Synthesis and anti-HIV activity of new urea and nitrosourea derivatives of diamino acids

Dulude, Hélène; Salvador, R. L.; Gallant, Gilles

doi:10.1016/0968-0896(95)00008-5

Cited by 9 publications

(9 citation statements)

References 19 publications

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“…evaluated as antitumor agents (Ahmed et al, 1995), oxytocin antagonists (Hobbs et al, 1995), anti-HIV drugs (Dulude et al, 1995), antianxiety agents (Prakash & Cui, 1997;Prakash et al, 1998), analgesics (Shafiee et al, 1999), and aldose reductase inhibitors (Kurono et al, 2001). Thus, the development of agents containing a succinimide ring continues to increase, and it is important to understand the potential toxicities that could result from succinimide-based agents.…”

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confidence: 99%

Mobile Telephones and Cancer—a Review of Epidemiological Evidence

Kundi

Mild²,

Hardell

et al. 2004

Journal of Toxicology and Environmental Health, Part B

135

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There is considerable public concern about possible long-term adverse health effects of mobile phones. While there is scientific controversy about long-term health effects of high-frequency electromagnetic fields lasting for at least 50 yr, the rise and success of mobile telecommunication made it necessary to investigate the problem more comprehensively and assess the possible risk cautiously because never before in history has a substantial proportion of the population been exposed to microwaves in the near field and at comparably high levels. Because the mostly localized exposure target region is the head, most epidemiological studies focus on brain tumors. Overall nine epidemiological studies have been published, four from the United States, two from Sweden, and one each from Denmark, Finland, and Germany. Seven studies were mainly on brain tumors, with one investigating in addition to brain tumors salivary gland cancer and another cancer of the hematopoietic and lymphatic tissues, and one examining intraocular melanoma. All studies have some methodological deficiencies: (1) too short duration of mobile phone use to be helpful in risk assessment, (2) exposure was not rigorously determined, and (3) there is a possibility of recall and response error in some studies. Nevertheless, all studies approaching reasonable latencies found an increased cancer risk associated with mobile phone use. Estimates of relative risk in these studies vary between 1.3 and 4.6 with highest overall risk for acoustic neuroma (3.5) and uveal melanoma (4.2), and there is evidence for enhanced cancer risk with increasing latency and duration of mobile phone use.

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confidence: 99%

Mobile Telephones and Cancer—a Review of Epidemiological Evidence

Kundi

Mild²,

Hardell

et al. 2004

Journal of Toxicology and Environmental Health, Part B

135

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“…Synthesis of (E or Z)-1-(9-benzylidene-9H-fluoren-2-yl)-3-phenylurea/thiourea derivatives The synthesized compounds were characterized by 1 H NMR, 13 C NMR, IR and elemental analysis. From the 1 H NMR spectra, the resonance due to the hydrogen attached to the amide nitrogen was between 8.50 and 10.00 ppm.…”

Section: Resultsmentioning

confidence: 99%

“…The precipitated product was filtered and washed with a few drops of ethyl ether. 13 3. CA ENZYME ASSAY…”

Section: General Procedures For the Synthesis Of (E Or Z)-1-(9-benzylimentioning

confidence: 99%

“…Due to their biological activities, substituted urea and thiourea compounds have potential as chemotherapeutic agents [11,12], HIV protease inhibitors [13], tyrosinase inhibitors [14,15], herbicides and antifungal agents [16]. In addition, recent studies have shown that different urea derivatives have dopamine hydroxylase inhibitory properties, and dopamine is a key precursor of norepinephrine [17].…”

Section: Introductionmentioning

confidence: 99%

“…benzylidene-9H-fluoren-2-yl)-3-phenylthiourea (5q): Yield 92%, m.p. 148-149 ºC; IR (, cm -1 ): 3217 (NH), 3051 and 3018 (C=C-H, Aromatic C-H), 1539 (S=C-N-H), 1255 (C-N); 1 H NMR (300 MHz, DMSO-d 6 , ppm): 7.25 (t, 1H, J = 7.9 Hz, =CH), 7.43-7.94 (m, 17H, Ar-H),9.73 (s, 1H, -NH),9.82 (s, 1H, -NH);13 C NMR (75 MHz, DMSO-d 6 , ppm): 120.2, 120.4, 120.8, 121.4, 124.4, 124.6, 125.1, 127.5, 129.0, 129.4, 129.8, 130.0, 135.6, 136.5, 137.9, 138.8, 140.0, 140.2, 180.0; Anal. Calcd.…”

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confidence: 99%

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In vitro inhibition of purified human carbonic anhydrase I and II by novel fluorene derivatives

Demirhan

Arslan

Kaya

et al. 2014

Maced. J. Chem. Chem. Eng.

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In this study, 9-benzylidene-9H-fluorene-substituted urea (5a-p) and thiourea derivatives (5q-v) were synthesized and their inhibitory effects on the activity of human carbonic anhydrase (hCA) I and II were evaluated. hCA I and II were purified from human erythrocytes using a Sepharose 4B-L-tyrosinesulphanilamide affinity column. All the synthesized compounds inhibited the activity of the hCA I and II isoenzymes. Among the synthesized compounds, 5f was found to be the most active (IC 50 = 21.4 μM) for inhibition of hCA I and 5s was the most active (IC 50 = 25.3 μM) for inhibition of hCA II. IN VITRO ИНХИБИЦИЈА НА ПРЕЧИСТЕНА ЧОВЕЧКА КАРБОНСКА АНХИДРАЗА I И II СО НОВИ ФЛУОРЕНСКИ ДЕРИВАТИВо оваа студија беа синтетизирани деривати на уреа (5a-p) и тиоуреа (5q-v) добиени со супституција на 9-безилиден-9H-флуорен и беше проценет нивниот инхибиторен ефект врз човечка карбонска анхидраза (hCA) I и II. HCA I и II беа пречистени од човечки еритроцити со употреба на афинитетната колона Sepharose 4B-L-тирозин-сулфаниламид. Сите синтетизирани соединенија ја инхибираа активноста на изоензимите на hCA I и II. Од синтетизираните соединенија, 5f се покажа најактивно (IC 50 = 21,4 μM) за инхибиција на hCA I, додека 5s беше најактивно (IC 50 = 25,3 μM) за инхибиција на hCA II.Клучни зборови: 9-безилиден-9H-флуорен; уреа; тиоуреа; карбонска анхидраза; инхибиција

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