Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo(1,2-a)pyridines.

Sundberg RJ; Biswas S; Kumar-Murthi K; Rowe D; McCall JW; Dzimianski MT

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Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo(1,2-a)pyridines.

机译：作为大型杀线虫剂的双阳离子杂芳族化合物：取代的咪唑并（1,2-a）吡啶的双am和双胍hydr衍生物的合成。

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A series of guanylhydrazone, amidine, and hydrazone derivatives of 2-phenylimidazo[1,2-a]pyridine have been prepared and evaluated for macrofilarial activity against Acanthocheilonema viteae and Brugia pahangi in jirds. Compounds with 4',6-bis-substitution by cyclic guanylhydrazone groups show activity. 4',6-Bis-amidines show some activity but are more toxic; 4'- or 6-monosubstituted compounds are inactive. 2,6-Bis-substituted compounds lacking the phenyl ring are inactive. 4',6-Bis-substituted compounds having additional double bonds inserted between the heterocyclic ring and the phenyl ring or between the substituent and the ring system show reduced activity.

机译：已经制备了一系列2-苯基咪唑并[1,2-a]吡啶的胍hydr，am和衍生物，并评估了其对蚕can中棘阿米奇虫和凤梨的大丝活性。被环状胍基团具有4'，6-双取代的化合物显示出活性。 4'，6-双-具有一定的活性，但毒性更大。 4'-或6-单取代的化合物是无活性的。缺少苯环的2,6-双取代化合物是无活性的。具有在杂环和苯环之间或在取代基和环系统之间插入的附加双键的4'，6-双取代的化合物显示出降低的活性。

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来源
《Journal of Medicinal Chemistry》 |1998年第22期|共12页
作者
Sundberg RJ; Biswas S; Kumar-Murthi K; Rowe D; McCall JW; Dzimianski MT;
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正文语种 eng
中图分类药学;
关键词
Amidines; Filaricides; Hydrazones; Pyridines; 脒类; 抗丝虫药; 腙类; 吡啶类;

机译：Amidines;Filaricides;Hydrazones;Pyridines;脒类;抗丝虫药;腙类;吡啶类;

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1. Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo(1,2-a)pyridines. [J] . Sundberg RJ, Biswas S, Kumar-Murthi K, Journal of Medicinal Chemistry . 1998,第22期

机译：作为大型杀线虫剂的双阳离子杂芳族化合物：取代的咪唑并（1,2-a）吡啶的双am和双胍hydr衍生物的合成。
2. 1H-Imidazo(4,5-c)quinoline derivatives as novel potent TNF-alpha suppressors: synthesis and structure-activity relationship of 1-, 2-and 4-substituted 1H-imidazo(4,5-c)quinolines or 1H-imidazo(4,5-c)pyridines. [J] . Izumi T, Sakaguchi J, Takeshita M, Bioorganic and medicinal chemistry . 2003,第12期

机译：1H-咪唑（4,5-c）喹啉衍生物作为新型有效的TNF-α抑制剂：1、2-和4-取代的1H-咪唑并（4,5-c）喹啉或1H-的合成与构效关系咪唑并（4,5-c）吡啶。
3. Efficient one-pot synthesis of functionalised imidazo[1,2-a]pyridines and unexpected synthesis of novel tetracyclic derivatives by nucleophilic aromatic substitution [J] . Changunda Charles R. K., Venkatesh B. C., Mokone William K., RSC Advances . 2020,第14期

机译：通过亲核芳族取代的高效单钾合成官能化咪唑[1,2-A]吡啶和意外合成新型四环衍生物
4. Methyl(11aS)-1,2,3,5,11,11a-Hexahydro-3,3-dimethyl-1-oxo-6H-imidazo-3',4':1,2pyridin3,4-b-indol-2-Substituted Acetates: Synthesis and Three-Dimensional Quantitative Structure-Activity Relationship Investigation as a Class of Novel Vasodilator [C] . Jiawang Liu, Ming Zhao, Guohui Cui, 第四届国际分子模拟与信息技术应用学术会议（The 4th International Conference of Molecular Simulations and Applied Informatics Technologies）论文集 . 2008

机译：甲基（11aS）-1,2,3,5,11,11a-六氢-3,3-二甲基-1-氧代-6H-咪唑-3'，4'：1,2吡啶3,4- b-吲哚-2-取代的乙酸酯：一类新型血管扩张剂的合成与三维定量构效关系研究
5. I. SYNTHETIC APPROACHES TO SUBSTITUTED 2-OXABICYCLO(3.2.1)OCTANE DERIVATIVES AND II. THE SYNTHESIS OF 1-SUBSTITUTED DERIVATIVES OF ANHYDRO (3-CHLOROACETYL-2-HYDROXYIMIDAZO(1,2-A)PYRIDINIUM HYDROXIDE). [D] . FRIEDMAN, ALAN E. 1973

机译：I.取代2-氧杂双环（3.2.1）正己烷衍生物的合成方法和II。合成1-取代的酸酐（3-氯乙酰基-2-羟基咪唑并（1,2-A）吡啶鎓氢氧化物）。
6. Tertiary Alkylamines as Nucleophiles in Substitution Reactions at Heteroaromatic Halide During the Synthesis of the Highly Potent Pirinixic Acid Derivative 2-(4-Chloro-6-(23-dimethylphenylamino)pyrimidin-2-ylthio)octanoic Acid (YS-121) [O] . Matthias Gabler, Manfred Schubert-Zsilavecz 2011

机译：叔烷基胺作为亲核试剂在高强的吡喃酸衍生物2-（4-氯-6-（23-二甲基苯基氨基）嘧啶-2-基硫基）辛酸（YS-121）合成过程中在杂芳族卤化物上的取代反应中的亲核体
7. Imidazo(1,2-a)pyridines. I. Synthesis and Inotropic Activity of New 5-Imidazo(1,2-a)pyridinyl-2(1H)-pyridinone Derivatives. [O] . Motosuke YAMANAKA, Kazutoshi MIYAKE, Shinji SUDA, 1991

机译：咪唑（1,2-A）吡啶。 I.新的5-咪唑（1,2-A）吡啶基-2（1H） - 吡啶酮衍生物的合成和渗透活性。

Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo(1,2-a)pyridines.

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