CAS: 56518-41-3; 5-(4-Bromo-3,5-Dimethoxybenzyl)Pyrimidine-2,4-Diamine

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CAS号96103-67-2 2-bromo-5-[(2,4...

📜4-溴-3,5-二甲氧基苯甲醛置于potassium Tert-Butylate体系中,用 乙醇,二甲基亚砜 作为反应溶剂,化学反应 17.5H,反应生成 溴莫普林
参考文献:抗菌活性的光控:从紫外线到红光激活的转变
标题:抗菌活性的光控:从紫外线到红光激活的转变
摘要:光药理学领域旨在引入智能药物,通过结合分子光开关,允许光对生物活性进行远程空间和时间控制.通过减少抗生素的全身和环境副作用,这一概念在治疗细菌感染方面可能特别有益.实现这种光响应药物的一个主要问题是所施加的光的波长.对生物活性剂光控制的研究主要依赖于紫外线,紫外线具有细胞毒性,不适合组织穿透.在我们努力开发光控抗生素的过程中,我们在这里引入了抗菌剂,其活性可以通过可见光控制,同时进入治疗窗口.为了这个目的,确定了基于具有合适抗菌性能的二氨基嘧啶的紫外线响应核心结构.随后对偶氮苯光开关部分的修饰导致了结构,使我们能够利用可见光区域的光在两个方向上控制它们对大肠杆菌的活性.绿光和紫光首次在细菌存在下实现了对抗菌活性的完全原位光控制.最值得注意的是,其中一种二氨基嘧啶在用 652 Nm 红光照射之前和之后显示出至少 8 倍的活性差异,这表明在研究的浓度范围内没有活性的生物制剂的有效"激活",并且这样做治疗窗内的红灯.
DOI:10.1021/jacs.7B09281

专利信息

专利号:US-9149445-B2
优先权日:2009-07-27
标 题:Inhibition of glycerol-3-phosphate acyltransferase (GPAT) and associated enzymes for treatment of viral infections
发明人：LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS
权利人:LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS; UNIV PRINCETON
摘要:A method of treating or preventing a viral infection in a mammal by administering a compound or pharmaceutically acceptable derivative thereof that inhibits a phosphatidic acid synthesis enzyme.

专利号:US-9295731-B2
优先权日:2013-04-01
标题 :Cleavable drug conjugates, compositions thereof and methods of use
发明人：NGUYEN MARK QUANG
权利人:NGUYEN MARK QUANG
摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.

专利号:US-5084458-A
优先权日:1987-05-14
标 题 :Substituted 2-acylpyridine-β-(N)-hetaryl-hydrazones and medicaments containing the same
发明人：SCHAPER KLAUS-JUERGEN; SEYDEL JOACHIM K
权利人:SCHAPER KLAUS JUERGEN; SEYDEL JOACHIM K
摘要:PCT No. PCT/DE88/00289 Sec. 371 Date Mar. 7, 1989 Sec. 102(e) Date Mar. 7, 1989 PCT Filed May 14, 1988 PCT Pub. No. WO88/08842 PCT Pub. Date Nov. 17, 1988.Substituted 2-acylpyridine- alpha -(N)-hetarylhydrazones are described, which are suitable as active substances for the treatment of antimicrobial and in particular antimycobacterial diseases, as well as active substances for the treatment of malaria or malignant tumours. The compounds have a marked synergistic activity combined with inhibitors of folate synthase, dihydrofolic acid reductase, DNA-synthesis and RNA-synthesis.

专利号:US-2023398101-A1
优先权日:2022-06-09
标题 :Co-agents as Therapy Against Anaerobic Pathogens
发明人：PACE JOHN LEE; HARTSELL THERESA LYNN
权利人:FLEURIR ABX LLC
摘要:Co-agent combinations and/or formulations herein unexpectedly display significantly better antimicrobial activity (e.g., more efficacy and/or more potency) against anaerobic pathogens not previously considered targets. With three or more co-agents, selected from a group of a fosfomycin, a diaminopyridine, a sulfonamide, a beta lactam antibacterial, a bacterial beta-lactamase inhibitor, a bacterial fosfomycin-modifying enzyme, and a bacterial peptidoglycan synthesis inhibitor, the therapeutic potential of the three or more co-agents is expanded by targeting a broader spectrum of pathogens. Co-agents, by unexpected synergistic action in an anaerobic environment, are now active and efficacious against difficult to treat pathogenic anaerobes (including anaerobes that cannot utilize oxygen and/or reside in an anaerobic environment, some being inhibited by oxygen), as well as pathogens considered resistant or intolerant to at least one of the co-agents when used singly in an anaerobic environment. Some co-agent combinations and/or formulations contain one or more existing antibiotic agents being repurposed for utility against difficult to treat anaerobic pathogens.

专利号:CN-103193651-A
优先权日:2013-04-12
标题 :Synthesis and industrial production process of a pharmaceutical intermediate 3,5-dihydroxybenzoic acid methyl ester