7471-33-2Relevant academic research and scientific papers
Synthesis, crystal structure, and characterization of dimeric tetraorganodistannoxane and two tricyclohexyltin carboxylates
Sakho, Adama Moussa,Du, Dafeng,Li, Wenjie,Liu, Shuangshuang,Zhu, Dongsheng,Xu, Lin
, p. 2317 - 2327 (2010)
Three diorganotin(IV) series and triorganotin(IV) complexes, [(C 6H11)2Sn]4(L1)2O 2(OH)2 (1), (C6H11) 3Sn(HL2) (2), and (C6H11) 3SnL3 (3) (where HL1 is 2-(4-isopropyl benzoyl) benzoic acid, H 2L2 is phthalic acid and HL3 is 2-benzoyl benzoic acid), were synthesized and their crystal structures were determined. There are four crystallographically unique Sn centers in the structure of 1, which consists of a Sn4O2(OH)2 ladder unit, and the ladder consists of four tins held together by two 3-oxygens and two 2-oxygens. The supermolecular motif of 1 is a 2-D structure linked by O-H O hydrogen bonds. The asymmetric unit of 2 contains two crystallographically independent monomers. The supramolecular architecture of 2 is a 2-D layer structure linked by face-to-face - interactions between phenyl rings of adjacent L2 anions. The structure of 3 contains one tricyclohexyltin cation and one L3 anion. The Sn O interactions lead the whole structure to a supramolecular chain. Elemental analysis, infrared, and 1H NMR of 1-3 were investigated and discussed.
Phthalazines and phthalazine hybrids as antimicrobial agents: Synthesis and biological evaluation
Mourad, Asmaa Kamal,Makhlouf, Abdelmoneim Abdelsalam,Soliman, Ahmed Yousef,Mohamed, Samar Ahmed
, p. 31 - 41 (2019/11/14)
Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. Herein, a benzoic acid derivative (2), a benzoxazin-1-one derivative (3), and an oxophthalazin-2(1H)-yl)acetohydrazide (13) are utilized as precursors to construct a novel series of phthalazinones bearing various valuable functional groups in excellent yields via several simple and promising approaches. Finally, the antimicrobial activity of the newly synthesized phthalazines is screened against different microbial strains; namely, Gram-negative and Gram-positive bacteria utilizing Amoxicillin as a standard drug.
Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents
Hameed, Alhamzah Dh.,Ovais, Syed,Yaseen, Raed,Rathore, Pooja,Samim, Mohammed,Singh, Surender,Sharma, Kalicharan,Akhtar, Mymona,Javed, Kalim
, p. 150 - 159 (2016/02/09)
The chemistry of phthalazine derivatives has been of increasing interest since many of these compounds have found many chemotherapeutic applications. So this study aims to synthesize a library of phthalazine derivatives and to investigate their anti-inflammatory and anti-proliferative activities. Sixteen new phthalazinone derivatives (2a-p) were synthesized and tested for their in vitro antiproliferative and in vivo anti-inflammatory activities. All the synthesized compounds were identified and characterized by IR, 1H NMR, 13C NMR spectroscopy, and MS. Two compounds, 2b and 2i, showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib in the carrageenan-induced rat paw edema model at 3 and 5 h, respectively. Three compounds (2h, 2j, and 2g) showed moderate sensitivity toward the renal cancer cell line UO-31. A library of new phthalazone compounds (2a-p) was synthesized as dual inhibitors (COX-2/LOX-5) and evaluated for their anti-inflammatory, anticancer activities. Two compounds showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib, whereas three compounds showed moderate sensitivity toward the renal cancer cell line UO-31.
The discovery of 1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 1
Bond, Silas,Draffan, Alistair G.,Fenner, Jennifer E.,Lambert, John,Lim, Chin Yu,Lin, Bo,Luttick, Angela,Mitchell, Jeffrey P.,Morton, Craig J.,Nearn, Roland H.,Sanford, Vanessa,Stanislawski, Pauline C.,Tucker, Simon P.
, p. 969 - 975 (2015/02/19)
Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. Compound 1a (9b-(4-chlorophenyl)-1-(4-fluorobenzoyl)-1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-one) was identified as an inhibitor of A and B strains of RSV targeting the fusion glycoprotein. SAR was developed by systematic exploration of the phenyl (R1) and benzoyl (R2) groups. Furthermore, introduction of a nitrogen at the 8-position of the tricyclic core resulted in active analogues with improved properties (aqueous solubility, protein binding and log D) and excellent rat pharmacokinetics (e.g., rat oral bioavailability of 89% for compound 17).
A facile synthesis of new 3,3-disubstituted phthalides of pharmacological interest
Chamoli, Tanu,Rawat
, p. 453 - 465 (2013/03/14)
A series of new phthalides of pharmacological interest were synthesized by a protocol involving condensation of two γ-keto acids, 2-(4-isopropylbenzoyl)benzoic acid (1a) and 2-(4-isopropyl-3-nitrobenzoyl) benzoic acid (1b) with phenolic compounds in the presence of catalytic quantity of concentrated sulphuric acid. The method is simple, efficient, economical and environmentally benign as the reaction is carried out under solvent free condition attempting a green approach. Structural characterization of these newly synthesized compounds was accomplished by IR, UV, 1H NMR, 13C NMR, Mass spectral data, elemental analysis and chemical reactions. Some of the synthesized phthalides were found to exhibit antifungal and antibacterial activity against various human pathogenic bacterial and fungal strains.
Synthesis, crystal structure and biological activities of four novel tetranuclear di-organotin(IV) carboxylates
Kang, Wanli,Wu, Xiaoyan,Huang, Jianbin
experimental part, p. 2402 - 2408 (2009/09/30)
Four complexes: [Bu2(L1)SnOSn(L1)Bu2]2 (1), [Bu2(L2)SnOSn(L2)Bu2]2 (2), [Bu2(L3)SnOSn(L3)Bu2]2 (3), and [Bu2(L4)SnOSn(L4)Bu2]2 (4), (HL1 = 2-(4-methylbenzoyl)benzoic acid, HL2 = 2-(2,4-diethylbenzoyl)benzoic acid, HL3 = 2-(4-chlorobenzoyl)benzoic acid, HL4 = 2-(4-isopropylbenzoyl)benzoic acid) have been prepared and structurally characterized by means of elemental analysis and vibrational, 1H NMR and FT-IR spectroscopies. The crystal structures of all complexes have been determined by X-ray crystallography. Three distannoxane rings are present to the dimeric tetraorganodistannoxane of planar ladder arrangement. Each structure is centro-symmetric and features a central rhombus Sn2O2 unit with two additional tin atoms linked at the O atoms. Complex 1 exhibited good antibacterial and antitumor activities and have a potential to be used as drugs.
Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-imidazolyl)alkyl]- 1(2H)-phthalazinones
Yamaguchi,Kamei,Koga,Akima,Kuroki,Ohi
, p. 4052 - 4060 (2007/10/02)
A number of 4-substituted 2-[ω-(1-imidazolyl)alkyl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane A2 synthetase inhibitory and bronchodilatory activities. The pharmacological evaluation of these compounds disclosed that they have both activities to various extents. Both activities were slightly dependent on the length of the 2-substituents and largely affected by the nature of the 4-substituents. Compounds bearing phenyl and thienyl groups exhibited relatively high and well-rounded activities. Among these compounds, 12j and 15f were found to be the most effective agents having well-rounded activities in vitro and in vivo. Introduction of a carboxyl group reduced both activities contrary to our expectation. 4-(3-Pyridyl)phthalazinone 18b was of particular interest because of unexpectedly high in vivo activities in spite of an absence of significant in vitro activities.
