Synthesis, anti-HIV activity and molecular modeling study of some new pyrimidine analogues

A new series of 2,6-diamino-5-arylazo-4-chloropyrimidine analogues (6-13) were synthesized from the pyrimidine scaffold 5, via diazotization with various amines. Nucleophilic displacement of compound 5 by ethanethiolate or arylthio nucleophiles, afforded the 4-alkylthio analogues (14-16). Treatment of compound 17 or 18 with thiourea under MWI gave the 4-thione derivatives 19 and 20, respectively. On treatment of compound 20 with 2-mercaptoacetic acid furnished the 4-thio analogue (21). Reaction of compound 19 or 20 with sodium hypochlorite followed by ammonium hydroxide afforded the 4-aminothio analogues 22 and 23, respectively. Oxidation of compound 23 with H2O2 led to the 4-sulphonamide derivative 24. All new compounds were evaluated for their in vitro antiviral activity against the replication of HIV-1 and HIV-2 in MT-4 cells. Compounds 14-16 and 21 showed an EC50 values of > 2.12, 1.99, 1.80 and 1.92 μg/mL, respectively. In addition, preliminary structure-activity relationship and molecular modeling of compound 15 has been studied

Synthesis, antimicrobial activity, computational and modeling studies of some new organotellurium compounds containing azo moities

A new series of organonotellurium compounds containing azo groups were prepared by new and convenient methods. Reaction of 1-(4-mercuric chloride-2,3-dichlorophenyl)-2-chloro diazine (4) with 8-hydroxyquinoline (5) gave the new organomercury compound 6 in good yield. Telluratio of compound 6 with tellurium tetrabromide in 1:1 and 1:2 mole ratio gave the o-tellurated azo compounds ArTeBr3 (7) and Ar2TeBr2 (9), respectively. Reduction of both ArTeBr3 and Ar2TeBr2 by hydrazine hydrate gave the ditelluride 8, and telluride 10, respectively. The synthesized compounds were screened for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Klebsiella pneumonia, Salmonella spp., Streptococcus spp. and Bacillus cereus. Additionally, the prepared compounds were tested for antifungal activity against Candida sp., Aspergillus multi and Aspergillus niger. All compounds exhibited good antibacterial and antifungal activity. Computational study of the new compounds was calculated using Gaussian 09 program package. Molecular modeling studies were performed and showed hydrogen binding and hydrophobic interactions

Molecular Detection of β-Giardin Gene of Giardia lamblia in Peptic Ulcer Patient in Babylon Province

الخلفية: الجيارديا اللامبليا واحدة من اكثر الطفيليات المعوية للانسان انتشارا فهي عالمية الانتشار وبشكل وبائي في جميع انحاء العالم مع مجموعة واسعة من المضائف الثدية. الهدف: الكشف الجزيئي لجين بيتا-جياردين في مرضى القرحة الهضمية للتحقق من وجود علاقة بين الاصابة بالجيارديا اللامبليا مع بكتريا الملوية البوابية. طرائق العمل: ما مجموعة 64 عينه براز جمعت من مرضى القرحة الهضمية المراجعين لوحدة الناضور الداخلي (مستشفى مرجان التخصصي لامراض القلب والباطنية في محافظة بابل),ممن لديهم اعراض القرحة الهضمية. اجري تفاعل البلمرة المتسلسل باستخدام البادئ المستهدف للبيتا- جياردين جين(218pb)   للجيارديا اللامبليا. النتائج: في هذه الدراسة تم جمع 64 عينه براز من مرضى القرحة الهضمية، تم العثور على الاصابة بالجيارديا اللامبلية  في (%18.7 ) 12 باستخدام الفحص المباشر لعينه البراز.في حين 21(32.8%) عينه كانت موجبة للجيارديا اللامبيليا عند استخدام تفاعل البلمرة المتسلسل للكشف عن جين البيتا جياردين. كما ان نسبة الاصابة بالجيارديا لامبليا في الذكور كانت اعلى معنويا(p <0.05)   من الاناث، واكثر الاعراض شيوعا هي الحرقة بنسبة 15.6 % ، اسهال بنسبة 9.3 % تلتها الام في البطن بنسبة 7.8%. الاستنتاج: من نتائج هذه الدراسة نستنتج ان نسبة الاصابة بالجيارديا اللامبيليا عالية في مرضى القرحة الهضمية. للكشف عن القرحة الهضمية ينبغي الاخذ بنظر الاعتبار الاصابة بالجيارديا اللامبليا كعامل مسبب للقرحة الهضمية وهذه الطريقة مفيدة في تشخيص وعلاج القرحة.background: Giardia lamblia is one of the  commonest human intestinal protozoa, it cosmopolitan  and is endemic throughout the world with a wide range of mammalian hosts. Objective: This object aimed to focus on molecular detection of β-Giarin gene of Giardia lamblia  in patient with peptic ulcer to investigate an association between Giardia lamblia and Helicobacter pylori infection.   Methods: a total of 64 stool sample were collected from patients  attending to endoscopy unit (specialized Marjan Hospital for Internal and Cardiac Diseases   in Babyoln province) for their peptic ulcer symptoms And were positive for H. pylori.  Polymerase chain reaction was achived by primers that targeted the (β-Giardin) gene (218pb) of Giardia lamblia. Results: in this study 64 stool sample were collected from patients with peptic ulcer,  Giardia lamblia infection was found in 12 (18.7%)  according to direct examination of stool sample, while 21 (32.8%) was positive to giardiasis when used PCR for detection of β-Giardin gene (218pb) ,also the percentage of infection in  male was significantly (p <0.05)  higher than female with giardiasis infection isolated from peptic ulcer patients and the most frequent symptom was  heartburn (15.6%) and diarrhea ( 9.3%), followed by abdominal pain (7.8%).   Conclusion: from the results of this study we conclude that Giardia lamblia is high in patients with peptic ulcer. To investigate the causes of peptic ulcer, it should be considered the Giardia lamblia infection as an etiologic factor. This approach will be useful in diagnosis and management of peptic ulce

Synthesis, antimicrobial activity and molecular modeling study of some new pyrimidine derivatives

Condensation of 2-amino-4-chloro-6-methoxypyrimidine with aromatic aldehydes (2-hydroxy-1-naphthaldehyde, 3,4-dihydroxybenzaldehyde and piperonal) afforded products in good yields. The synthesized compounds (Schiff base of pyrimidine derivatives) were screened for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Klebsille, Pseudomonas aeruginosa and Salmonella. Additionally, the compounds were tested for antifungicidal activity against Candida albicans, Candida tropicalis and Aspergillus fumigatus. All compounds exhibited potent antibacterial and antifungal activity. Molecular modeling studies were performed, showing the hydrogen bindings and hydrophobic interactions

Derivati aminokiselina. Dio 1. Sinteza, antivirusno i antitumorsko djelovanje novih estera alfa-aminokiselina s kumarinskim supstituentom

A series of amino acid esters bearing coumarin (3-15) were synthesized and evaluated, in vitro, against HIV-1, and bovine viral diarrhea virus (BVDV). The in vitro cytotoxicity of 3-10 and 12 were assyed against a panel of tumor cell lines consisting of CD4 human T-cells. Compound 14 showed inhibition of HIV-1 with EC50 > 1.6 microg mL-1, meanewhile compound 9 exhibited activity against leukaemia (MT4) with CC50 = 24 micromol L-1).U radu je opisana sinteza estera aminokiselina s kumarinskim ostatkom 3-15. Ispitano je antivirusno djelovanje sintetiziranih spojeva na HIV-1 i goveđi virus diareje (BVDV) te in vitro citotoksičnost spojeva 3-10 i 12 na tumorskim linijama CD4 humanih T-stanica. Spoj 14 pokazao je inhibiciju HIV-1 s EC50 > 1.6 microg mL-1, dok je spoj 9 djelotvoran na leukemiju (MT4) s CC50 = 24 micromol L-1

Spectroscopic Study of some Schiff Bases Derived from Dibenzoylmethane

A series of Schiff bases 7-11 derived from dibenzoylmethane have been prepared. The UV, IR, 1H NMR and mass spectra revealed theses compounds were existed mainly as the keto-enamine tautomer in the solution. The absorption bands which appeared in the range λmax = 376-406 nm were assigned to the electronic transitions which arised from the central hydrogen bonded chelated unsaturated ring system in this tautomer. The appearance of the broad singlet near d  = 13 ppm due to the N-H proton and a singlet near d  = 6 ppm due to the –C=C-H proton inaddition to benzoyl fragment ion     signal m/z =105 in the mass spectra supported the above suggested products

Computational study and antimicrobial activity of few Dapsone Schiff base derivatives

Condensation of 4,4-diaminodiphenyl sulfone (Dapsone) with aliphatic and aromatic aldehydes yielded a few Schiff base derivatives in good yields. The optimized structural parameters (bond lengths and bond angles) of three azomethine compounds have been obtained by using the GAUSSIAN 09 program package. Conformer of compound 1 has the highest energy, which has less stability than compounds 2 and 3 at the same model. The synthesized compounds were screened for antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis and fungicidal activity against Aspergillus niger and Candida albicans. All compounds exhibited potent antibacterial and antifungal activity with the reference standard ciprofloxacin and Amphotericin B, respectively

Synthesis, characterization and acute toxicity of new Schiff base derived from L-arginine and vanillin

Condensation of L-arginine with 4-hydroxy-3-methoxy benzaldehyde (vanillin) yielded a novel Schiff base derivative of arginine in good yield. This new Schiff base was characterized by elemental analysis, IR and 1H NMR spectroscopy. The toxicity of the compound was also assayed via the determination of their LD50 value by using Dixon method. Studied compound was found to have an LD50 of 718.6 mg/kg of body weight