共查询到20条相似文献,搜索用时 8 毫秒
1.
Libo Xu Amy K. Farthing James F. Dropinski Peter T. Meinke Christine McCallum Emily Hickey Kun Liu 《Bioorganic & medicinal chemistry letters》2013,23(1):366-369
Semi-synthetic water-soluble analogs were synthesized from nocathiacin I through the formation of a versatile intermediate nocathiacin amine 5, and subsequent transformation via reductive amination, acylation or urea formation. Several of the novel analogs displayed much improved aqueous solubility over 1, while retained antibacterial activity. Compound 15 and 16 from the amide series, demonstrated excellent in vitro and in vivo antibacterial activity. 相似文献
2.
Zhang J Redman N Litke AP Zeng J Zhan J Chan KY Chang CW 《Bioorganic & medicinal chemistry》2011,19(1):498-503
Reported previously by our group, one-pot cycloaddition using naphthoquinone, sodium azide and alkyl halides can lead to the formation of both 1-alkyl-1H- and 2-alkyl-2H-naphtho[2,3-d]triazole-4,9-diones. Herein, the effect of leaving group and additive in dictating the selectivity between the formation of 1-alkyl-1H- and 2-alkyl-2H-naphtho[2,3-d]triazole-4,9-diones has been further investigated. In the process of investigating the factors that control the selectivity and the biological activity associated with these two compounds, a novel class of antibacterial cationic anthraquinone analogs has been developed. Although these compounds are structurally similar, different antibacterial profiles are noted. One lead compound, 4e manifests high potency (MIC < 1 ??g/mL) and selectivity against Gram positive (G+) pathogens including methicillin-resistant Staphylococcus aureus (MRSA) while exerting only modest activity against Gram negative (G−) bacteria. Other lead compounds (4f and 4g) exhibit broad antibacterial activity including MRSA and vancomycin-resistant Enterococcus faecalis (VRE) that is comparable to other commercially available cationic antiseptic chemicals. This unique difference in antibacterial profile may pave the way for the development of new therapeutic agents. 相似文献
3.
D'Andrea S Zheng ZB Denbleyker K Fung-Tomc JC Yang H Clark J Taylor D Bronson J 《Bioorganic & medicinal chemistry letters》2005,15(11):2834-2839
The synthesis and antibacterial activity of oxazolidinones containing dihydro-1,2-oxazine and 2-pyrazoline ring systems are described. Linezolid analogs utilizing dihydro-1,2-oxazines as morpholine mimics were prepared utilizing a nitrosoamine/diene 4+2 cycloaddition strategy. Pyrazolidine, hexahydro-pyridazine, and 2-pyrazoline analogs more closely related to eperezolid were also prepared. The most active of these new oxazolidinones were the dihydro-1,2-oxazine 6 and the 2-pyrazoline 20 both of which had potency similar to linezolid against a panel of Gram-positive bacteria. 相似文献
4.
《Bioorganic & medicinal chemistry letters》2014,24(7):1724-1729
A series of 11 novel amides of salinomycin were synthesized for the first time. All the obtained compounds were found to show potent antiproliferative activity against human cancer cell lines including the drug-resistant cancer cells. Four new salinomycin derivatives revealed good antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus epidermidis (MRSE). 相似文献
5.
Akritopoulou-Zanze I Phelan KM Marron TG Yong H Ma Z Stone GG Daly MM Hensey DM Nilius AM Djuric SW 《Bioorganic & medicinal chemistry letters》2004,14(14):3809-3813
We report the discovery of a novel class of macrolide antibiotics that have improved antibacterial activity against Ery-resistant organisms. 相似文献
6.
Novel quinazolines, having interesting antibacterial activity have been prepared, characterized and tested against a panel of susceptible and resistant Gram positive and Gram negative organisms. 相似文献
7.
A new class of enolphosphates derivatives, the 1-alkenyldiphosphates, was designed and a rapid and efficient synthesis for these compounds was developed. These new molecules showed interesting in vitro antibacterial activities (MIC) against Gram-positive bacteria (Staphylococcus aureus) and Gram-negative pathogens including Pseudomonas aeruginosa and Escherichia coli. 相似文献
8.
Minowa N Akiyama Y Hiraiwa Y Maebashi K Usui T Ikeda D 《Bioorganic & medicinal chemistry letters》2006,16(24):6351-6354
Synthesis and activity of derivatives at the O5 or O6 positions of 1-N-((S)-4-amino-2-hydroxybutyryl)-3′,4′-dideoxyneamine, which is the neamine moiety of arbekacin, were reported. Among these results, the 5-O-aminoethylaminocarbonyl derivative showed effective activity against Staphylococcus aureus expressing a bifunctional aminoglycoside-modifying enzyme AAC(6′)-APH(2″). 相似文献
9.
The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7 alpha positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol. 相似文献
10.
Morten Brændvang Colin Charnock Lise-Lotte Gundersen 《Bioorganic & medicinal chemistry letters》2009,19(12):3297-3299
Pyrimidine analogs of antimycobacterial purines have been synthesized and their biological activities evaluated. Several 5-formamidopyrimidines exhibited profound activity against Mycobacterium tuberculosis in vitro (IC90 ? 1.5 μg/mL), and they were essentially inactive against other bacteria. 相似文献
11.
Rajakumar P Mohammed Abdul Rasheed A Iman Rabia A Chamundeeswari D 《Bioorganic & medicinal chemistry letters》2006,16(23):6019-6023
Macrocyclic di- and tetra-amides with thia- and oxylinkages were synthesized and screened for in vitro anti-inflammatory activity. Cyclophane diamide 15 showed a dose-dependent activity, while the other cyclophane amides 16-20 exhibited mild activity. 相似文献
12.
John D. Williams Son T. Nguyen Shen Gu Xiaoyuan Ding Michelle M. Butler Tommy F. Tashjian Timothy J. Opperman Rekha G. Panchal Sina Bavari Norton P. Peet Donald T. Moir Terry L. Bowlin 《Bioorganic & medicinal chemistry》2013,21(24):7790-7806
The prevalence of drug-resistant bacteria in the clinic has propelled a concerted effort to find new classes of antibiotics that will circumvent current modes of resistance. We have previously described a set of bisamidine antibiotics that contains a core composed of two indoles and a central linker. The first compounds of the series, MBX 1066 and MBX 1090, have potent antibacterial properties against a wide range of Gram-positive and Gram-negative bacteria. We have conducted a systematic exploration of the amidine functionalities, the central linker, and substituents at the indole 3-position to determine the factors involved in potent antibacterial activity. Some of the newly synthesized compounds have even more potent and broad-spectrum activity than MBX 1066 and MBX 1090. 相似文献
13.
Xiaozhuo Chen Peng Xu Yanpeng Xu Lu Liu Yi Liu Di Zhu Pingsheng Lei 《Bioorganic & medicinal chemistry letters》2012,22(24):7402-7405
A series of novel modified 5-O-desosamine-ketolides were synthesized. The 5-O-desosamine fragment was removed from ketolide by an efficient and mild manipulation. 4-O-substituted desosamine was introduced into the ketolide aglycon and various coupling methods were essayed for the glycosylation. Three novel ketolides were tested for in vitro antibacterial activity against a panel of susceptible and resistant pathogens. Compound 26 showed potent activity against all the methicillin-sensitivity and resistant pathogens. 相似文献
14.
Perumal Rajakumar Rathinam Raja Subramaniyan Selvam Ramasamy Rengasamy Subramani Nagaraj 《Bioorganic & medicinal chemistry letters》2009,19(13):3466-3470
Synthesis of novel quinoline based dicationic benzimidazolophanes and imidazolophanes incorporating various spacer units is described. Some of the quinolinophanes 1b, 3a, 3b and 4a exhibit good antibacterial activity against most of the human pathogenic bacteria in the tested concentrations as compared to the other cyclophanes as well as the test control, streptomycin. 相似文献
15.
Burger MT Hiebert C Seid M Chu DT Barker L Langhorne M Shawar R Kidney J Desai MC Plattner JJ 《Bioorganic & medicinal chemistry》2006,14(16):5592-5604
A novel series of C(12) ethyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens, including those resistant to erythromycin. The C(12) modification involves replacing the natural C(12) methyl group in the erythromycin core with an ethyl group via chemical synthesis. From the C(12) ethyl macrolide core, a series of C(12) ethyl ketolides were prepared and tested for antibacterial activity against a panel of relevant clinical isolates. Several compounds were found to be potent against macrolide-sensitive and -resistant bacteria, whether resistance was due to ribosome methylation (erm) or efflux (mef). In particular, the C(12) ethyl ketolides 4k,4s,4q,4m, and 4t showed a similar antimicrobial spectrum and comparable activity to the commercial ketolide telithromycin. The in vivo efficacy of several C(12) ethyl ketolides was demonstrated in a mouse infection model with Streptococcus pneumoniae as pathogen. 相似文献
16.
Takhi M Murugan C Munikumar M Bhaskarreddy KM Singh G Sreenivas K Sitaramkumar M Selvakumar N Das J Trehan S Iqbal J 《Bioorganic & medicinal chemistry letters》2006,16(9):2391-2395
Novel oxazolidinone antibacterials containing N-hydroxyacetamidine moiety are synthesized with the diversity at C-5 terminus. These compounds have been evaluated against a panel of clinically relevant gram-positive and gram-negative pathogens. Most of the analogs in this series displayed activity superior to Linezolid and in vivo efficacies of selected oxazolidinones are also disclosed herein. 相似文献
17.
The design and synthesis of new fluoroquinolone antibacterial agents having substituted piperidine rings at the C-7 position are described. Most of the new compounds demonstrated high in vitro antibacterial activity. Several of them exhibited significant activities against gram-positive organisms, which were more potent than those of gemifloxacin, Linezolid, and vancomycin. 相似文献
18.
Eun Lee SeulAa Han Guo Hua Jin Hwa Jin Lee Woo-Young Kim Jae-Ha Ryu Raok Jeon 《Bioorganic & medicinal chemistry letters》2013,23(13):3976-3978
A series of 2-aminodihydroquinoline analogs were synthesized and their in vitro cytotoxicities against metastatic breast adenocarcinoma cell line MDA-MB-231 were tested. Five out of 16 compounds exhibited promising activity and structure–activity relationship revealed major role of dialkylaminoethyl substituents on dihydroquinoline ring for the activity. Two compounds, 5f and 5h, presented cytotoxicity with IC50 values of about 2 μM when the compounds were treated to the cells without serum. The cell proliferation was inhibited mildly when the cells cultured with serum. Flow cytometry analyses showed that those compounds arrested the cells at G2/M checkpoint when the cell cycle is active while they induce apoptosis when the cell growth is restricted due to the absence of growth factors. These results suggest the two novel compounds may have anticancer activity through cell cycle arrest and pro apoptosis mechanism. 相似文献
19.
Boonsong Kongkathip Anuch Hasakunpaisarn Suthinee Boonananwong Ngampong Kongkathip 《Steroids》2010,75(12):834-847
In an effort to determine the pharmaceutical utility and the structural requirements for activity against tumor cell lines, 30 novel 9,11-secosterol analogues with different side chains and degrees of oxidation at C-9 were synthesized starting from hecogenin. Evaluation of the synthesized compounds for cytotoxicity against KB, HeLa and MCF-7 cell lines revealed that some important structural features are required for activity. The presence of a cholesterol-type side chain, which appears to play a major role in determining the biological activity, the existence of a ketone functional at C-9 is also crucial for anticancer activity whereas hydroxyl/ketone function at C-22 on the side chain did not increase cytotoxicity. 相似文献
20.
Maffioli SI Ciabatti R Romanò G Marzorati E Preobrazhenskaya M Pavlov A 《Bioorganic & medicinal chemistry letters》2005,15(16):3801-3805
New derivatives of the glycopeptide antibiotic A40926 were synthesized and evaluated for antimicrobial activity against VRE. Deacylated A40926 was obtained by microbial transformation of the parent antibiotic with the use of Actinoplanes teichomyceticus ATCC 31121. Regioselective synthesis of alkylated derivatives of Deacyl A40926 was carried out using lipophilic aliphatic and aromatic halides or aldehydes. Further modification of the two carboxylic acids was performed to increase antibiotic activity. Poor antimicrobial activity was observed for the derivatives obtained by lipophilic mono- or dialkylation of the amino groups present on the molecule, while simultaneous condensation of both carboxylic groups, in hydrophobic derivatives, with dibasic amines led to a strong increase in antibiotic activity. 相似文献