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.

Response of bisphosphonate therapy in recurrent tumoral calcinosis

Tumoral calcinosis is a rare condition characterized by solitary or multiple, periarticular masses. Surgical excision of the tumoral calcinosis lesion is a well-documented treatment, but recurrences are not uncommon. A case of 42 year old male patient of tumoral calcinosis presented to us with history of repeated surgical excision twice in past 8 years for recurrent swellings. He was started on IV zoledronic acid and the patient has shown improvement after two years with no recurrence in follow up.

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 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 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.

Aplicação de fosfito de potássio, cálcio ou magnésio para a redução da podridão-do-pé do mamoeiro em casa de vegetação / Papaya foot rot reduction under nursery conditions with application of potassium, calcium, or magnesium phosphate

O controle da podridão-do-pé (Phytophthora palmivora) do mamoeiro (Carica papaya) é essencial para reduzir perdas e aumentar a produtividade dos plantios. Sete fosfitos foram avaliados em plântulas (~10cm de altura) de mamoeiro da cultivar 'Tailândia Roxão'. Experimentos foram conduzidos com os seguintes objetivos: determinar a melhor forma de aplicação do fosfito (pulverização ou rega); determinar o melhor período prévio à inoculação do patógeno para aplicação do fosfito; determinar a quantidade de aplicações de fosfito; determinar o efeito de diferentes fosfitos sobre a doença. Os resultados dos testes mostraram que: o método mais adequado para aplicação dos fosfitos foi a pulverização da parte aérea; a aplicação dos fosfitos deve ocorrer com pelo menos 48h antes da inoculação do patógeno; duas pulverizações semanais por três semanas consecutivas antes da inoculação do patógeno reduziram a doença; e fosetyl-Al e todos os fosfitos testados [fosfito A (40 por cento P2O5 + 20 por cento K2O, 150mL p.c. 100L-1), B (40 por cento P2O5 + 20 por cento K2O, 250mL), C (10 por cento P2O5 + 6 por cento Ca, 400mL), D (20 por cento P2O5 + 20 por cento K2O, 200mL), E (40 por cento P2O5 + 6 por cento Mg, 150mL), F (30 por cento P2O5 + 20 por cento K2O, 175mL), G (20 por cento P2O5 + 20 por cento K2O, 200mL)] reduziram a doença.

Foot rot, caused by Phytophthora palmivora, is an important disease of papaya (Carica papaya). Disease control is of extreme importance to reduce losses and to increase productivity. Seven phosphites were tested in greenhouse using papaya seedlings (~ 10cm height) of the cultivar 'Tailândia Roxão'. Experiments were conducted with the following objectives: to determine the most effective method for phosphite application (spray or drench) to reduce disease; to determine the period for phosphite application before pathogen inoculation on plants; to determine the number of phosphite applications; to determine the effects of different phosphites on disease severity. Data from experiments showed that: spraying of aerial plant parts was the most adequate method for phosphite application; phosphites should be applied at least 48h before the inoculation of the pathogen on plants; two weekly phosphite sprays for three consecutive weeks before the pathogen inoculation on plants reduced disease, and; fosetyl-Al and all tested phosphites [phosphite A (40 percent P2O5 + 20 percent K2O, 150mL c.p. 100L-1), B (40 percent P2O5 + 20 percent K2O, 250mL), C (10 percent P2O5 + 6 percent Ca, 400mL), D (20 percent P2O5 + 20 percent K2O, 200mL), E (40 percent P2O5 + 6 percent Mg, 150mL), F (30 percent P2O5 + 20 percent K2O, 175mL), G (20 percent P2O5 + 20 percent K2O, 200mL)] reduced disease severity.