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"Telah dil p kukan uji teratogenisitas kiorpropamidapada mencit strain Biomedis, bertujuan untuk lebih dapatmeramalkan apakab kiorpropamida menyebabkan cacat bawaanpada manusia atau tidak. Dosis kiorpropamida yang diguriakanadalah 50 mg/kg BB, 200 mg/kg BB dan 400 mg/kg BB (lebihkurang setara dengan 5X, 20X dan 40X dosis lazim tertinggipada manusia), diberikan per oral melalul sondelambung. Dalam penelitian ml digunakan dua kelompok kon-.trol. Kelompok kontrol I tidak diberikan apa-apa kecualimakarian dan minuman ad libitum seperti halnya kelompok lainnya,sedangkan kelompok kontro]. II diberikan suspensiCNO (vehikel) 0,5%. Pemberian obat kepada kelompok keloladan suspensiCj kepada .kelompok' kontrol II dilakukan selama10 hari yaltu dari hari ke 6 sampal dengan 15 keharnilan.(selarna periode organogenesis). J1encit dimatikan pada harike 18 kehamilan dengan eter dan dilakukan histerektomi.- Pemeniksaan yang dilakukan : juml.ah fetus hidup dengan Cacatbawaan (eksternal dan internal termasuk cacat tulangrangka) yang dapat dilihat secara makroskopis dan jenisCacat bawaan yang terjadi, jumlah fetus hidup tanpa cacat,jumlah resorpsi dri fetus mati intrauterus. Juga dianalisakenaikari berat bp d.an mencit seisma kehamilan.Klorpropamlda dosis 50 mg/kg BB per hari tidk menunjukkanefek yang bermakna balk terhadap terjadinya Cacatbawaan (Fisher test), terhadap frekuensi resorpsi danfetus mati intrauterus (Chi-square test), maupun terhadapkenaikan berat badan induk mencit selama kehamilan (Testanalisa vanians satu arah dan student 't' test).Kiorpropamida dosis 200 mg/kg BB per . hari menunjukkanefek yang bermakna terhadap terjadinya cacat bawaan(Fisher test), tetapi tidak menunjukkan efek yang bermaknaterhada.p frekuensi resorpsl dam kematlan fetus intrauterus(Chi-square test) dan terhadap kenaikan berat badan indukmencit sela.ma kehmllan (Test analisa vanians satu arahdan student I t' test).Kiorpropamida dosis. 400 mg/kg BB per hari menunjukkanefek yang bermakna terhadap terjadlnya cacat bawaan(Fisher test), terhadap frekuensi resorpsi dan kematianfetus intrauterus (chi-square test) dan terhadap kenaikanberat badan induk mencit selama keharnhla.n (Test analisavanians satu srah dan student 't' test).Jenis cacat bawsan yang merupakan efek yang bermaknads.ri kiorpropamida adiah 'cleft palate' (Fisher test).

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The teratogenicity of chiorproparnide has been investigted

on Biomedis strain mice, in order to be able

to predict whether chiorpropamide causes congenital mall ormations

in man or not. The dosages of 50 mg/kg B.W., 200 mg/

kg B.W. and 400 mg/kg B.W. (equivalent to about 5, 20 9 and

40 times the higest usual dose in man) daily were used,,

They were given orally with a stomach tube. This investigation

had two control groups. The first one was given nothing

except diet given ad libitum and the second one was given

suspension of 0,5 % CMC. ChJorpropnmlde suspensions ind CMC

suspension were respectively given to treated groups of mice

and the second control group for 10 days i.e. on 6 to 15th

of gestation day (orgsnogenesis period). The animals were

sacrificed on 18th day of pregnancy by an over dose of ether.

The number of all living and intact, dead and resorbed, and

malformed fetuses (evaluated macroscopically), the kind of

malformations (external and internal malformations, including

skeletal defects) were observed and recorded. The weight

gain along the pregnancy were also analysed.

With dnily doses of 50 mg/kg B.W. , chlorpropimide

didn't show significant effects on the congenital anomalies

prevalence (Fisher test), the frequency of resorptions and

intrauterine deaths (Chi-square test) and the weight gain

along the pregnancy (Analysis of variance one way test and

Student 't' test).

With daily doses of 200 mg/kg B.W., chiorpropamide

showed significant effect on the congenital anomalies prevalence

(Fisher test), but it didn't show significant effect

on the frequency of resorptions and Intrauterine deaths

(Chi-square test) and the weight gain along the pregnancy

(Analysis of variance one way test and Student 't' test).

With daily doses of 400 mg/kg B.W., chiorpropamide

showed significant effects on the congenital anomalies prevalence

(Fisher test), the frequency of resorptions and intrauterine

deaths (Chi-square test) and the weight gain

along the pregnancy (Analysis of variance one way test and

Student I t' test).

The kind of congenital anomaly which was significant

effect of chiorpropamide was cleft palate (Fisher test)."

"Turunan 4(3H)-kuinazolin-4-on dilaporkan mempunyai aktivitas inhibisi COX-2 dan antiinflamasi. Sebagai upaya optimisasi aktivitasnya, pada penelitian ini, 32 senyawa 2,3-diaril-4(3H)-kuinazolinon tersubstitusi sulfonamida telah didisain dan diskrining secara virtual. Hasil studi menunjukkan bahwa senyawa turunan 2,3-diaril-4(3H)-kuinazolinon mempunyai gugus p-benzensulfonamida pada C-2 dan cincin fenil pada N-3 mempunyai afinitas pengikatan sepadan hingga lebih tinggi dibandingkan ligan acuan SC-558 dengan orientasi pose penambatan yang serupa. Atas dasar hasil tersebut, 4-[(E)-2-(4-Okso-3-fenilkuinazolin-2-il)etenil]benzensulfonamida dan lima analognya disintesis dan diuji aktivitas inhibisinya pada COX-1 dan COX-2 secara in vitro. Sintesis dilakukan melalui empat tahap. Tahap 1, sintesis 2-metil-3,1-benzoksazin-4-on dari asam antranilat. Tahap 2, sintesis 2-metil-3-fenil-4(3H)-kuinazolinon dan analognya dari 2-metil-3,1-benzoksazin-4-on dan anilin/anilin tersubstitusi. Tahap 3a, sintesis 4-sianobenzensulfonamida dari 4-aminobenzensulfonamida. Tahap 3b, sintesis 4-formilbenzensulfonamida dari 4-sianobenzensulfonamida. Tahap 4, sintesis 4-[(E)-2-(4-okso-3-fenilkuinazolin-2-il)etenil]benzensulfonamida dan analognya dari 2-metil-3-fenil-4(3H)-kuinazolinon/analognya dengan 4-formilbenzensulfon amida. Struktur senyawa hasil sintesis dikonfirmasi menggunakan spektra UV-Vis, FT-IR, 1H-NMR, 13C-NMR, HMQC, HMBC, LC-MS-ESI+ dan HRMS-ESI+ dan bioaktivitas diuji menggunakan kit uji skrining inhibitor COX. Hasil penelitian menunjukkan bahwa 4-[(E)-2-(4-okso-3-fenilkuinazolin-2-il)etenil]benzensulfonamida dan analognya (2a-f) berhasil disintesis, diperoleh murni dan struktur molekulnya sesuai dengan yang diharapkan. Senyawa 2a hanya aktif menginhibisi COX-1, senyawa 2e dan 2f hanya aktif menginhibisi COX-2, sedangkan senyawa 2b, 2c dan 2d aktif menginhibisi COX-1 dan COX-2. Hasil ini menunjukkan bahwa gugus fungsi pada posisi para N3-fenil meningkatkan aktivitas inhibisi senyawa tersebut pada COX-2. Senyawa 2d menunjukkan aktivitas inhibisi terbesar pada COX-1 (43,7% pada konsentrasi 100 μM), dan senyawa 2c menunjukkan aktivitas inhibisi terbesar pada COX-2 (47,1% pada konsentrasi 20 μM). Hasil studi pemodelan molekul menunjukkan bahwa adanya gugus fungsi pada posisi para cincin N3-fenil meningkatkan afinitas pengikatan pada COX-2 dan mendekatkan jarak antara oksigen karbonil 4(3H)-kuinazolinon dengan OH Ser530.

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Some of 4(3H)-quinazolinone detivatives reported to have COX-2 inhibition and anti-inflammatoy agent. As aims to optimize their activity, in this research, 32 sulfonamide-substituted 4(3H)-quinazolinone detivatives have been designed and screened virtually. The results show that 2,3-disubstituted-4(3H)-quinazolinones possessing p-benzenesulfonamide moiety at C-2 and phenyl ring at N-3 had equal to higher binding affinity than that of reference ligand SC-558 with similar docking orientation pose. Then, 4-[(E)-2-(4-Oxo-3-phenylquinazolin-2-yl)ethenyl]benzenesulfonamide and analogs were synthesized and evaluated their COX-1 and COX-2 inhibitory activity. The synthesize of titled compounds are performed via four steps. Step 1, synthesize 2-methyl-3,1-benzoxazin-one from antranilic acid. Step 2, synthesize 2-methyl-3-phenyl-4(3H)-quinazolinone and analogs from 2-methyl-3,1-benzoxazin-one and aniline/substituted aniline. Step 3a, synthesize 4-cyanobenzenesulfonamide from 4-aminobenzenesulfonamide. Step 3b, synthesize 4-formylbenzenesulfonamide from 4-cyanobenzene sulfonamide. Step 4, synthesize 4-[(E)-2-(4-oxo-3-phenylquinazolin-2-yl)ethenyl] benzenesulfonamide and analogs from 2-methyl-3-phenyl-4(3H)-quinazolinone/ analogs and 4-formylbenzenesulfonamide. Structures of the synthesized compounds were confirmed using UV-Vis, FT-IR, 1H-NMR, 13C-NMR, HMQC, HMBC, LC-MS-ES+ and HR-MS-ESI+ spectral data and their bioalogical activity were investigated using COX inhibitor screening assay kit. The results show that 4-[(E)-2-(4-oxo-3-phenylquinazolin-2-yl)ethenyl]benzenesulfonamide and analogs (2a-f) were succesfully synthesized, were sufficiently pure and structurally confirmed. Compound 2a inhibits only to the activity of COX-1, compound 2e and 2f inhibit only to the activity of COX-2 and compound 2b, 2c and 2d inhibit to the activity of COX-1 and COX-2. The results indicate that the substituent at para position of N3-phenyl of the compound enhances COX-2 inhibitory potency. Compound 2d shows the highest inhibition activity to COX-1 (43,7% at 100 μM concentration) and compound 2c shows the highest inhibition activity to COX-2 (47,1 % at 20 μM concentration). Results of molecular docking studies show that the presence of substituent at para position of N3-phenyl ring enhances the binding affinity toward COX-2 enzyme and brings the distance between O atom of carbonyl 4(3H)-quinazolinone closer to OH of Ser530."

"The determination of pseudoephedrine hydrochloride and triprolidine hydrochloride in influenza syrup medicine has been performed using TLC densitometric method. Pseudoephedrine hydrochloride and triprolidine hydrochloride were extracted using chloroform at pH 12 from the syrup, and separated using HPTLC silica Kieselguhr glass plates 60 F 254, 20x10 cm2 as stationary phase, and a mixture of methanol, ammonia and chloroform (40:2:30) as mobile phase. The plates were analyzed using Camag TLC Scanner 3 with UV-detector at 257 nm for pseudoephedrine hydrochloride and at 290 nm for triprolidine hydrochloride. The results showed that the linearity, limit of detection, and limit of quantitation of the method for pseudoephedrine hydrochloride were 0.9999, 0.0064 ìg, and 0.2124 ìg respectively; while for triprolidine hydrochloride were 0.9999, 0.0076 ìg, and 0.0254 ìg respectively. The coefficient of variance (CV) of repeatability for the two substances were less than 2.0%; and the recovery values for pseudoepherine hydrochloride and triprolidine hydrochloride were 99.98 + 1.05% and 99.73 + 1,54% respectively. The result showed that the samples analysed contained pseudoephedrine hydrochloride 94.36% of the labeled ammount, and triprolidine hydrochloride 94.44% of the labeled ammount."

"The determination of triprolidine hydrochloride and pseudoephedrine hydrochloride in anti influenza tablet has been performed using derivative spectrophotometry method. Triprolidine hydrochloride and pseudoephedrine hydrochloride were determined by measuring the first derivative ratio amplitudes, at 227,6 nm (zero crossing for pseudoephedrine hydrochloride) and at 230,0 nm (zero crossing for triprolidine hydrochloride) respectively. The linear calibration graphs were obtained for 5-50 ppm of triprolidine hydrochloride and for 100-800 ppm of pseudoephedrine hydrochloride. The results showed that the method is rapid, simple and can be applied successfully to assay simultaneously of two components in tablet preparation."

"As the food and beverages industry grows in Indonesia, there also has been an increase in the soft-drinks production in the society. There are elements often added into the drinks; such as caffeine, artifical sweetener and preservatives,which the content should be monitored. Because, if they are over-used, they will be hazardous to health. The purpose of this research is to obtain the optimum analysis condition for determining the content of saccharin, aspartame, benzoic acid, sorbic acid and caffeine, which are in the soft-drinks, using the reversed phase High-Performance-Liquid-Chromatography (HPLC). In this study, the condition used are Latek 18 column (15 cm x 4.0 mm), mobile phase as a mixture of acetonitrile and acetat buffer pH 5(5:95), flow rate 1,0 ml/minutes and detected by a 254 nm length-wave. The detection limit discovered by this method are for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,2 ppm; 0,2 ppm; 0,007 ppm; 0,142 ppm; and 6,5 ppm. Whereas, the quantitative limit for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,689 ppm; 0,852 ppm; 0,027 ppm; 0,452 ppm; 25,2 ppm. The calibration curve ranged between 1-60 ppm for saccharin and benzoid acid, 1-40 ppm for caffeine, 0.05-2 ppm for sorbic acid, and 30-100 ppm for aspartame. The investigation has been done for five (5) brands od soft-drinks. The analysis results are sample A contains caffeine 96,66 ppm, sample B contains saccharin 112,13 ppm, benzoic acid 206,81 ppm, and caffeine 130,63 ppm. Sample C contains benzoic acid 10,83 ppm and caffeine 97,66 ppm. Sample D contains benzoic acid 163,78 ppm, caffeine 101,52 ppm, and aspartame 231,20 ppm. The amounts of saccharin, benzoic acid, caffeine, and aspartame which has been found in the sample, do not exceed the tolerance limit of usage, whereas the amount of benzoic acid which has been found in sample B exceed the tolerance limit of usage."

"The objective of the study is to synthesize of 2-(phenylamino)methyl-2-nitro-4(3H)-quinazolinone and their derivatives under microwave irradiation. Solution of 2-bromomethyl-6-nitro-4(3H)-quinazolinone, aniline or subtituted aniline and pyridine was irradiated under modified home microwave completed with reflux condensor. The structure of the synthesized compounds were confirmed on the basis of IR, 1H-NMR and 13C-NMR data. The results showed that the reactions for 7 minutes in power level 30 to give corresponding 2-(phenylamino)methyl-2-nitro-4(3H)-quinazolinones in facile and good yield "