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Khang X. Nguyen,Phuc H. Pham,An C.D. Nguyen,Chuc T. Nguyen,Tung T. Nguyen,Phong D. Tran,Nam T.S. Phan 한국공업화학회 2020 Journal of Industrial and Engineering Chemistry Vol.92 No.-
A Fe-Mo-Se nanopowder, synthesized by a solvothermal protocol, was utilized as a heterogeneouscatalyst for the synthesis of 2-arylquinazolines from DL-α-phenylglycine-based α-amino acids and2-nitrobenzyl alcohols via domino transformations. High yields and selectivity were achieved undersolvent-free conditions. The Fe-Mo-Se catalyst offered considerably higher activity than numeroushomogeneous and heterogeneous catalysts. To our best knowledge, this domino reaction is new, and theutilization of iron-molybdenum selenide catalyst in the synthesis of quinazolines was not previouslyreported.
Mostafa M. Ghorab,Zienab H. Ismail,Mohamad Abdalla,Awwad A. Radwan 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.6
A novel series of quinazolines 5–10, triazoloquinazolines11–17 and triazinoquinazoline 19 bearing abiologically active sulfonamide moiety were synthesized,utilizing methyl 2-isothiocyanato benzoate 2. Some of thenewly synthesized compounds revealed promising bacterialgrowth inhibition, compared with the ampicillin, as thereference drug. A LigandScout approach-generated pharmacophoremodel for the Staph aureus bacteria growthinhibition was done. The degree of fitting of the test setcompounds (3, 4, 6, 8, 11, 17) to the generated hypotheticalmodel revealed a qualitative measure of the more orless microbial inhibition of Staphylococcus aureus. Compounds(7, 8, 10, 12, 15, 17 and 22), which revealed significantactivity, are able to effectively satisfy the proposedpharmacophore geometry, using the energy accessibleconformers (Econf\20 kcal/mol).
이병국,류현호,허탁,민용일,이형연,정경운 대한응급의학회 2010 大韓應急醫學會誌 Vol.21 No.4
Fenazaquin (4-[[4 (1,1-dimethylethyl) pheynyl]ethoxy]quinazoline)is an insecticide that inhibits NADH ubiquinone oxidoreductase of the mitochondria, which is also known as complex I. An 83 year old female was brought to our emergency department (ED) having been found collapsed and unconscious at home by her family. She had ingested up to 100 ml from a bottle of 20% fenazaquin solution. In the ED,she showed severe persistent lactic acidosis despite a seemingly stable hemodynamic condition. Despite intensive supportive management, including positive pressure ventilation,packed red cell transfusion, hemodialysis, and intravenous N-acetylcysteine administration, the lactic acidosis did not respond. To our knowledge, this is the first report of fenazaquin poisoning in humans. No antidote for fenazaquin is known. In this case report, we discuss clinical characteristics and possible pathophysiologic mechanism of fenazaquin poisoning with a literature review.
안명주,정기선,김성태,이지은,임성희,이민영,권희진,김인영,선종무,안진석,Keunchil Park,김혜수,유쾌한 한양대학교 의과대학 2015 Hanyang Medical Reviews Vol.35 No.3
There have been conflicting reports on the continuation of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) in patients with newly developed or progressive brain metastasis of non-small cell lung cancer (NSCLC). Patients with newly developed or progressive intracranial lesions, but who maintained well-controlled extracranial disease during erlotinib treatment, were enrolled in this study. The proposed therapy included stereotactic radiosurgery (SRS), whole brain radiotherapy (WBRT), and/or surgical resection for intracranial lesions. Erlotinib treatment was continued simultaneously unless extracranial disease progressed. The evaluation of both extra- and intra-cranial lesions was performed every 3 months. From October 2009 to June 2012, 14 patients were enrolled in this pilot study. For intracranial disease, 4 patients received SRS alone, 7 patients received both SRS and WBRT, 2 patients received SRS, WBRT and surgical resection, and 1 patient received no local therapy due to the presence of asymptomatic lesions. Of the patients with extracranial disease who were placed on continued erlotinib therapy, 6 patients (42.9%) showed partial response (PR), while 7 patients (50.0%) remained in stable disease (SD). The progression-free survival (PFS) of extracranial and intracranial disease was 11.1 (range 1.6-34.6) and 10.2 (range 1.5-34.6) months, respectively. In 5 cases, brain lesions relapsed before the progression of extracranial disease. Overall survival (OS) was 22.6 (range 2.1-50.4) months. For NSCLC patients with progression of only intracranial disease during erlotinib treatment, the continuation of erlotinib in combination with local therapy to brain metastases can be an effective treatment option.
T. Panneer Selvam,P. Vijayaraj Kumar 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.11
A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index (0.51 ± 1.63, 0.48 ± 1.28and 0.50 ± 1.53, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino)thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.
Selvam, T. Panneer,Kumar, P. Vijayaraj Korean Chemical Society 2010 Bulletin of the Korean Chemical Society Vol.31 No.11
A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index ($0.51{\pm}1.63$, $0.48{\pm}1.28$ and $0.50{\pm}1.53$, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.
Chung-Kyu, Ryu,Yang Hui, Kim,Hyun Ah, Im,ji Young, Kim,joo Hee, Yoon,Aram, Kim 이화여자대학교 약학연구소 2012 藥學硏究論文集 Vol.- No.22
6,7-Bis(arylthio)-quinazoline-5,8-dione and furo[2,3-f]quinazolin-5-ol derivatives were synthesized and tested for in vitro antifungal activity against Candida, Aspergillus species, and Cryptococcus neoformans. Among them tested, many of furo[2,3-f]quinazolin-5-ols and 6,7-bis(arylthio)-quinazoline-5,8-diones showed good antifungal activity. The compounds completely inhibited the growth of all against Candida and Aspergillus species tested at the MIC level of 12.5μg/mL. The results suggest that furo[2,3-f]quinazolin-5-ols and 6,7-bis(arylthio)-quinazoline-5,8-diones would be promising antifungal agents.
Govindaraj Saravanan,Veerachamy Alagarsamy,Pandurangan Dineshkumar 대한약학회 2021 Archives of Pharmacal Research Vol.44 No.8
A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterizedby FT-IR, 1H NMR, mass spectroscopy and bases of elementalanalysis with the aim of developing potent analgesic,anti-inflammatory and antimicrobial agents. Tailflicktechnique, carrageenan-induced foot paw edema testand agar streak dilution test were performed for screeninganalgesic, anti-inflammatory and in vitro antimicrobialactivity respectively. Moreover all compounds wereexamined for its ulcerogenicity. Results revealed that entireseries of compounds exhibited mild to good analgesic, antiinflammatoryand antimicrobial activity with low to moderateulcer index. The relationship between the functionalgroup variation and the biological activity of the evaluatedcompounds was discussed. Out of various synthesizedcompounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl)isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was foundto be the most active compound.