专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
专利号:US-9868747-B2 优先权日:2014-02-18 标题:Marinopyrrole derivatives and methods of making and using same 发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI 权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD 摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
专利号:WO-9740030-A1 优先权日:1996-04-24 标 题:Solid phase and combinatorial synthesis of substituted 2-methylene-2,3-dihydrothiazoles and of arrays of substituted 2-methylene-2,3-dihydrothiazoles
专利号:CN-114854703-B 优先权日:2022-05-23 标 题 :A kind of flavone synthase I/flavanone-3-hydroxylase and its application in the field of synthesis of flavonoids
1: LAGEZE P, PIEDIMONTE L. LE TRAITEMENT DES INFECTIONS BRONCHO-PULMONAIRES R'ECIDIVANTES ET DES BRONCHORRH'EES PURULENTES TRA INANTES PAR LE SULFASOMIZOL [THE TREATMENT OF RECURRENT BRONCHOPULMONARY INFECTIONS AND PROTRACTED PURULENT BRONCHORRHEA WITH SULFASOMIZOLE]. Lyon Med. 1964 Oct 25;212:855-75. French. 64:169-79. French. 93:851-61. French.
合成参考文献
摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956