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

Nitroimidazoli. V. Sinteza i anti-HIV djelovanje novih 5-supstituiranih piperazinil-4-nitroimidazol derivata

A series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin-1-yl]ethanones (3-9) and alkyl-[4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin-1-yl)ketones (11-20) as well as the indole analogue 22 were synthesized from 4-nitro-5-piperazinyl imidazole derivative 1, with the aim to develop new non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound 4 showed inhibition of HIV-1 (EC50 0.45 µg mL1) and HIV-2 (0.50 µg mL1), while 11 showed inhibition of HIV-1 (EC50 2.48 µg mL1, SI = 4).Iz 4-nitro-5-piperazinil derivata imidazola 1 sintetizirana je serija 2-alkiltio-1-[4-(1-benzil-2-etil-4-nitro-1H-imidazol-5-il)-piperazin-1-il]etanona (3-9) i alkil-[4-(1-benzil-2-etil-4-nitro-1H-imidazol-5-il)-piperazin-1-il)ketona (11-20) te indol analog 22, s ciljem da se razviju novi nenukleozidni inhibitori reverzne transkriptaze (NNRTIs). Novosintetiziranim spojevima ispitano je djelovanje na HIV-1 i HIV-2 u MT-4 stanicama. Spoj 4 pokazao je značajno djelovanje na HIV-1 (EC50 0,45 µg mL1) i HIV-2 (0,50 µg m-1), a spoj 11 na HIV-1 (EC50 2.48 µg mL-1, SI = 4)

Antibacterial Activity of Some Selected 1,2,4-Triazole Derivatives Against Standard, Environmental, and Medical Bacterial Strains

Abstract Recently, four heterocyclic compounds containing 1,2,4-triazole (designated as Y2, Y3, Y30, and Y32) were synthesized by our lab. Previous data showed that 1,2,4-triazole nucleus posses a wide range of pharmacological activities such as antioxidant, antiviral, antitumor and antibacterial activities. Currently, the need for triazole derivatives with a broad spectrum of antibacterial activity are in the rise. Therefore, these data encouraged us to test newly synthesized 1,2,4-triazole compounds for their antibacterial activity against three types of bacteria: standard, environmental and medical bacteria. Both well diffusion and broth dilution methods were employed to examine the potential antibacterial activity against the aforementioned types of bacteria. The standard bacteria include Staphylococcus aureus ATCC 29213, Staphylococcus epidermis ATCC 12228, and Bacillus 292 Jacob H. Jacob et al. cereus ATCC11778, whereas environmental bacteria include Citrobacter sp., Bacillus pumilis, and Yersinia enterocolitica. The medical bacteria consists of three pathogenic bacteria (assigned as CS1, CS2, and CS3) isolated from medical samples obtained from a local hospital. These strains were further identified by means of biochemical tests and 16S rDNA sequencing. Based on these analyses, the CS1, CS2, and CS3 strains were Escherichia coli, Shigella sonnei and Pseudomonas aeruginosa, respectively. Data revealed that the compound Y2 and Y3 were effective against all tested bacterial strains except E. coli. Interestingly, compound Y3 was found to have antibacterial activity higher than penicillin G (the positive control) against P. aeruginosa and similar to penicillin G against B. cereus. However, the compounds Y30 and Y32 has no recognizable antibacterial effect. The antibacterial activity of Y2 and Y3 was appeared to be attributed to the type and the position of substituent groups

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

A new class of dihaloquinolones bearing N'-aldehydoglycosylhydrazides, mercapto-1,2,4-triazole, oxadiazoline and a-amino ester precursors: synthesis and antimicrobial activity

Reaction of the quinolones 6-8 with hydrazine afforded the hydrazide 9-11 in moderate yields. Condensation of 9 and 11 with CS2 /KOH furnished the potassium salts 13 and 14, respectively, which spontaneously afforded the 3-(1,2,4-triazolyl)-quinolones 15 and 16, respectively, on treatment with hydrazine. Reaction of 9 in refluxing CS2 /KOH gave the 3-(1,2,4-oxadiazolyl)-quinolone 17. Alternatively, 15 was prepared from 17. The azide derivative 12, obtained from 10, furnished the a-amino ester derivative 18, on reaction with the glycine ethyl ester. Coupling of 10 with various sugars gave the N'-aldehydoglycosyl-quinolone-3-yl)carbohydrazides 19a-e. The newly synthesized compounds were screened for their antibacterial activity

Synthesis and biological evaluation of new benzothiazoles as antimicrobial agents

A new series of hydrazide derivatives were synthesized, characterized, and biologically evaluated. The reaction of 2-chloro benzo[d]thiazole 1, with ethyl 2-(piperazin-1-yl) acetate 2, led to the formation of ethyl 2-(4-(benzo[d]thiazol-2-yl)piperazin-1-yl)acetate 3. The reaction of compound 3 with excess amount of hydrazine hydrate gave 2-(4-(benzo[d]thiazol-2-yl) piperazin-1-yl) acetohydrazide 4. Hydrazide derivatives 5(a–j) were prepared by the reaction of compound 4 with the appropriate acid chloride. The in vitro antibacterial activity of compounds 3, 4, 5a, and 5b were screened against Staphylococcus aureus, Escherichia coli, and Candida albicans bacteria, no activity has been witnessed

Nitroimidazoles, Part 3. Synthesis and anti-HIV Activity of New N-Alkyl-4-nitroimidazoles Bearing Benzothiazole and Benzoxazole Backbones

A series of 4-nitroimidazole derivatives bearing substituted piperazines (5, 8, 9, 12, 14, 16, 17, and 19 -21) were synthesized with the aim to develop new non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. All compounds are inactive, except compound 21 which showed inhibition of HIV-1 with EC 50 0.20 µg/mL, and therapeutic indexes (SI) of 12