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Aakanksha R. Patil M. H. Keswani 《Burns : journal of the International Society for Burn Injuries》1985,11(6):444-445
The use of potato peels as a dressing for burn wounds has been reported previously. A technique of preparing bandage rolls with boiled potato peels is now presented, which makes dressing of a burn wound more convenient. 相似文献
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Sohn EY Noetzli LJ Gera A Kato R Coates TD Harmatz P Keens TG Wood JC 《British journal of haematology》2011,155(1):102-105
This study compared pulmonary function tests (PFTs) with cardiac, pancreatic and liver iron in 76 thalassemia major (TM) patients. Restrictive lung disease was observed in 16%, hyperinflation in 32% and abnormal diffusing capacity in 3%. While no patients met Global Initiative for Chronic Lung Disease criteria for airways obstruction, there were indicators of small airways disease and air trapping. PFTs did not correlate with somatic iron burden, blood counts or haemolysis. Restrictive lung disease was associated with inflammation. We conclude that TM patients have pulmonary abnormalities consistent with small airways obstruction. Restrictive disease and impaired diffusion are less common. 相似文献
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N‐hydroxy‐substituted 2‐aryl acetamide analogs: A novel class of HIV‐1 integrase inhibitors 下载免费PDF全文
Utsab Debnath Prachi Kumar Aakanksha Agarwal Ajay Kesharwani Satish K. Gupta Seturam B. Katti 《Chemical biology & drug design》2017,90(4):527-534
An in silico method has been used to discover N‐hydroxy‐substituted 2‐aryl acetamide analogs as a new class of HIV‐1 integrase inhibitors. Based on the molecular requirements of the binding pocket of catalytic active site, two molecules (compounds 2 and 4b ) were designed as fragments. These were further synthesized and biologically evaluated. In vitro potency along with docking studies highlighted compound 4b as an active fragment which was further used to synthesize new leads as HIV‐1 integrase inhibitors. Finally, six promising compounds (compounds 5b , 5c , 5e, 6–2c, 6–3b, and 6–5b ) were identified by integrase inhibition assay (>50% inhibition). Based on in vitro anti‐HIV‐1 activity in a reporter gene‐based cell assay system, compounds 5d , 6s , and 6k were found as novel HIV‐1 integrase inhibitors due to its better selectivity index. Additionally, docking study revealed the importance of H‐bond as well as hydrophobic interactions with Asn155, Lys156, and Lys159 which were required for their anti‐HIV‐1 activity. 相似文献
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A Me3SI-mediated simple and efficient protocol for the chemoselective deprotection of acetyl groups has been developed via employing KMnO4 as an additive. This chemoselective deacetylation is amenable to a wide range of substrates, tolerating diverse and sensitive functional groups in carbohydrates, amino acids, natural products, heterocycles, and general scaffolds. The protocol is attractive because it uses an environmentally benign reagent system to perform quantitative and clean transformations under ambient conditions.A catalytic and practical approach for the selective removal of acetyl groups using various substrates bearing orthogonal moieties has been demonstrated under ambient conditions.The divergent protection–deprotection approach and extensive functional group manipulation continues to serve as an important chemical tool to access biologically potent molecules and complex natural products.1 In particular, the hydroxyl moieties and their derivatives are ubiquitous in natural products and recognized as renowned scaffolds because of the overwhelming number of chemical and biological applications that they can be used in.2,3 The selective and orthogonal protection–deprotection of free hydroxyl group(s) are significant chemical transformations and frequently employed in target-oriented synthesis (TOS).4 Due to the widespread use and relative ease of protection–deprotection, introduction of an O-Ac group to mask the hydroxyl-moiety has remained as a highly reliable and convenient strategy, especially in synthetic carbohydrate chemistry.1–3 However, the chemoselective deprotection of O-Ac in the presence of analogous and sensitive O-protective groups such as benzoyl (Bz) or pivaloyl (Pv) is a notoriously challenging yet important task.1–3Thus, considerable effort has been devoted to developing robust and selective methods for the deprotection of the acetate ester. As outlined in Scheme 1, the cleavage of O-Ac is conventionally performed under a homogeneous reagent system including: (a) Brønsted acids/Lewis acids such as HCl/MeOH,5 HBF4·Et2O,6 BF3·Et2O,7p-TsOH or CSA,8 (b) inorganic/organic basic conditions employing Zemplén hydrolysis (NaOMe/MeOH),1 ammonia solution,9 hydrazine/AcOH/pyridine,10 DBU/PhH,11 guanidine/EtOH/DCM,12 Mg–metal or Mg(OMe)2,13 KCN/EtOH,14 K2CO3/MeOH/H2O,15 NaHCO3/H2O2,16 (c) metallic compounds or oxidants such as MoO2Cl2,17 molecular iodine/MeOH,18a Sm/I2,18b Bu2SnO/heating,19a Bu3SnOMe/DCE.19b Although, the use of heterogeneous catalysts such as CuFe2O4 nanoparticles20 and enzymes21 have also been demonstrated for deacetylation with limited substrate scope. Recently, a tetranuclear zinc cluster, Zn4(OCOCF3)6O has been investigated for use in trans-esterification and deacylation with discriminate selectivity.22Open in a separate windowScheme 1Previous advances, and the Me3SI-catalyzed chemoselective deacetylation developed in this work.Despite the synthetic challenges and demands placed on modern chemistry, advancing green chemical syntheses employing milder and environmentally benign reagent systems remains a constant motivation and is actively pursued. In this context and our continued interest23 developing versatile and selective protocols inspired the development of a simple and chemoselective deacetylation method with remarkable and distinctive synthetic applicability. Recently the dual-reactivity of KMnO4 for selective deacetylation and one-pot deacetylation–oxidation of benzyl-O-acetates under controlled reaction conditions was successfully investigated.23aEmerging from these precedents, the Me3SI-catalyzed, simple and chemoselective removal of O-acetate, an elegant and promising alternative approach for the deprotection of the acetate ester (Scheme 1d) is presented herein. Inspired by recent research,23f an initial experiment employing Me3SI(OAc)2, generated in situ oxidative transfer of the acetyl groups from PhI(OAc)2 to Me3SI, which gave the regioselective 2-iodoglycosylation of enol ether functionality in 3,4,6-tri-O-acetyl-d-glucal (1a) with methanol together with traces of the deacetylated product 1 (23f,g Meanwhile, the reaction using 0.2 equiv. of both Me3SI and NaIO4 was found to suffice for obtaining the complete deacetylation of 1a after 40 min ( Entry Catalyst (equiv.) Additive (equiv.) Solvent Time Yieldb 1 Me3SI (1.0) PhI(OAc)2 (1.0) MeOH 24 h Trace 2 Me3SI (1.0) NaIO4 (1.0) MeOH 10 min 100% 3 Me3SI (0.4) NaIO4 (0.4) MeOH 30 min 100% 4 Me3SI (0.2) NaIO4 (0.2) MeOH 40 min 100% 5 Me3SI (0.1) NaIO4 (0.1) MeOH 12 h 95% 6 n-Bu4NI (0.1) NaIO4 (0.1) MeOH 12 h 90% 7 KI (0.1) NaIO4 (0.1) MeOH 12 h 50% 8 NaI (0.1) NaIO4 (0.1) MeOH 16 h 90% 9c Me3SOI (0.1) NaIO4 (0.1) MeOH 12 h NR 10c Me3SBr (0.1) NaIO4 (0.1) MeOH 12 h NR 11c n-Bu4NBr (0.1) NaIO4 (0.1) MeOH 12 h NR 12c KBr (0.1) NaIO4 (0.1) MeOH 12 h NR 13 Me 3 SI (0.1) KMnO 4 (0.1) MeOH 5 min 100% 14 Me3SI (0.1) KMnO4 (0.1) MeCN 24 h NR 15 Me3SI (0.1) KMnO4 (0.1) Toluene 24 h NR 16 Me3SI (0.1) KMnO4 (0.1) THF 24 h NR 17 Me3SI (0.1) KMnO4 (0.1) DCM 24 h NR 18 Me3SI (0.1) K2S2O8 (0.1) MeOH 12 h Trace 19 Me3SI (0.1) Oxone (0.1) MeOH 12 h Trace 20 Me3SI (0.1) KBrO3 (0.1) MeOH 12 h Trace 21 Me3SI (0.1) NaBO3·H2O (0.1) MeOH 12 h 40% 22 Me3SI (0.1) Na3BO3 (0.1) MeOH 12 h Trace