• Title/Summary/Keyword: urea derivatives

Search Result 63, Processing Time 0.02 seconds

Studies on the Syntheses and Antimicrobial Activity of Substituted Benzothiazolyl Urea Derivatives (Substituted Benzothiazolyl Urea 유도체의 합성 및 항균작용에 관한 연구)

  • 강회양
    • Journal of Environmental Health Sciences
    • /
    • v.7 no.2
    • /
    • pp.113-117
    • /
    • 1981
  • Twelve benzothiazolyl and 6-substituted benzothiazoly phenyl and chlorophenyl ureas have been newly synthesized by reacting 2-amino benzothiazole and 2-amino-6-substituted benzothazole with three or four phenyl and chlorophenyl isocyanate, respectively. The structures of these compounds were determined by measurement of the molecular weights and elementary analysis as well as IR spectrophotometry. The compounds generally exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli in the concentration of $50\mu g/ml$. The compounds containing chloro group exhibited stronger antibacterial activity than those containing methyl group against Eschichia coli. The difference in the antibacterial activity according to the substituted group (phenyl, o-, m-, and p-chlorophenyl) was also noted. The compounds containing o-chlorophenyl group, on the whole, exhibited more potent growth-inhibitory activity againsts staphylococcus aureus.

  • PDF

Toxicological and Pharmacological Studies of New Coumarin and Furocoumarin Derivatives in Albino rats

  • Shabrawy, Osama A. El;Batran, Seham Abd El Sattar El;Mahran, Mohamed Refat H.;Ibrahim, Nabila M.
    • Natural Product Sciences
    • /
    • v.17 no.4
    • /
    • pp.309-314
    • /
    • 2011
  • Synthetic coumarin and furocoumarin derivatives were evaluated for anticoagulant activity and the effect on liver and kidney function. It was found that all of the compounds under investigation proved to be neither toxic nor lethal up to 500 mg/100 g body weight as a single dose for 24 hrs. All tested compounds showed a significant increase in prothrombin time (PT) in the acute model but failed to show a significant action in the chronic model. Furthermore, all tested compounds revealed a significant increase in activated partial thromboplastin time (APTT) as compared to control value in both acute and chronic model. Also, all tested compounds did not cause any significant changes on liver and kidney functions in rats.

Synthesis and Antiproliferative Activity of Quinazolinylmethoxybenzene Derivatives against Melanoma Cell Line (Quinazolinylmethoxybenzene 유도체 합성 및 흑색종 세포증식 저해효능)

  • Lee, Jun-Sang;Yoo, Kyung-Ho
    • Journal of the Korean Applied Science and Technology
    • /
    • v.27 no.1
    • /
    • pp.20-28
    • /
    • 2010
  • Melanoma is the most aggressive form of skin cancer and is the fastest growing type of cancer in the United States. We report here the synthesis of a novel series of quinazolinylmethoxybenzene derivatives 1a-c and their antiproliferative activities against A375 human melanoma cell line. Among them, urea compound 1a ($IC_{50}\;=\;4.8\;{\mu}M$) having 4-chloro-3-trifluoromethylphenyl moiety showed superior antiproliferative activity to Sorafenib ($IC_{50}\;=\;5.5\;{\mu}M$) as a reference compound. These results will helpful for designing structure of a therapeutic agent for the treatment of melanoma.

Microwave-Assisted One-Pot Synthesis of Octahydroquinazolinone Derivatives Catalyzed by Thiamine Hydrochloride Under Solvent-free Condition

  • Badadhe, Pravin V.;Chate, Asha V.;Hingane, Dattatraya G.;Mahajan, Pravin S.;Chavhan, Namdev M.;Gill, Charansingh H.
    • Journal of the Korean Chemical Society
    • /
    • v.55 no.6
    • /
    • pp.936-939
    • /
    • 2011
  • Thiamine hydrochloride (VB1) has been used as an acid catalyst in organic synthesis. One pot three component Biginelli condensation of dimedone, urea/thiourea and substituted aromatic aldehydes catalyzed by 10 mol % of thiamine hydrochloride (VB1) in solvent free condition under microwave irradiation in good to excellent yields has been investigated. Utilization of microwave irradiation, simple reaction conditions, short reaction time, ease of product isolation, and purification makes this manipulation very interesting from an economic and environmental perspective.

A Novel Synthesis of Heterocyclic Compounds Containing Coumarin Moiety of Potential Antimicrobial Activity

  • El-Fattah, M. E. Abd
    • Archives of Pharmacal Research
    • /
    • v.21 no.6
    • /
    • pp.723-728
    • /
    • 1998
  • The chemical behaviours of 4-methyl-2-oxo-2H-benzopyran-7-yl oxoacetyl hydrazine (2) towards some different reagents such as anhydride compounds, aromatic aldehydes, carb on disulphide, and nitrous acid yielded the corresponding pathalazine derivatives (3, 4, 5), hydrazone derivative (6), 1,3,4-oxadiazole derivative (7, 8, 9) and acid azide (10) respectively. Treatmen of 10 with absolute alcohols, amines and ethyl amino acid ester gave the corresponding carbamate derivative (11), substituted urea derivative (12) and ethyl substituted alkyl acetate (13) respectively. The biological activity of some synthesized compounds was evaluated.

  • PDF

Synthesis and Biological Activity of 1$\beta$-Methyl-2-[5-(2-N-Substituted aminoethylcarbamoyl)pyrrolidin-3-ylthio]carbapenem Derivatives.

  • An, Soo-Hyun;Oh, Chang-Hyun;Lee, Joo-Shin;Lee, Soo-Chul;Choi, Jung-Hun;Baik, Dae-Jin;Cho, Jung-Hyuck
    • Proceedings of the PSK Conference
    • /
    • 2003.04a
    • /
    • pp.238.2-238.2
    • /
    • 2003
  • The synthesis of a new series of 1${\beta}$-methylcarbapenems having the substituted aminoethyl-carbamoylpyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular. the compound 11 g having piperazinyl urea moiety showed the most potent antibacterial activity.

  • PDF

Herbicidal Activity and Persistency in Aqueous Solution of Ortho Disubstituted Benzenesulfonyl Urea Derivatives (새로운 Ortho 이치환 Benzenesulfonyl Urea 유도체의 제초활성과 수용액중의 잔류성)

  • Kim, Yong-Jip;Chang, Hae-Sung;Kim, Dae-Whang;Sung, Nack-Do
    • Applied Biological Chemistry
    • /
    • v.38 no.6
    • /
    • pp.570-576
    • /
    • 1995
  • The new sixteen herbicidal N-2-(1-hydroxy-2-fluoroethyl)-6-substituted(X)-benzenesulfonyl-N'-4,6-dimethoxypyrimidinyl-2-yl urea derivatives(S) were synthesized and thier herbicidal activities$(pI_{50})$ in vivo against rice(Orysa Sativa L.), Barnyard grass(Echninochloa orizicola) and Bulrush(Scirpus juncoides) were measured by the pot test under paddy conditions. The structure activity relationship(SAR) were studied using the physicochemical parameters of ortho-substituents(X) and hydrolysis rate constant(logk) and herbicidal activities by the multiple regression technique. The SAR suggested that the herbicidal activities were more dependant on the hydrolysis rate constant(logk>0) than the steric constants $(Es, small width($B_4$) and length($L_1$). Among them, halogens(2 & 5), methyl(15) and non(H) substituent(1) showed higher herbicidal activity for weeds which was not tolerent to rise and weeds. The herbicidal activity was increased and the persistency in aqueous solution was decreased by electron donating(${\sigma}0<0$) groups as ortho-substituent(X). From the relationship equation between herbicidal activity and hydrolysis rate constant, it was assumed that the both reactions would be proceeds with similar process. And the conditions on the ortho substituents to show higher herbicidal activity and the persistency in aqueous solution were also discussed.

  • PDF

Effect of Molasses or Rice Gruel Inclusion to Urea Supplemented Rice Straw on Its Intake, Nutrient Digestibilities, Microbial N Yield, N Balance and Growth Rate of Native (Bas indicus) Growing Bulls

  • Chowdhury, S.A.;Huque, K.S.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.11 no.2
    • /
    • pp.145-151
    • /
    • 1998
  • The possibility of using rice gruel compared to that of the cane molasses as a source of readily fermentable energy for a urea supplemented straw diet has been studied. Twelve native growing bulls of $237{\pm}8.7kg $ live weight and months old were randomly allocated to three treatments fed solely rice straw enriched with : (1) 3% urea (US), (2) 3% urea + 15% molasses (UMS) and (3) 3% urea + 30% rice gruel (UGS). The feeding trial continued for sixty days. Organic matter (OM) intake was significantly (p < 0.05) higher in the UMS ( $64g/kg\;W^{0.75}/d$) followed by UGS ($53g/kg\;W^{0.75}/d$) and US ($49g/kg\;W^{0.75}/d$). Estimated (from digestible OM intake) metabolizable energy (ME) intake were 396, 348 and $301kJ/kg\;W^{0.75}/d$ for UMS, UGS and US respectively. The maintenance (i.e., no change in live weight) ME intake calculated to be $308{\pm}7.4kJ/kg\;W^{0.75}/d$. Urinary purine derivatives excretion was nonsignificantly higher in the UMS (51.73 mmol/d), followed by UGS (42.53 mmol/d) and US (35.26 mmol/d). The estimated microbial N (MN) yield were 21.10, 14.00 and 11.60 g/d for UMS, UGS and US respectively. For each MJ increase in ME intade, MN yield increased by $1.29{\pm}0.134g$. Observed live weight changes during the experimental period were 292, 125 and -19 g/d respectively for UMS, UGS and US. It was concluded that supplementation of readily fermentable N (urea) alone was not enough to optimize the rumen function and a source of readily fermentable energy was required. Rice gruel was less effective than molasses as fermentable energy source to remove a restriction on voluntary intake and provide less amino acids of microbial origin for absorption from the small intestine, Thus more substrate for protein synthesis and gluconeogenesis were available for growth in the molasses than the rice gruel supplemented animals. However, in situation where molasses is not available or costly, rice gruel does appear to have a place as readily fermentable energy source on a urea supplemented straw diet.