Syntheses and diuretic activity of 1,2-dihydro-2-(3-pyridyl)-3H-pyrido[2,3-d]pyrimidin-4-one and related compounds

Abstract

The title compound, 5, was prepared and found to be a potent diuretic in the rat. At 27 mg/kg, urine output was 250% of the saline control, and the excretion of electrolytes was similar to th^hydrochlorothiazide control. At 80 mg/kg, the potassium excretion was the same as the saline control, and the sodium and chloride excretions more than doubled. Several analogues were prepared and tested. Some show diuretic activity.

Design and synthesis of a new steroid-macrocyclic derivative with biological activity

“…There are several reports on the preparation of pyrimidinethiones and pyrimidine-ones derivatives using several reagents such as 3-isothiocyanato-propene [19], oxalyl chloride [20], cyanothioacetamide [21], formaldehyde [22], furoyl chloride [23], and diazotized anilines [24]; however, some of these reagents require condition specials. In this study, the first stage involved the preparation of a pyrimidine-thione using the three-component system (α-naphthol, benzaldehyde, and thiourea) in mild conditions (Fig.…”

Synthesis of Some New Pyridines, Thienopyridines and Pyrido[2,3:4′,5′]thieno[3′,2′‐d]pyrimidin‐8‐ones from 2‐Acetylbenzoimidazole.

“…13,14 Nucleophilic amines 12a,b can attack the carbonyl carbon atom C1 or C3 of the ketones 2. Actually, only the first attack takes places and the corresponding 14a-e or 17a,b were isolated.…”

Molecular Iodine Promoted Synthesis of New Pyrido[2,3‐d]pyrimidin‐4‐ols

“…Pyrido [2,3-d]pyrimidine ring system is present in a number of biologically active compounds which includes antitumor, 1 antipyretic, 2 analgesic, 3 antihistaminic, 4 PDE4 inhibitor, 5 adenosine kinase inhibitor, 6 tyrosine kinase inhibitor 7 and diuretic 8,9 activities. Although there are a number of well-established methods to prepare pyrido [2,3-d]pyrimidine ring system, they mainly depend on the availability of the indispensable metal-catalyzed C-H functionalization and subsequent formation of C-N bonds.…”