Novel 3-substituted pyridothienopyrimidine derivatives have been synthesized via the reaction of 2-{7,9-dimethyl-4-oxopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-3(4H)-yl}acetohydrazide(5) with a variety of activer...Novel 3-substituted pyridothienopyrimidine derivatives have been synthesized via the reaction of 2-{7,9-dimethyl-4-oxopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-3(4H)-yl}acetohydrazide(5) with a variety of activereagents and chemicals. Structures of the newly synthesized compounds were established based on spectral data.The resulting pyridothienopyrimidine derivatives were evaluated for their possible antimicrobial activity and some ofthem represent a new class of potentially antimicrobial compounds, especially compounds 9 and 18 which displayedthe highest activity against Gram-positive bacteria, Gram-negative bacteria, and Fungi in MIC range of 0.12--1.95 μg/mL.展开更多
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...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.展开更多
文摘Novel 3-substituted pyridothienopyrimidine derivatives have been synthesized via the reaction of 2-{7,9-dimethyl-4-oxopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-3(4H)-yl}acetohydrazide(5) with a variety of activereagents and chemicals. Structures of the newly synthesized compounds were established based on spectral data.The resulting pyridothienopyrimidine derivatives were evaluated for their possible antimicrobial activity and some ofthem represent a new class of potentially antimicrobial compounds, especially compounds 9 and 18 which displayedthe highest activity against Gram-positive bacteria, Gram-negative bacteria, and Fungi in MIC range of 0.12--1.95 μg/mL.
文摘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.