Synthesis and Structure-Activity Relationships of Novel Neocryptolepine Derivatives

Herein we reported the synthesis of a novel series of neocryptolepine（5-methyl-5H-indolo[2,3-b]quinoline） derivatives containing different substituents at Cll using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their axltibacteria...

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Published inChemical research in Chinese universities Vol. 33; no. 3; pp. 373 - 377
Main Authors El-Gokha, Ahmed A., Boshta, Nader M., Abo Hussein, Mona K., El Sayed, Ibrahim El-T.
Format Journal Article
LanguageEnglish
Published Changchun Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01.06.2017
Springer Nature B.V
Subjects
Analytical Chemistry
Bacteria
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Derivatives
E coli
Gram-positive bacteria
In vitro methods and tests
Inorganic Chemistry
N-甲基苯胺
Organic Chemistry
Physical Chemistry
Quinoline
Synthesis
合成
构效关系
枯草芽孢杆菌
衍生物
金黄色葡萄球菌
革兰氏阳性细菌
革兰氏阴性菌
Indoloquinoline
Neocryptolepine
Antibacterial
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Summary:Herein we reported the synthesis of a novel series of neocryptolepine（5-methyl-5H-indolo[2,3-b]quinoline） derivatives containing different substituents at Cll using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their axltibacterial activity in vitro against gram-positive bacteria（B, subtilis and S. aureus） and gram-negative bacteria（E, coli and S.typhi）. Almost all the tested compounds showed moderate to high activities against the four bacterial strains at the minimum inhibitory concentrations（MICs） of 1-10μg/mL. The obtained results suggest that part of the novel synthetic neocryptolepine derivatives exhibit significant antibacterial effect against all the tested organisms.
Bibliography:22-1183/O6
Herein we reported the synthesis of a novel series of neocryptolepine（5-methyl-5H-indolo[2,3-b]quinoline） derivatives containing different substituents at Cll using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their axltibacterial activity in vitro against gram-positive bacteria（B, subtilis and S. aureus） and gram-negative bacteria（E, coli and S.typhi）. Almost all the tested compounds showed moderate to high activities against the four bacterial strains at the minimum inhibitory concentrations（MICs） of 1-10μg/mL. The obtained results suggest that part of the novel synthetic neocryptolepine derivatives exhibit significant antibacterial effect against all the tested organisms.
Neocryptolepine; Indoloquinolme; Antibacterial
ISSN:1005-9040
2210-3171
DOI:10.1007/s40242-017-6502-6