals , Anti-Inflammatory Agents/therapeutic use , Arthritis, Rheumatoid/drug therapy , Arthritis, Rheumatoid/immunology , Carrageenan , Edema/chemically induced , Edema/drug therapy , Freund's Adjuvant , Pyridines/chemical synthesis , Pyridines/therapeutic use , Pyrimidinones/therapeutic use , Rats , Structure-Activity Relationship
3.
J Med Chem
; 16(11): 1237-45, 1973 Nov.
Article
in English
| MEDLINE
| ID: mdl-4747965