Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.

Sunduru N; Gupta L; Chaturvedi V; Dwivedi R; Sinha S; Chauhan PM

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Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.

机译：发现了对结核分枝杆菌H37Rv具有强效活性的新1,3,5-三嗪支架。

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A series of eighty one 2,4,6-trisubstituted-1,3,5-triazines were synthesized and evaluated in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv. Fifteen compounds from this series exhibited good to moderate activity with an MIC in the range 1.56-3.12 microg/mL and most of them were found to be nontoxic against VERO cells and MBMDMQs (mouse bone marrow derived macrophages). This is for the first time that 2,4,6-trisubstituted-1,3,5-triazines were identified as a potent inhibitors of M. tuberculosis H37Rv.

机译：合成了八十一种2,4,6-三取代-1,3,5-三嗪，并在体外评估了结核分枝杆菌H37Rv的生长抑制。该系列中的15种化合物在MIC为1.56-3.12 microg / mL的范围内表现出良好至中等的活性，并且发现其中大多数对VERO细胞和MBMDMQ（小鼠骨髓衍生的巨噬细胞）无毒。这是首次确定2,4,6-三取代-1,3,5-三嗪是结核分枝杆菌H37Rv的有效抑制剂。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第8期|共11页
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Sunduru N; Gupta L; Chaturvedi V; Dwivedi R; Sinha S; Chauhan PM;
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1. Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv. [J] . Sunduru N, Gupta L, Chaturvedi V, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第8期

机译：发现了对结核分枝杆菌H37Rv具有强效活性的新1,3,5-三嗪支架。
2. 1,3,5-triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity [J] . Xuan Yang, Wassihun Wedajo, Yoshiyuki Yamada, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2018,第期

机译：1,3,5-三咔啉[5.5] UNDECA-2,4-DIENES作为选择性分枝杆菌二氢化酸盐酸还原酶抑制剂，具有有效的全细胞活性
3. Novel fluoroquinolones: design, synthesis, and in vivo activity in mice against Mycobacterium tuberculosis H37Rv. [J] . Shindikar AV, Viswanathan CL Bioorganic and Medicinal Chemistry Letters . 2005,第7期

机译：新型氟喹诺酮类药物：小鼠抗结核分枝杆菌H37Rv的设计，合成和体内活性。
4. Synthesis of potassium salts of 2,4-diamino(alkylamino)-6-dinitromethyl-1,3,5-triazine and 2-hydrazinyl-4-amino(alkylamino)-6-dinitromethyl-1,3,5-triazine [C] . Alexander A. Gidaspov, Vladimir V. Bakharev, Olga V. Golovina, Seminar on New Trends in Research of Energetic Materials . 2014

机译：2,4-二氨基（烷基氨基）-6-二硝基甲基-1,3,5-三嗪和2-肼基-4-氨基（烷基氨基）-6-二硝基甲基-1,3,5-三嗪的钾盐的合成
5. Molecular studies and comparative genomic analysis related to the virulence genes of Mycobacterium tuberculosis strain H37Ra versus H37Rv. [D] . Srinivasan, Vittala Gopal. 2010

机译：与结核分枝杆菌菌株H37Ra与H37Rv毒力基因相关的分子研究和比较基因组分析。
6. Immunological activity of a 14-kilodalton recombinant protein of Mycobacterium tuberculosis H37Rv. [O] . A E Kingston, P R Salgame, N A Mitchison, 1987

机译：结核分枝杆菌H37Rv的14千克多尔顿重组蛋白的免疫活性。
7. Potent antibacterial activity of dihydydropyrimidine‐1,3,5‐triazines via inhibition of DNA gyrase and antifungal activity with favourable metabolic profile [O] . Anup Masih, Jitendra Kumar Shrivastava, Hans Raj Bhat, 2020

机译：二氢吡啶胺-1,3,5-三嗪通过抑制DNA乙酶和抗真菌活性的有效抗菌活性，具有良好的代谢曲线
8. Results of an acute algal study and acute oral study with 2-Amino-4-methylamino- 6-ethoxy-1,3,5-triazine, heterocycle-(triazine) with 2-Amino-4-methylamino- 6-ethoxy-1,3,5-triazine, heterocycle-(triazine) (Asterisk 1). [R] . 2011

机译：2-氨基-4-甲氨基-6-乙氧基-1,3,5-三嗪，杂环 - （三嗪）与2-氨基-4-甲氨基-6-乙氧基-1的急性藻类研究和急性口服研究结果，3,5-三嗪，杂环 - （三嗪）（asterisk 1）。

Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.

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