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1986| July-August | Volume 48 | Issue 4
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Quest for anthelminitic agents, part II benzothiazole and benzotriazole carbamates and 2-benzazolyl vinyl ketones.
K Nagarajan, SB Hendi, AN Goud, HG Sen, BN Deb
July-August 1986, 48(4):85-88
Several benzthiazole carbamate analouges 12-17 and 21 of anthelminitic benzimidazole carbamates like mebendazole (1) and fenbendazole(3) are synthesised from the corresponding 2-aminobenzthiazoles. 1,2-Diamino-5,6,7,8-tetrahydronapthalene asffords through the aminonaphthimidazole 23, the carbamate 24 which is a cyclised version of parbendazole (4). 3,4-Diaminobenzophenone upon diazotisation gives the benzotriazole 25 and thence the ester 26. 2-Acetylbenzimidazole (27) and 2-acetylbenzthiazole (28) are condensed with aldehydes to give 2-benzazolyl vinyl ketones 29-34. All the products are found to be inactive in curing hamsters of N. americanus infection.
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Synthesis and evaluation of antifungal and antibacterial activity of 2-amino- and 2-mercapto-4-(2',3'-dihydro-2'-methylbenzofuran-5'-yl) thiazoles and their derivatives.
VK Ahluwalia, KK Arora, G Kaur
July-August 1986, 48(4):95-98
Synthesis of 2-amino-4-(2,3-dihydro-2-methylbenzofuran-5-yl) thiazole and 2-mercapto-4-(2,3-dihydro-2-methyl benzofuran-5-yl) thiazole have been carried out starting from 5-acetyl-2,3-dihydro-2-methylbenzofuran. These compounds have shown marginal activity when tested against Aspergillus fumigatus, Aspergillus niger Staphylococcus aureus and Escherichia coli at 25 and 50 mcg ml concentrations.
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Some cns depressant steroidal tetrazoles.
TR Bhardwaj, SN Singh, SK Kulkarni, D Paul, H Singh
July-August 1986, 48(4):98-101
Eight steroidal tetrazoles were studied for their CNS activity in mice. Their effects on analgesia, pentobarbital hypnosis, spontaneous motor activity and body temprature were examined. Compounds (2,3 and 4) showed CNS depressant activity in the above mentioned parameters. The other compounds tested had varying degrees of CNS activity. However, none of the compounds exhibited any anticonvulsant property in maximal electro-shock-induced convulsions, although compound (3) offered 80 percent protection against mortality.
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Metal chelates of juglones and their antimicrobial activity.
CR Joshi
July-August 1986, 48(4):101-104
Metal chelates of 2-hydroxy-1,4-napthoquinone (L') and 5-hydroxy-1,4-naptho-quinone (L") with Cu, Ni, Co, Mn and Fe having composition ML2 2H2O have been synthesised, their structure assigned and screened for antimicrobial activities. The activity of metal chelates of compound (L") were found to be more than that of compound (L') against some micro-organisms.
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Synthesis and in vitro amoebicdal activity of some n, n'-disubstituted diamines.
PL Kachroo, R Gupta, R Wadhawan
July-August 1986, 48(4):89-91
Eighteen N, N'-di[3-(2,4-dialkoxy-5-alkylphenyl) propyl]-1,2 ethane; 1,4-butane and 1,4-benzene diamines have been synthesised by condensation of 2,4-dialkoxy-5-alkylbenzenepropanoyl chlorides with 1,2-diamino ethane, 1,4-di-aminobutane and 1,4-diaminobenzene followed by reduction of the diamides with LAH. the diamine dihydrochlorides have been tested in vitro for amoebicidal activity against E. histolytica.
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Synthesis of a new series of 1-(arylideneamino)-3-(4'-substituted sulphone)-guanidines as hypoglycemic agents.
VR Agarwal, DD Mukerji
July-August 1986, 48(4):104-106
Eight title compounds were synthesized by refluxing 1-(arylidene)-S-methylthiosemicarbazide with appropriate sulphonamides and their structures established by elemental analyses and spectral (IR, PMR) studies. In pharmacological screening, the compounds showed a reduction in blood glucose level upto 25 in rats at an oral dose of 250 mg/kg (tolbutamide 40 percent).
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Antidepressants fail to adenosine-induced relaxation of the rat caecum.
AK Mehta, SK Kulkarni
July-August 1986, 48(4):92-93
Adenosine induced a concenration-dependent relaxation of the rat caecum preparation. Imipramine, trimipramine, desipramine, tranylcypromine and amitriptyline in a concentration of 20 mu M neither exhibited any effect per se nor modified adenosine-induced relaxation of the rat caecum preparation. These observations suggested that antidepressants do not cause a functionally important inhibition of adenosine uptake, and the reported interactions of antidepressants with adenosine in in vitro may be pharmacologically irrelevent.
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