أن إحدى اكبر مشاكل الصحة العالمية هي ظهور مقاومة الميكروبية للأدوية الشائعة لذلك هناك حاجة ملحة لمضادات جرثومية جديدة ذات نشاط أحيائي معزز .في هذا الدراسة, تم تحضير خمسة مشتقات جديدة من الكينولين A,B,C,D وEكمضادات جرثومية. تم فحص بنية المركبات المحضرة باستخدام UV light , FTIR NMR . تم استخدام طريقة الانتشار بالحفر في الطبق لاختبار الخصائص المضادة للبكتريا للمركبات المحضرة في المختبر ضد نوعين من البكتريا الموجبة (المكورة العنقودية الذهبية و المكورة العقدية المقيحة ) ونوعين من البكتريا السالبة ( الكلبسيلة الرئوية والبكتريا الاشريكية القولونية). تم استخدام عقار السبروفلوكساسين كمضاد حيوي قياسي للمقارنة مع المركبات المحضرة. تم عرض أفضل نشاط بواسطة المركب C ضد البكتريا الاشريكية القولونية مع منطقة تثبيط تتراوح من 30مم و 33مم عند 250 و500 مايكرو غرام على التوالي .بينما يحتوي المركب B في المكورة العنقودية الذهبية على منطقة تثبيط عالية تتراوح تبلغ 42مم و 47 مم عند 250 و500 مايكرو غرام على التوالي. لكن المركب D في الكلبسيلة الرئوية على منطقة تثبيط عالية تبلغ 32مم و 35مم عند 250 و 500 على التوالي . بينما المركب Aفي المكورات العقدية المقيحة تبلغ منطقة التثبيط 45مم و47مم عند 250 و 500 مايكرو غرام على التوالي .
By condensation of benzaldehyde with thiourea in absolute ethanol in the presence of glacial acetic acid as a catalyst, the Schiff base(1-benzylidenethiourea)[I] was synthesized by synthesis of 4-(3-benzylidenethioureido)-4-thioxobut-2-enoic acid compound[II] by reaction of maleic anhydride with schiff base [I] in DMF. When treating compound [II] with ammonium persulfate (NH4)2S2O8 (APS) as an ethanol initiator to obtain polymer [III], compound [III] reacted to polymer [IV] with SOCl2 in benzene. Sulfamethizole, celecoxib, salbutamol, 4-aminoantipyrine to yield polymers [V-VIII], compound [IV] reaction with different drugs. Spectral evidence established the structure of synthesized compounds: FTIR an
This research included the preparation of 2-mercaptobenzoxazole (N1) by the reaction of ortho-aminophenol with carbon disulfide in an alcoholic potassium hydroxide solution. The 2-mercapto benzoxazole (N1) was then treated with hydrazine to obtain the 2-hydrazino benzoxazole (N2). A number of hydrazones (N3-N5) were prepared through the reaction of N2 with different benzaldehydes. The compound (N6) was also prepared whereby the ring closing of hydrazone (N3) using chloroacetylchloride, while the compound (N7) was prepared by treating 2-hydrazino benzoxazole with acetylacetone. When the compound (N1) was treated with formaldehyde, it afforded the compound (N8). Also, the N9 was obtained from the reaction of N1 with chloroacetic acid in th
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard
... Show MoreIbuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard compoun
... Show MoreIn search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.
Condensation of 1,2- dibromo ethane with para hydroxy benzoic acid gave 1,2-Ethane-bis- 4-oxybenzoic [1]. This Compound was converted with the thionyl chloride to give 1,2-Ethane-bis- 4-oxybenzoyl chloride [2]. Reaction of compound [2] with thiosemicarbizades gave 1,2-Ethanebis[4-oxybenzoyl-thiosemicarbazide] [3] and opteined 1,2-Ethane-bis[3-mercapto-5-phenoxy- 1,2,4-triazole] [4] from treatment compound [3] with NaOH (4%) .The new compounds 1,2- Ethane-bis[3-(substituted thioacyl)-4-(substituted acyl)-5 phenoxy-1,2,4-triazole] [5a-d] and 1,2- Ethane-bis[3-(substituted alkylthio)-5 phenoxy-1,2,4-trizole] [5e-f] derived from compound [4] were synthesized and characterized by physical and spectral data. All the compounds [4], [5a-d] and [5e-
... Show MoreThe Chemistry of heterocyclic sulphur and nitrogen containing compounds have a great role in the field of scientific studies, The 2-amino 5-mercapto-1,3,4-thiadiazole ring for instance, has gained more importance in recent years because they are considered as potent biologically active nucleus. In this study disulfide derivative can be obtained by oxidation with hydrogen peroxide of thiol group of the heterocyclic 2-amino 5-mercapto-1,3,4-thiadiazole ring to obtain compound (3) with expected antibacterial activity. In order to use it as a diazo component to prepare some new bis azo compounds as possible antibacterial agents, the reaction of two primary amino groups on both sides of disulfide dimer with sodium nitr
... Show MoreThe formation and structural investigation of three new Mannich bases are reported. The synthesis of these compounds was accomplished via a multicomponent one-pot reaction using CaCl2 as a catalyst. The reaction of the benzaldehyde, m-bromoaniline and cyclohexanone or 4-methylcyclohexanone resulted in the formation of L1 and L3, respectively. The synthesis of L2 was achieved by mixing benzaldehyde, o-bromoaniline and cyclohexanone. The isolated compounds were characterised using a range of analytical and spectroscopic techniques. These include; NMR (1H and 13C-NMR), ESMS, FTIR, electronic spectroscopy, microanalyses and melting points. The NMR data for L1 and L2 indicated the presence of one isomer in solutions, on the NMR time scale. How
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