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Synthesis of Furodiketochroman and bis-Furocoumarin Derivatives and their Biological Activity
Hishmat, O.H.,El-Shabraway, O.A.,El Diwani, H.I.,Fawzy, N.M. The Pharmaceutical Society of Korea 1988 Archives of Pharmacal Research Vol.11 No.2
A number of substituted furodiketochroman derivatives ($lll_{a-f}$) have been synthesized by fusion of aromatic aldehydes with 5-hydroxybergapten and 5-hydroxyisopimpinellin. On the other hand, when the reaction was carried out in a solvent, the corresponding bis-furoccumarin derivatives ($lV_{c-n}$) were obtained. The anticoagulant effect of compounds $lll_{a,b,d}$ and $lv_{b,c,f,g,i,k}$ was tested. They failed to demonstrate any significant effect. The effect of the tested compounds on the arterial blood pressure was studied. Compounds $lV_c$, $lll_d$, $lll_b$, $lV_b$, $lV_k$ and $lV_i$ showed lowering effects on the normal systolic blooc pressure of anaesthetized rats in a decreasing manner.
Synthesis and Biological Activities of New Substituted Indoles
Hishmat, Orchidee H.,Nakkady, Sally S.,El Shabrawy, Osama A.,Mahmoud, Sawsan S. The Pharmaceutical Society of Korea 1992 Archives of Pharmacal Research Vol.15 No.1
2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.
Synthesis and antimickrobial activity of benzofuran-carboxamide derivatives
Hishmat, O.H.,Nasef, A.M.,El-Naem, Sh.I.A.,Shalaby, A.M. The Pharmaceutical Society of Korea 1989 Archives of Pharmacal Research Vol.12 No.4
The reaction of the sodium salts of 4-methoxy and 4, 7-dimethoxy 6-hydroxy benzofuran-5-carboxylic acid with ethyl chloroformate yields the corresponding dicarbethoxy derivatives. The N-substituted amides were obtained by treating the latter compounds with amines. The corresponding hydrazides were synthesized by the reaction of hydrazine hydrate on the dicarbethoxy derivatives which spontaneously cyclized to 5-substituted-2, 3- dihydro-1, 3, 4, -oxadiazol-2-one. Also the reaction with phenyl hydrazine has been studied. The dicarbethoxy derivatives and N-substituted amides were tested against Gram positive and Gram negative bacteria in vitro. Most of the compounds posses moderate or slight activity against Gram positive bacteria.
El-Diwani, H.I.,Nakkady, S.S.,El-Shabrawy, O.,Gohar, A-K.M.N.,Hishmat, O.H. The Pharmaceutical Society of Korea 1988 Archives of Pharmacal Research Vol.11 No.1
Several 4-cyano-1-benzofuranyl-1-butanone derivatives were synthesized and screened for potential antiinflammatory and analgesic activities. The effect of structural variation of these molecules on biological activities was systematically examined. Among these compounds $V_a,\;V_c\;and\;VI_e$ were found to demonstrate a significant antiinflammatory effect. Compounds $VI_e,\;V_a,\;I_d,\;I_band\;VII_f$ were also significantly effective as analgesic ones.
Refaie Marwa Monier Mahmoud,Shehata Sayed,El-Hussieny Maram,Fawzy Michael Atef,Ahmed Nagwa Zenhom Mustafa,Marey Heba,Hishmat Asmaa Mohammed,Alkully Turki,Rahman Eman Shaaban Mahmoud Abd El 한국독성학회 2024 Toxicological Research Vol.40 No.1
One of the commoly used chemotherapeutic agents is 5-Fluorouracil (5-FU). Unfortunately, the clinical administration of 5-FU is complicated with serious cardiotoxic effects and the safe use becomes an urgent task in cardio-oncology. Till now, there are no studies discussed the role of empagliflozin (EMP) against 5-FU cardiotoxicity. Thus, we investigated this effect and the involved mechanisms in 5-FU induced heart injury. Forty male rats of Wistar albino species were used and divided randomly into four groups. Group I is the control group, group II is EMP given group, group III is 5-FU cardiotoxic group and group IV is 5-FU plus EMP group. 5-FU (150 mg/kg) was administered as a single intraperitoneal (i.p.) dose on 1st day to induce cardiotoxicity with or without EMP (30 mg/kg/d) orally for 5 days. The dose of 5-FU is relevant to the human toxic dose. Our data showed that 5-FU given group caused cardiotoxicity with significant increase of serum cardiac enzymes, toll like receptors, enhancement of nuclear factor kappa B (NF-κB), interleukin1β (IL1β), IL6, myeloid-differentiation-factor 88 (MYD88), heart weight, malondialdehyde (MDA), tumor-necrosis-factor-alpha (TNFα), sodium glucose co-transporter 2 (SGLT2), P53 and caspase3 expression with clear histopathological features of cardiotoxicity. Moreover, there is a significant decrease in reduced glutathione (GSH) and total antioxidant capacity (TAC). Interestingly, co-administration of EMP could ameliorate 5-FU induced biochemical and histopathological changes. This effect may be due to modulation of SGLT2, decreasing inflammation, oxidative stress and apoptosis with downregulation of an essential inflammatory cascade that mediates 5-FU cardiotoxicity; TNFα/TLR/NF-κB.