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1.
Anatoliy P. Marchenko Georgiy N. Koidan Anastasiya S. Huryeva Radomyr V. Smaliy Aleksandr A. Yurchenko Aleksandr N. Kostyk 《Heteroatom Chemistry》2012,23(2):210-215
It was found that phosphinimidic isocyanates based on 3‐, 4‐, and 5‐aminopyrazoles could undergo intramolecular heterocyclization to yield previously unknown pyrazolo[1,3,2]diazaphosphorin‐4‐ones containing an endocyclic PN double bond. It was shown that phosphinimidic isocyanate based on 4‐aminopyrazole, in which there are two positions (3 and 5) available for the cyclization, reacts exclusively at the 5‐carbon atom. © 2012 Wiley Periodicals, Inc. Heteroatom Chem 23:210–215, 2012; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.21005 相似文献
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Liangnian He Yanping Luo Mingwu Ding Aihong Lu Xiaopeng Liu Tianjie Wu Fei Cai 《Heteroatom Chemistry》2001,12(6):497-500
Aromatic‐substituted derivatives of 1,3,2‐diazaphospholidin‐4‐ones 2a–g were readily prepared from 1,3‐diaryl glycinamides 1 by the reaction with hexaethylphosphoric triamide. Their chemical transformation was selectively effected with different thionation reagents to afford thionated products at the phosphorus atom to give 3a–g and at the carbonyl group to give 4a . An oxidation reaction at phosphorus to produce 5a was effected with 10% hydrogen peroxide. Preliminary bioassays revealed that some of the title compounds, 2a–g and 3a–g possess selective herbicidal activity against rape. © 2001 John Wiley & Sons, Inc. Heteroatom Chem 12:497–500, 2001 相似文献
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P. Haranath V. Sreedhar Kumar C. Suresh Reddy C. Naga Raju C. Devendranath Reddy 《Journal of heterocyclic chemistry》2007,44(2):369-373
Substituted benzoxazaphosphorin 2‐yl ureas were synthesized by reacting 2‐(4‐fluoro‐phenylamino)‐methylphenol (4) with different carbamidophosphoric acid dichlorides (3) in the presence of triethylamine in dry toluene at 45‐50 °C and characterized by spectral data. These compounds were found to possess good antimicrobial activity. 相似文献
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Ratnadeep S. Joshi Priyanka G. Mandhane Wajid Khan Charansingh H. Gill 《Journal of heterocyclic chemistry》2011,48(4):872-876
A new series of 2‐(p‐tolyloxy)‐3‐(5‐(pyridin‐4‐yl)‐1,3,4‐oxadiazol‐2‐yl)quinoline were synthesized from oxidative cyclization of N′‐((2‐(p‐tolyloxy)quinoline‐3‐yl)methylene)isonicotinohydrazide in DMSO/I2 at reflux condition for 3–4 h. The structures of the new compounds were confirmed by elemental analyses as well as IR, 1H‐NMR, and mass spectral data. All the synthesized compounds were screened for their antibacterial activities against various bacterial strains. Several of these compounds showed potential antibacterial activity. J. Heterocyclic Chem., (2011). 相似文献
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Anita Guesdon Alain Fogain‐Ninkam Bernard Decroix Pierre Netchitaïlo 《Journal of heterocyclic chemistry》2001,38(6):1441-1445
1‐(1,3‐Dioxo‐1,3‐dihydro‐2H‐isoindol‐2‐yl)‐1H‐pyrrol‐2 carbaldehyde 4 was synthesized by Vilsmeier‐Haack reaction from 2‐(pyrrol‐1‐yl) phthalimide. Reduction of 4 by sodium borohydride, or action of Grignard reagents on 4 led to the corresponding alcohols 5 which were cyclized to pyrroloxadiazino isoin‐doles 1 by heating in the presence of silica gel. Transformation of the hydroxylactam 6 with acetic acid derivatives led to the esters 7 which gave, after saponification, pyrroloxa(or thia)diazepinoisoindolones 2 by intramolecular cyclization. 相似文献
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Jordi Bols Teresa Loscertales Joan Nieto Aurelio Sacristn Jos A. Ortiz 《Journal of heterocyclic chemistry》2000,37(5):1203-1208
An efficient and versatile synthesis of variously substituted 3‐(hydroxymethyl)‐4H‐chromen‐4‐ones is reported. The compounds are prepared by hydroxymethylation of the precursor 2‐hydroxy‐4‐chromanones followed by acid dehydration. 相似文献
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Design and Synthesis of Novel 3‐(Phenyl)‐2‐(3‐substituted propylthio) Quinazolin‐4‐(3H)‐ones as a New Class of H1‐Antihistaminic Agents 下载免费PDF全文
A series of novel 3‐(phenyl)‐2‐(3‐substituted propylthio) quinazolin‐4‐(3H)‐ones were synthesized by the reaction of 2‐(3‐bromopropylthio)‐3‐(phenyl) quinazolin‐4‐(3H)‐one with various amines. The starting material, 2‐(3‐bromopropylthio)‐3‐(phenyl) quinazolin‐4‐(3H)‐one was synthesized from aniline. When tested for their in vivo H1‐antihistaminic activity on conscious guinea pigs, all the test compounds protected the animals from histamine‐induced bronchospasm significantly. Compound 2‐(3‐(4‐methylpiperazin‐1‐yl) propylthiothio)‐3‐(phenyl) quinazolin‐4(3H)‐one ( Ph5 ) emerged as the most active compound (73.23% protection) of the series when compared with the reference standard chlorpheniramine maleate (70.09% protection). Compound Ph5 shows negligible sedation (5.01 %) compared with chlorpheniramine maleate (29.58%). Therefore, compound Ph5 can serve as the leading molecule for further development into a new class of H1‐antihistaminic agents. 相似文献
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Heung‐Seop Yim Mi‐Ra Kim Gi‐Hyeon Sung Hyun‐A Chung Jin‐Kook Lee Sang‐Gyeong Lee Yong‐Jin Yoon 《Journal of heterocyclic chemistry》2008,45(1):215-220
trans‐2‐(2‐Aryl‐ or heteroarylvinyl)‐4,5‐dichloropyridazin‐3(2H)‐ones 3 were synthesized from 4,5‐dichloropyridazin‐3(2H)‐one via 2 step. The photochemical behavior of 3 in THF, methylene chloride, acetonitrile and methanol is dependent on the kind of aryl or heterocyclic ring and the solvent polarity 相似文献
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Himani N. Chopde Ramakanth Pagadala Jyotsna S. Meshram Venkateshwarlu Jetti 《Journal of heterocyclic chemistry》2011,48(6):1323-1328
5‐((3‐Aminophenyl)diazenyl)quinolin‐8‐ol ( 1 ) was synthesized by diazotization reaction and coupled with 8‐hydroxyquinoline moiety. This amine on facile condensation with aromatic aldehydes in presence of glacial acetic acid and ethanol affords anils ( 2 ). These anils on cyclocondensation reaction with thioglycolic acid (i.e., mercaptoacetic acid) yield the titled compound ( 3 ). The structure of the newly synthesized anils ( 2 ) and thiazolidinones ( 3 ) has been confirmed by elemental analysis and spectral analysis. The titled compounds have been screened against different bacterial and fungal strains. J. Heterocyclic Chem., (2011). 相似文献
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Ch. Sanjeeva Reddy M. Vani Devi G. Rajesh Kumar L. Sanjeeva Rao A. Nagaraj 《Journal of heterocyclic chemistry》2011,48(1):176-182
A series of novel 2‐(aryl)‐3‐[5‐(2‐oxo‐2H‐3‐chromenyl)‐1,3‐oxazol‐2‐yl]‐1,3‐thiazolan‐4‐ones 4a , 4b , 4c , 4e , 4f , 4g , 4h , 4i , 4j have been synthesized and assayed for their antibacterial activity against Gram‐positive bacteria viz. Bacillus subtilis (ATCC 6633), Staphylococcus aureus (ATCC 6538p), Micrococcus luteus (IFC 12708), and Gram‐negative bacteria viz. Proteus vulgaris (ATCC 3851), Salmonella typhimurium (ATCC 14028), Escherichia coli (ATCC 25922), and also antifungal activity against Candida albicans (ATCC 10231), Aspergillus fumigatus (HIC 6094), Trichophyton rubrum (IFO 9185), and Trichophyton mentagrophytes (IFO 40996). Among the screened compounds, 4d , 4e , 4f , 4g , and 4j exhibited potent inhibitory activity compared with the standard drug at the tested concentrations. The results reveal that, the presence of difluorophenyl in 4f and pipernyl ring in 4j at 2‐position of thiazolidine‐4‐one ring show significant inhibitory activity. The other compounds also showed appreciable activity against the test bacteria and fungi and emerged as potential molecules for further development. J. Heterocyclic Chem., 2011. 相似文献
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Domenico Armenise Nicolino De Laurentis Antonio Rosato Flaviano Morlacchi 《Journal of heterocyclic chemistry》2006,43(5):1371-1378
A series of 2‐(acyl or carboxyalkyl)‐3‐(H or alkyl or aryl)‐5 (or ‐6 or ‐8)‐monochloro, 7‐fluoro‐substituted‐4H‐1,4‐benzothiazines 3a‐x were prepared to investigate their potential biological activity. In this work the 3a‐w structures are supported with physical and analytical data and the results of their in vitro antimicrobial activity against some strains Gram positive, Gram negative, and Fungi are reported. It was found that compounds 3a, 3d displayed interesting antibacterial activity, whereas compound 3f displayed interesting antifungal activity. 相似文献
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Anatolii E. Shipov Mikhail V. Makarov Pavel V. Petrovskii Ekaterina Yu. Rybalkina Yulia V. Nelyubina Irina L. Odinets 《Heteroatom Chemistry》2013,24(3):191-199
Two novel series of phosphorus‐substituted 3,5‐bis(arylidene)piperid‐4‐ones bearing 1,3,2‐oxazaphosphorinane cycle either directly attached to the piperidone core through the P N bond (diamidophosphates 4 ) or connected with it via thiocarbamoyl linker (thioureas 5 ) were obtained by the phosphorylation of NH precursors with 2‐oxo‐1,3,2‐oxazaphosphorinane chloride or the reaction of the former ones with the corresponding cyclic isothiocyanate. According to the results of cytotoxicity screening against human carcinoma cell lines (A549, CaOv3, KB), thioureas 5 were more active than the diamidophosphates 4 bearing the same arylidene rings, with compounds with electron‐withdrawing side groups displaying IC50 in the micromolar range of 1.2–7 μM. © 2013 Wiley Periodicals, Inc. Heteroatom Chem 24:191–199, 2013; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.21082 相似文献
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Qing‐You Zhang Li‐Zhuang Xu Jing‐Ya Li Dan‐Dan Zhang Hai‐Lin Long Ji‐Yan Leng Lu Xu 《Journal of Chemometrics》2012,26(10):497-508
Chiral compounds are very important in drug development, organic synthesis, materials science, toxicology, or environmental chemistry. Therefore, for creating new drugs, several methods have been suggested in recent years. In several laboratories in the world, some new methods for the derivations of the parameters were constructed and used for studies on quantitative structure–activity/property relationships of chiral molecules. The algorithms reviewed in this paper involve Zargeb group chiral indices, chiral molecular connectivity index, chiral topological charge index, chiral Am index, chiral indices based on the matrixes, chiral indices based on chiral product, conformation‐independent chirality code, conformation‐dependent chirality code, quantitative two‐dimensional chirality degrees of benzenoids, and so on. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
17.
Wei‐Min Liu You‐Quan Zhu Yi‐Feng Wang Bin Liu Xiao‐Mao Zou Hua‐Zheng Yang 《Journal of heterocyclic chemistry》2007,44(4):967-971
A series of 2‐(3‐(trifluoromethyl)‐5‐(alkoxy)‐1H‐pyrazol‐1‐yl)‐4‐aryloxypyrimidine derivatives were designed and synthesized. The structures of all the title compounds were confirmed by 1H NMR and elementary analysis. These compounds were screened for herbicidal activity against rape and barnyard grass. Compound B13 exhibited moderate herbicidal activity. 相似文献
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Vahuni Karapetyan Satenik Mkrtchyan Gnuni Karapetyan Alexander Villinger Ashot Saghiyan Tariel V. Ghochikyan Peter Langer 《Helvetica chimica acta》2011,94(11):2045-2053
(Benzyloxycarbonyl)‐protected 3,4‐benzo‐7‐hydroxy‐2,9‐diazabicyclo[3.3.1]non‐7‐enes were prepared by one‐pot cyclizations of 1,3‐bis(silyl enol ethers) with quinazolines. Subsequent hydrogenation resulted in one‐pot deprotection and rearrangement to give 2‐(2‐aminophenyl)‐2,3‐dihydropyridin‐4(1H)‐ones. 相似文献
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A series of novel 3‐((4‐(t‐butyl)‐2‐(2‐benzylidenehydrazinyl)thiazol‐5‐yl)methyl)quinolin‐2(1H)‐ones ( 7a – 7z ) were designed, synthesized and evaluated for their ability of inhibiting neuraminidase (NA) of in?uenza H1N1 virus. Some compounds displayed moderate influenza NA inhibitory activity. Compound 7l with the scaffold of 2‐(2‐(2‐methoxybenzylidene)hydrazinyl)thiazole was the best one, exhibiting moderate NA inhibitory activity with IC50 of 44.66 µmol/L. Structure‐activity relationship showed that compounds with methoxy or hydroxy groups at the ortho position, fluorine and nitro groups at the meta position and chlorine and bromine groups at the para position of phenyl ring were more active. Docking study indicated that compound 7l has important interactions with some key residues (including Asp151, Glu119, Arg292, Tyr406, and Asn347) and binds to 430‐cavity adjacent to NA active site. 相似文献
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Vikas Shinde Pravin C. Mhaske Aakriti Singh Dhiman Sarkar Pramod Mahulikar 《Journal of heterocyclic chemistry》2019,56(11):3093-3101
A novel series of 4‐(4‐(1‐benzyl‐1H‐1,2,3‐triazol‐4‐yl)phenyl)‐2‐substitutedthiazole derivatives ( 8a‐l) have been synthesized by [3 + 2] cycloaddition reaction of 4‐(4‐ethynylphenyl)‐2‐substitutedthiazole with substituted benzyl azide in aqueous DMF. Starting compounds 4‐(4‐ethynylphenyl)‐2‐substitutedthiazole ( 6a‐d ) were synthesized by reaction of 4‐(2‐substitutedthiazol‐4‐yl)benzaldehyde with Ohira‐Bestmann reagent in methanol. The structures of these novel triazole‐thiazole clubbed derivatives were confirmed by the spectral analysis. The title compounds ( 8a‐l ) were tested for antimycobacterial activity against Mycobacterium tuberculosis H37Ra active and dormant (MTB, ATCC 25177) and antimicrobial activity against standard Gram‐positive bacteria, Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162), and Gram‐negative bacteria, Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059). Compounds 8a , 8b , 8c , and 8h reported good activity against B subtilis, compounds 8a , 8b , and 8c showed good activity against S aureus, and compound 8b showed good activity against dormant M tuberculosis H37Rv strain. Compounds 8b and 8c found more potent against Gram positive and dormant M tuberculosis H37Rv strains. These novel triazole‐thiazole clubbed analogues found to be a capable leads for further optimization and development. 相似文献