Synthesis, Characterization and Biological Activity of Piperidinothienopyrimidinones

Abstract

Nine new piperidinothienopyrimidinone derivatives were synthesized from the reaction of carbodiimide intermediate with primary, secondary amines and alcohols catalyzed by sodium alkoxide. The structures of the compound were confirmed by elemental analysis, 1 H NMR, MS and single crystal X-ray determination. The fungicidal activities of all the compounds were studied and some compounds exhibited good bacteriostasis activity. Among them, compound 7b exhibited fungicidal activity against Botrytis cinereapers, Rhizoctonia solani, and Gibberella zeae with inhibitive rates of 76.19%, 68.83% and 56.52%, respectively.

Synthesis and Antitumor Activity of Some Novel 5,6,7,8-Tetrahydro- benzo-thieno[2,3-d]pyrimidin-4(3H)-one Derivatives

“…在此基 础上, 我们进一步探讨 aza-Wittig 反应的应用, 以简易 的操作方法, 有效地合成新型的 3-烷基取代的 5,6,7,8-四氢苯并噻吩[2,3-d] 膦亚胺 2 与烷基异氰酸酯反应, 得到的碳二亚胺 3 与仲胺反应, 生成类胍中间体 4, 4 经醇钠催化关环, 即 得到 2-二烷氨基- 5,6,7,8-四氢苯并噻吩并嘧啶酮(5). 3 与 醇及相应醇钠反应, 直接得到 2-烷氧基- 5,6,7,8-四氢苯 并噻吩[2,3-d]并嘧啶酮(6); 3 与酚在无水碳酸钾催化下 反应, 制备了 2-芳氧基- 5,6,7,8-四氢苯并噻吩[2,3-d]并 嘧啶酮 (7). 该方法原料易得、条件温和、收率较高.…”

Absolute Quantification of Follicle Stimulating Hormone (FSH) Using Its Signature Peptides and Enzymatic Digestion in Human Serum by UPLC/LC–MS/MS

“…Quantification of FSH in plasma or serum using mass spectrometry is challenging due to its presence in low abundance and high matrix interferences. There are three main LC-MS-based approaches for absolute quantification of such low abundance protein in bio logical matrices, namely: direct mass spectrometric detec tion of intact proteins, immunocapture using anti-antibody, and identification of representa tive peptides released from target protein by enzymatic digestions [14][15][16][17].…”

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“…[1][2][3][4][5][6][7][8][9] Among all the heterocyclic derivatives, the class of multicycle compounds bearing thienopyrimidine nucleus exhibit a diversity of pharmacological effects such as antibacterial, antifungal, kinase inhibition, immunosuppressive, antidiabetic and anticancer activity .Up to now, there are many different structures containing thienopyrimidine nucleus have been synthesized and evaluated for biological activities. [10][11][12][13][14][15][16][17] Similarly, the Shiff bases have also been reported to possess an array of biological activities namely antimicrobial, ulcerogenic, anti HIV, anticonvulsant, and CNS depressant activities [18][19][20][21] The promising bioactive diversity of these class of heterocyclic compounds and Schiff bases urged us to synthesize and biologically evaluate a series of novel structural variants of thieno [2, 3-d] pyrimidinone derivatives. We have synthesized and utilized 3-amino 2-methyl 4, 5-tetramethylene thieno [2, 3-d] pyrimidin (3H)-4-one as key prototype structural unit, and treated the 3-active amino group with substituted aryl aldehydes to get a new series of Schiff bases.…”