Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment / 药学学报

Based on the principle of molecular hybridization, fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment. The results showed that these compounds had better inhibitory effects on the tested bacteria. In particular, the activities of compounds Ⅲf and Ⅲi against S. aureus, E. coli, methicillin-resistant S. aureus (MRSA) and fluoroquinolone-resistant E. coli (FREC) were the most significant, the minimal inhibitory concentration (MIC) of Ⅲf was 1, 8, 4, 16 μg·mL-1 respectively, and the MIC of Ⅲi was 4, 4, 16, 8 μg·mL-1 respectively, which were slightly lower than that of the control drug oxacillin, and their anti-E. coli, MRSA and FREC activities were superior to that of the control drug oxacillin. Their activities to S. aureus were close to that of oxacillin, and to E. coli, MRSA and FREC were superior to that of oxacillin, which is worthy of further study.

Synthesis and antibacterial activities of novel sulfonamide derivatives containing a fused-ring / 药学学报

To find antibacterial candidate compounds, eighteen novel sulfonamide derivatives containing a fused-ring were designed and synthesized on the basis of previous studies, with structures confirmed by 1H NMR, 13C NMR and MS. Antibacterial activities of the products were evaluated by the agar dilution method. The results show that these derivatives have different degrees of inhibitory activity on the tested bacteria, with the compounds IIi and IIr the most potent. The MIC of IIi for S. aureus, E. coli and MRSA was 8, 32 and 16 μg·mL-1, respectively, and the MIC of the IIr was 8, 64 and 32 μg·mL-1, respectively. The anti-MRSA activities of the two compounds is significant and is worthy of further structural optimization and study.

Synthesis and Antibacterial Activity of Novel 7-Phosphoryl Quinolone Derivatives / 中国药学杂志

OBJECTIVE: To search more effective antibacterial candidate agents by designing a series of 7-phosphoryl quinolone derivatives,exploring the synthetic methods, and evaluating their antibacterial activities. METHODS: The quinolone derivatives were synthesized using phosphate and quinolone intermediates as raw materials and alkaline ionic liquid [Bmim] OH as catalyst with microwave assistance. The antibacterial activities of the products were evaluated by agar dilution method. RESULTS: Eight title compounds were prepared, and their structures were clearly established by IR, NMR and MS. The in vitro experiment showed that the derivatives had potential antibacterial activity. Especially, compound Ⅱc showed more potent activities against S. aureus, E. coli, MREC-1# and MREC-2# with minimum inhibitory concentrations (MICs) of 1.6, 6.4, 12.8,6.4 mg•mL-1, respectively, and the MICs of compound Ⅱ gagainst S. aureus, E. coli, MREC-1# and MREC-2# were 1.6, 3.2, 6.4, 6.4 mg•mL-1, respectively. Its activity on drug-resistant bacteria was better than that of the control drug norfloxacin. CONCLUSION: The quinolone derivatives are highly active on drug-resistant bacteria.It is worth of further study.

Synthesis and bioactivity of novel ester derivatives of rhein / 中国药学杂志

OBJECTIVE: To design and synthesize a series of novel ester derivatives of rhein were designed and synthesized, and evaluate their anti-MRSA activity. METHODS: The title compounds were synthesized with rhein and α-hydroxyphosphonate as starting materials, EDCI/HOBT and [Bmim] BF4 as catalyst system. And the anti-MRSA activities of the products were evaluated by the agar dilution method. RESULTS: Ten title compounds were synthesized,and their structures were clearly established by IR, NMR and MS. The RESULTS: showed that the derivatives have different anti-MRSA activity. Especially, showed potent activity against MRSA with the minimum inhibitory concentration(MIC) and minimum bactericidal concentration(MBC) values of compound Ⅱ-3 was 128, 512 μg·mL-1 respectively,superior to rhein and oxacillin. And the MIC and MBC of compound Ⅱ-10 to MRSA was 32, 64 μg·mL-1, its anti-MRSA activity was obviously better than that of rhein and oxacillin. CONCLUSION: The ester derivatives of rhein are significant resistant to MRSA, which is worth for further study.

Synthesis and Bioactivity of Novel Phosphonate Derivatives Containing Thiophene and Sulfonamide Group / 中国药学杂志

OBJECTIVE: To design and synthsize a series of novel phosphonate derivatives. METHODS: First, the intermediates of aminophosphonate was prepared by solvent-free one-pot method using aromatic aldehyde, ammonium acetate, diethyl phosphite and Al(OTf)3 as raw materials. Then, using basic ionic liquid OH as catalyst, the target compounds were synthesized by the reaction of intermediate with sulfonyl chloride. And the antibacterial activities of the products were evaluated by the agar dilution method. RESULTS: Twelve title compounds were synthesized, and their structures were clearly established by 1H-NMR, 13C-NMR and MS. The results showed that the derivatives have different inhibitory activities against Gram-positive bacteria and Gram-negative bacteria, especially the compounds Ⅱe and Ⅱk showed better activity, the MIC of the former for S.aureus, E. coli, MRSA and MREC was 32, 64, 32, and 128 μg•mL-1, respectively, and the MIC of the latter was 16, 64, 32, and 64 μg•mL-1, respectively. Its antibacterial activities were significantly better than that of the control drug sulfadiazine, and close to that of gatifloxacin. CONCLUSION: These derivatives have potential antibacterial activity, which is worth for further structural optimization and study.

Synthesis and antitumor activity of phosphonate derivatives containing amino acid / 药学学报

In search of effective anticancer agents, fifteen new phosphonate derivatives were designed and synthesized. Their structures were clearly established by elemental analysis, IR, 1H NMR and 13C NMR, and their antitumor activities were evaluated by MTT assay. Preliminary results in bioactivity tests indicated that some title compounds exhibited better activity. Among the active compounds, compounds 4e, 4n had better inhibition effect on A-549 cells growth with IC50 values of 8.7±0.8, 8.2±1.0 μmol·L-1, the IC50 values of compound 4c was 9.8±0.9 μmol·L-1 against SGC-7901 cells and compounds 4l, 4n exhibited more potent activities against EC-109 with IC50 values of 9.5±0.6, 9.4±0.5 μmol·L-1.

Synthesis and antitumor activity of cinnamoyloxy phosphonate derivatives / 药学学报

In search of more effective anticancer agents, twelve compounds were designed and synthesized via microwave-assisted reactions of cinnamoyl chloride with α-hydroxyphosphonate. The structures of all the compounds were confirmed by IR, NMR and elemental analysis. Bioassay of the compounds were tested. They exhibited certain antitumor activities. Especially, compound 3c had obvious inhibitory effect on growth of SGC-7901 cells in vitro at 20 μmol·L-1, and compound 3h showed better inhibitory effect on growth of SGC-7901 cells in vitro at 5 μmol·L-1, the inhibition ratio were 68.8% and 48.0%, respectively.

Synthesis and bioactivity evaluation of novel chlorogenic acid derivatives containing amide group / 中国药学杂志

OBJECTIVE: To design and synthesize a series of chlorogenic acid derivatives in order to improve the solubility and lipid-water partition coefficients of chlorogenic acid, and test the bioactiviteies of the target compounds. METHODS: The target compounds were synthesized from chlorogenic acid by three-step reactions of hydroxyl protection, acylation, and deprotection. The antitumor activities of the compounds were evaluated against two different tumor cell lines by MTT assay, and the DPPH method was used to measure the antioxidant activities of the compounds. RESULTS: Eight title compounds were prepared, the structures of the compounds were confirmed by IR and NMR. The MTT assay showed that the compounds exhibited certain antitumor activities and better antioxidant activities, and the activities against A-549 and SGC-7901 tumor cells and the scavenging ratio to DPPH· were similar to those of chlorogenic acid. CONCLUSION: Chlorogenic acid derivatives containing amide group still have antitumor and antioxidant activities.

Design, synthesis and antitumor activities of novel E-substituted 2,3-diaryl propenoic acyloxy phosphonate derivatives / 药学学报

According to the super-position principle of the reinforcement of biological activities, a series of novel E-substituted 2, 3-diaryl propenoic acyloxy phosphonate derivatives were designed and synthesized. And the structures of the target compounds were confirmed by IR, 1H NMR, 13C NMR and elemental analysis. Furthermore, the cytotoxicities of all compounds on A-549, SGC-7901 and EC-109 in vitro were evaluated by MTT assay, and some of them showed good antitumor activity. Among the active compounds, especially, the IC50 value of compound 3e was (12.7 ± 1.9) μmol x L(-1) against A-549 cells, similar to cisplatin [IC50 = (8.0 ± 1.5) μmol x L(-1)], compounds 3g and 3k had better inhibition effect on EC-109 cells growth, with the IC50 values of (9.5 ± 1.8) μmol x L(-1) and (11.5 ± 0.9) μmol x L(-1) respectively, and compounds 3i and 3k exhibited good cytotoxic property on A-549, SGC-7901 and EC-109, which were worth further investigation.

Analysis on the diagnosis and treatment of a cluster of cases infected by new bunyavirus / 中华预防医学杂志

<p><b>OBJECTIVE</b>To analyze and summarize the clinical characteristics, experience of diagnosis and treatment of cases infected by new bunyavirus, which occurred in Henan province in 2010.</p><p><b>METHODS</b>The clinical characteristics and effect of diagnosis and treatment of 5 cases were analyzed using descriptive epidemiological method. Blood specimens were detected by RT-PCR and pathogen separation.</p><p><b>RESULTS</b>PCR testing was positive for all 5 cases. New bunyavirus were isolated from 2 cases. In 5 cases, fever (5/5), the whole body aches (5/5), fatigue (5/5), anorexia (5/5), nausea (5/5), the chills (4/5), cough (4/5), expectoration (4/5), vomiting (3/5), conjunctival hyperemia (3/5); Leukocyte reduction (5/5), thrombocytopenia (5/5), elevated alanine aminotransferase (4/5), elevated aspartate aminotransferase (4/5), elevated lactate dehydrogenase (5/5), creatine kinase elevations (4/5), urinary protein (3/5). By symptomatic and supportive treatment and prophylactic antibiotics, the first case died and the other 4 cases were cured. The average course of disease was 15.4 days.</p><p><b>CONCLUSION</b>Cases infected by new bunyavirus have complicated clinical feature and multiple organ damage. If symptomatic treatment is in time, prognosis will be good.</p>