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1.
SPJ-Saudi Pharmaceutical Journal. 2005; 13 (4): 185-191
in English | IMEMR | ID: emr-172117

ABSTRACT

S-Triazoles have been utilized to produce reagents that can react with drugs containing carbonyl group and drugs that are susceptible to oxidation with periodic acid to produce carbonyl function such as diols and amino alcohols. In this study, glucosamine and mannitol were analyzed through oxidation with periodic acid to give formaldehyde which was allowed to condense with 4-Amino5-hydrazino-4H[1,2,4]-triazole-3-thiol [AHTT] [1]. The condensation product was further oxidized to yield a purple colored compound [II] with maximum absorption at 550 nm. Beer's law was obeyed in the range of 12.5-125 lig for glucosamine and 25-150 mg ml for mannitol. Both drugs were also successfully determined in their pharmaceutical formulations with mean percentage recoveries +/- RSD ranged between 100.69-101.51% +/- 1.57-0.44 for glucosamine and 100.06% +/- 1.08 for mannitol

2.
SPJ-Saudi Pharmaceutical Journal. 2005; 8 (4): 198-204
in English | IMEMR | ID: emr-75119

ABSTRACT

The synthesis and biological evaluation of many 3-[4-[[[[cyckohexylamino] carbonyl]amino]sulfonyl]phenyl-4[3H]-quainzolinones [IVa-t] as oral hypoglycemics are described. Derivates [IVf], [IVg], [IVh], [IVj], [IVk], [IVm], [IVq] and [IVr] showed appreciable glucose lowering effects in alloxanized diabetic rats at a dose of 5 mg/kg. They decreased the blood glucose level by 40.7, 36.4, 37.2, 35.4, 43.7, 38.8, 35.3, 42.9 and 45.9 respectively. The hypoglycemic action of the synthesized compounds is comparable to, and in few cases is higher than that exhibited by the well known antidiabetic drug "glyburide" which showed 35.1 percent decrease of the blood glucose level


Subject(s)
Quinazolines/chemistry , Quinazolines/pharmacology , Sulfonylurea Compounds , Hypoglycemic Agents , Glyburide
3.
SPJ-Saudi Pharmaceutical Journal. 2000; 8 (2-3): 110-115
in English | IMEMR | ID: emr-55799

ABSTRACT

Some new 6-substituted 5H-dibenz[c,e]azepine-5,7[6H]-diones [VII] were synthesized and tested for possible hypolipidemic activity. Thus anthranilic acid [I] was converted to diphenic acid [II] which was cyclodehydrated to give diphenic anhydride [III]. Ammonolysis of [III] afforded diphenamic acid [IV] which was cyclodehydrated to yield diphenimide [V]. Potassium salt of [V] was condensed with chloroacetic acid, ethyl chloroacetate or N-substituted and unsubstituted chloroacetamides to produce the target compounds [VII]. The preliminary evaluation of the hypolipidemic activity of [VII] against Triton WR 1339-induced hyperlipidemia in rats showed that several derivatives have demonstrated significant lowering of serum total cholesterol and triglyceride levels at dose of 150 mg/kg comparing with clofibrate


Subject(s)
Dibenzazepines/pharmacology , Dibenzazepines/chemical synthesis , Lipids/blood
4.
SPJ-Saudi Pharmaceutical Journal. 1994; 2 (1): 21-31
in English | IMEMR | ID: emr-35606

ABSTRACT

Condensation of various 4H-3.1 benzoxazin-4-ones [III] with homoslfanilamide afforded some new derivatives of 3-[p-sulfamoylbenzyl]-4 [3H]-quinzolinone [V]. Some o-amido-N- [p-sulfamoylbenzyl]-benzamides [IV] were isolated as reaction intermediates. Structures of the newly synthesized compounds were confirmed by IR, 1H-NMR, MS and elemental analyses. Several target compounds [V] exhibited good anticonvulsant effects against pentylentetraxol -induced convulsions in frogs. Compound [V-4] was 2.33 times as potent as phenobarbitone


Subject(s)
Quinazolines/analogs & derivatives , Anticonvulsants/chemical synthesis , Quinazolines
5.
SPJ-Saudi Pharmaceutical Journal. 1994; 2 (3): 123-130
in English | IMEMR | ID: emr-35625

ABSTRACT

A number of 3-[4'-carbamoylphenyl] 2-methyl-4[3H]-quinazolinones were prepared as potential anticonvulsants. Their 1H-and 13CNMR parameters were measured. Assignments of the different proton and carbon signals were made depending on the basis of the chemical shift theory, signal multiplicity, additivity rules and comparison with the data reported for analogous compounds, in addition to CH-COSY and DEPT experiments. By alteration of the substituents on the amide nitrogen, the spin system of the aromatic protons of the 3-[4'-carbamoy1pheny1] moiety could be changed from two doublets of AA' XX' type to a pair doublets of AA'BB' type and finally to a singlet


Subject(s)
Anticonvulsants/chemistry , Quinazolines/analysis , Quinazolines/chemistry , Magnetic Resonance Spectroscopy
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