Atividade residual e carência irregular do ácido diclorofenoxiacético (2, 4-d) no desenvolvimento inicial da soja / Residual activity and irregular depletion of dichlorophenoxyactic acid (2, 4-d) in the early development of soybean / Actividad residual y carencia irregular del ácido diclorofenoxiacético (2, 4-d) en el desarrollo inicial de la soja

O 2,4-D (ácido diclorofenoxiacético) é amplamente utilizado no controle seletivo, pós-emergência, de plantas de folha estreita, como trigo, milho, arroz, entre outras. Contudo seu uso indiscriminado pode ocasionar problemas no desenvolvimento da cultura. O objetivo do trabalho foi avaliar os danos causados pelo uso inadequado do 2,4-D no desenvolvimento inicial da soja (Glycine max). Os tratamentos consistiram na combinação de cinco períodos de carência: um, quatro, oito, 12 e 15 dias antes da semeadura da soja e duas doses de aplicação: a dose recomendada e a dose duplicada (L/ha), consistindo em um esquema fatorial 5x2 com três repetições. As plantas foram cultivadas por 44 dias, e em seguida coletadas e analisadas quanto à taxa de germinação (%), número de rebrota, índice de clorofila, comprimento de raiz e parte aérea (cm), massa seca e fresca (g). A dose duplicada revelou maior efeito sobre todas as variáveis analisadas, reduzindo em 20% a porcentagem de emergência. O índice de clorofila decresceu quando comparados o menor período de carência (um dia) e o maior (15 dias), e na dose duplicada. A massa seca também foi superior na dose recomendada, assim como o comprimento da raiz e da parte aérea. Os períodos de carência de um, quatro e oito dias foram os que mais influenciaram o crescimento da raiz.

Dichlorophenoxyacetic acid (2,4-D) is widely used in the selective, post-emergence control of narrow-leaf plants such as wheat, corn, and rice, among others. However, its uncontrolled use can cause problems in the development of the crop. The purpose of this paper was to evaluate the damage caused by the inadequate use of 2,4-D in the early development of soybean (Glycine max). The treatments consisted of a combination of five grace periods: 1, 4, 8, 12 and 15 days before sowing; and two application doses: the recommended dose and a duplicate dose (L/ha), consisting of a factorial matrix of 5x2, with three replicates. The plants were cultivated for 44 days, then collected and analyzed for germination rate (%), regrowth number, chlorophyll index, root and shoot length (cm), dry and fresh mass (g). The duplicate dose showed a greater effect on all analyzed variables, reducing the emergency percentage by 20%. The chlorophyll index decreased when compared to the shortest (1 day) and longest (15 days) grace periods, and in the duplicate dose. Dry mass was also higher when using the recommended dose, as well as the root and shoot length. Grace periods of 1, 4 and 8 days were the ones that were most influenced the root growth.

El 2,4-D (ácido diclorofenoxiacético) es ampliamente utilizado en el control selectivo, pos emergencia, de plantas de hoja estrecha, como trigo, maíz, arroz, entre otras. Sin embargo, su uso indiscriminado puede ocasionar problemas en el desarrollo de la cultura. El objetivo del trabajo fue evaluar los daños causados por el uso inadecuado del 2,4-D en el desarrollo inicial de la soja (Glycine max). Los tratamientos consistieron en la combinación de cinco períodos de carencia: 1, 4, 8, 12 y 15 días antes de la siembra de la soja y dos dosis de aplicación: la dosis recomendada y la dosis duplicada (L/ha), consistente en un esquema factorial 5x2 con tres repeticiones. Las plantas fueron cultivadas por 44 días, y luego recolectadas y analizadas en cuanto a la tasa de germinación (%), número de rebrote, índice de clorofila, longitud de raíz y parte aérea (cm), masa seca y fresca (g). La dosis duplicada reveló un mayor efecto sobre todas las variables analizadas, reduciendo en un 20% el porcentaje de emergencia. El índice de clorofila disminuyó cuando se comparó el menor período de carencia (1 día) y el mayor (15 días), y en la dosis duplicada. La masa seca también fue superior en la dosis recomendada, así como la longitud de la raíz y de la parte aérea. Los períodos de carencia de 1, 4 y 8 días fueron los que más influenciaron el crecimiento de la raíz.

Design, synthesis and PPAR agonist activities of novel L-tyrosine derivatives containing phenoxyacetyl moiety / 药学学报

The design, synthesis and bioevaluation of a series of novel L-tyrosine derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Four intermediates and twenty L-tyrosine derivatives containing phenoxyacetyl moiety TM1 were synthesized starting from L-tyrosine via four step reactions including the esterification of carboxyl group, phenoxyacetylation of a-amino group, bromoalkylation of phenolic hydroxyl group and then nucleophilic substitution reaction with various heterocyclic amines in 21%-75% overall yield. Subsequently TM1 were hydrolyzed to give sixteen corresponding target compounds TM2 in 77%-99% yield. The chemical structures of the thirty-nine new compounds were identified using 1H NMR, 13C NMR techniques and thirty-five were confirmed by HR-MS techniques. Screening results in vitro showed that the PPAR relative activation activities of the target molecules are weak overall, while compound TM2i reaches 50.01%, which hints that the molecular structures of these obtained compounds need to be modified further.

Síntese de tiossemicarbazonas derivadas de 2-(fenoxi)acetaldeídos com potencial atividade antiviral / Synthesis of some thiosemicarbazones of 2-(phenoxy)acetaldehydes as potential antiviral agents

As tiossemicarbazonas constituem classe de compostos que têm apresentado amplo espectro de ação, englobando atividades antibeoplásica, antiinflamatória, tuberculostática e antiviral, inclusive anti-HIV. Diante da potencial atividade antiviral das tiossemicarbazonas, planejamos sintetizar nova série de compostos a partir da tiossemicarbazida e fenoxiacetaldeídos diversamente substituídos. Os produtos obtidos tiveram sua estrutura química comprovada por meio de métodos espectroscópicos no infravermelho e ressonância magnética nuclear de hidrogênio e microanálise. Cinco compostos foram testados visando encontrar possível atividade antiviral. Nos ensaios utilizaram-se culturas de células contínuas VERO e L929 infectadas pelo vírus herpes humano tipo I, da vaccínia, poliomielítico tipo I e da estomatite vesiculosa...

Purification and characterization of extracellular penicillin V acylase from Fusarium sp. SKF 235.

Penicillin V acylase from Fusarium sp. SKF 235 culture filtrate was purified to homogeneity. The enzyme was a glycoprotein and composed of single polypeptide chain with molecular weight of 83,200 Daltons. The pH and temperature optima were 6.5 and 55 degrees C, respectively. The KM for penicillin V was 10 mM but the enzyme was inhibited by penicillin V at concentrations above 50 mM. Products of reaction, 6-aminopenicillanic acid and phenoxyacetic acid inhibited the enzyme competitively and noncompetitively with Ki values of 18 mM and 45 mM, respectively. The enzyme specifically hydrolyzed penicillin V, cephalosporanic acid V and penicillin V sulphoxide. Other phenoxy acetyl amides studied were not hydrolysed. It is proposed that phenoxyacetyl moiety alone is not recognized by the penicillin V acylase and in addition, the beta-lactam structure contributes in formation of enzyme-substrate complex.

Diuretics physiology pharmacology and clinical use

Uricosuric diuretics have been developed to counteract renal urate retention accompanying diuretic-induced extracellular volume contraction. Their intrinsic uricosuric activity would prevent diuretic-induced hyperuricemia. Ticrynafen, a prototype uricosuric diuretic, has largely fallen into disuse because of hepatic toxicity. However, one lesson learned during the short period that ticrynafen was available in the US is that the administration of a potent uricosuric agent to a patient previously trated with diuretics can precipitate acute renal failure, possibly as a consequence of uric acid nephropathy. Another novel uricosuric diuretic, indacrinone, is composed of two enantiomorphic isomers exhibiting predominantly either a uricosuric or a natriuretic action. Manipulation of the isomer ratio currently is being attempted with a view toward obtaining a combination that produces little change in the serum urate during chronic diuretic therapy. Uricosuric diuretics have the therapeutic potential to treat hypertension and edematous states without increasing the serum urate. Although current information suggests that chronic asymptomatic hyperuricemia poses very little health hazard, future data could indicate that it may be desirable to maintain the serum urate near the normal range