BIOMAT Database Logo BIOMAT Database Logo

Synthesis and pharmacological activity of 2-alkylthio substituted thieno[2,3-d]pyrimidine-4-one and 5H-pyrimido [5,4-b]indol-4-one. 1990

F Russo, and N A Santagati, and R Venturini, and S Spampinato
Istituto di Chimica Farmaceutica e Tossicologica dell'Università di Catania, Italy.

Quaternary salts of several 2-alkylthio substituted derivatives of thieno [2,3-d]pyrimidin-4-one and 5H-pyrimido [5,4-b]indol-4-one with a basic group in position 2 of the alkyl chain were synthesized and screened for potential spasmolytic activity. These substances were prepared by condensation of the corresponding mercapto compounds with a 2-chloroalkyltertiary amine. The tertiary bases were quaternized with methyl iodide. Among the assayed compounds, the thieno [2-3-d]pyrimidin-4-one derivatives displayed a potent spasmolytic activity in the in vitro and in vivo assays.

UI MeSH Term Description Entries
D007082 Ileum The distal and narrowest portion of the SMALL INTESTINE, between the JEJUNUM and the ILEOCECAL VALVE of the LARGE INTESTINE.
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008297 Male Males
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009130 Muscle, Smooth Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed) Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D010276 Parasympatholytics Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS. Antispasmodic,Antispasmodic Agent,Antispasmodic Drug,Antispasmodics,Parasympathetic-Blocking Agent,Parasympathetic-Blocking Agents,Parasympatholytic,Parasympatholytic Agent,Parasympatholytic Drug,Spasmolytic,Spasmolytics,Antispasmodic Agents,Antispasmodic Drugs,Antispasmodic Effect,Antispasmodic Effects,Parasympatholytic Agents,Parasympatholytic Drugs,Parasympatholytic Effect,Parasympatholytic Effects,Agent, Antispasmodic,Agent, Parasympathetic-Blocking,Agent, Parasympatholytic,Agents, Antispasmodic,Agents, Parasympathetic-Blocking,Agents, Parasympatholytic,Drug, Antispasmodic,Drug, Parasympatholytic,Drugs, Antispasmodic,Drugs, Parasympatholytic,Effect, Antispasmodic,Effect, Parasympatholytic,Effects, Antispasmodic,Effects, Parasympatholytic,Parasympathetic Blocking Agent,Parasympathetic Blocking Agents
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D011744 Pyrimidinones Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O. Pyrimidinone,Pyrimidone,Pyrimidones
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus

Related Publications

F Russo, and N A Santagati, and R Venturini, and S Spampinato
Synthesis and pharmacological evaluation of thieno[2,3-d]pyrimidin-2,4-dione and 5H-pyrimido [5,4-b]indol-2,4-dione derivatives.
October 1995, Farmaco (Societa chimica italiana : 1989),
F Russo, and N A Santagati, and R Venturini, and S Spampinato
Targeted Synthesis and Study of Anti-tyrosinase Activity of 2-Substituted Tetrahydrobenzo[4,5]Thieno[2,3-d]Pyrimidine-4(3H)-One.
December 2022, Iranian journal of pharmaceutical research : IJPR,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
Synthesis and pharmacological study of antihyperlipaemic activity of 2-substituted thieno(2,3-d)pyrimidin-4(3H)-ones.
May 1990, Arzneimittel-Forschung,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
Synthesis and activity of phenyl derivatives containing 5,6-dimethylthieno[2,3-d]pyrimidin-4(1H)-one or 4H-pyrimido[5,4-b]indol-4-one heterocyclic system as potential nonsteroidal anti-inflammatory drugs.
January 2002, Arzneimittel-Forschung,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
Synthesis and Antimicrobial Evaluation of Thieno[2,3-d]-pyrimidine, Thieno[2',3':4,5]pyrimido[1,2-a][1,3,5]triazine, Thieno[2,3-d]-1,3-thiazine and 1,2,4-Triazole Systems.
January 2015, Chemical & pharmaceutical bulletin,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
[Studies on the synthesis of sulfur containing pyrimido [5,4-d]pyrimidine derivatives. II. Syntheses and rearrangement of 2-methylsulfonyl pyrimido[5,4-d]pyrimidine-6-sulfonamide derivatives].
May 1976, Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
Synthesis of novel thieno[2,3-d]pyrimidine, thieno[2,3-b]pyridine and thiazolo[3,2-a]thieno[2,3-d]pyrimidine derivatives and their effect on the production of mycotoxins.
May 1992, Archiv der Pharmazie,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
2-benzazepines. 6. Synthesis and pharmacological properties of the metabolites of 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d] [2]benzazepine.
November 1983, Journal of medicinal chemistry,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
[Pharmacological properties of a new coronary dilator substance 2, 6-bis(diethanolamino)-4, 8-dipiperidino-pyrimido[5,4-d]pyrimidine].
January 1959, Arzneimittel-Forschung,
F Russo, and N A Santagati, and R Venturini, and S Spampinato
[Synthesis and antihypertensive activity of 2-methyl-5H,6H-[1,3]thiazino[2,3-b]quinazolin-4-one].
April 1983, Archiv der Pharmazie,
Copied contents to your clipboard!