Condensed thienopyrimidines. II. Synthesis and gastric antisecretory activity of thiazole and polymethylene condensed thienopyrimidine derivatives.

Abstract

Thiazolo[3,2-a]thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (6, 11 and 16), and polymethylene condensed thieno[3,2-d]-, [3,4-d]- and [2,3-d]pyrimidin-5-one derivatives (19-21), in which the oxygen atom of the oxazolidine moiety in 3 was replaced by a sulfur atom or methylene groups, were synthesized and evaluated for gastric antisecretory activity in pylorus-ligated rats. The structure-activity relationships of these compounds are discussed.

New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines

“…Heterocycles bearing a symmetrical pyrimidoquinoline moiety are reported to show a broad spectrum of pharmacological and medicinal [1,2] properties such as anti-microbial [3][4][5][6][7], antifungal [8], anticancer [9], antiviral [10], analgesic [11], antiinflammatory activities [12]. Also, acyclic nucleosides of the HEPT type 1-[(2-hydroxyethoxy)-methyl]-6-(phenylthio)thymine have shown high selectivity towards HIV-1 [13].…”

Synthesis of Polynuclear Heterocyclic Compounds Derived from Thieno[2,3-d]pyrimidine Derivatives

“…The solid so-precipitated was filtered off and crystallized from benzene. [3,2-e] [1,2,3,4]tetrazolo [1,5- General procedure for the preparation of 4`a,b…”

“…The biological [1][2][3][4][5], bactericidal [6], and medicinal [7,8] activities of thieno [2,3-d]-pyrimidine derivatives have stimulated considerable research in this field [9][10][11][12]. In continuation of our work on the synthesis of fused pyrimidine derivatives [13], we report here the utility of 3-methyl-2-methylthio-3,4-dihydrotheino [2,3-d]pyrimidine-4-one derivatives 1a,b for the synthesis of azolothienopyrimid-ines, thienopyrimido-as-triazines, pyrazolylthienopyrimidines and tetrazolothienopyrimidines.…”

Thieno[2,3‐d]pyrimidines in the Synthesis of Antitumor and Antioxidant Agents

“…Moreover, condensed heterocycles containing thienopyrimidines have acquired conspicuous popularity in recent years due to their wide spectrum of biological activities including analgesic [2][3][4][5][6], anti-inflammatory [3][4][5][6][7][8], antipyretic [4], antihypertensive [9,10], pesticidal [11], herbicidal [12,13], plant growth regulatory [13], spasmolytic [14], gastric antisecretory [15], antihistaminic [16], antibacterial [17][18][19][20], antifungal [21,22], antimalarial [23], anti-HIV-1 and antiHerpes simplex virus HSV-1 [24], antitumor [25,26], as selective 5-HT 3 receptor ligands [27], hypnotics [28], and many more. Indeed, several series of heterocyclic compounds possessing a bridgehead thiazole or thiazine moiety play a vital role in many biological activities: thiazole derivatives such as pyrimidobenzothiazole and benzothiazoloquinoline derivatives, imidazobenzothiazoles as well as polymerized benzothiazoles showed remarkable antitumor activity [29].…”