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Moid, A.
- Synthesis, Characterization and Pharmacological Screening of Novel Substituted Isoxazole Derivatives
Authors
1 Department of Pharmaceutical Chemistry, Luqman College of Pharmacy, Gulbarga – 585102, Karnataka, IN
Source
Asian Journal of Research in Chemistry, Vol 5, No 1 (2012), Pagination: 69-73Abstract
As per our previous paper published (AJRC vol. 04, issue 7, 2011), here some more substituted novel isoxazole derivatives were synthesized to enhance its biological activities, so we found that the ortho and meta position has shown highest activity than para, particularly Nitro substituted groups have shown good activity than others. The present research work was aimed to synthesize some novel substituted isoxazole derivatives and screened them for anti-microbial and analgesic activities. The prevalence of isoxazole cores in natural and biologically active molecules has stimulated the need for elegant and efficient ways to make these heterocycles as lead. In this research work the 3- substituted N-(4-hydroxyphenyl) propanamides (B1-B10) were prepared by the reaction of N-(4-hydroxy phenyl) acetamide (A) with various substituted aryl aldehydes by refluxing in ethanol. The resultant compounds on refluxing with hydroxylamine hydrochloride gave the title compounds 4-(5'-substituted-aryl-4', 5'-dihydro-isoxazole-3'-ylamino) phenols (C1-C10). The structure of newly synthesized compounds has been characterized and established by spectral data viz, FT-IR, 1HNMR and Mass. All the derivatives synthesized were subjected for their anti-bacterial and antifungal activities by cup-plate method at the concentration level of 100 μg/ml and compared with the standard Amoxicillin and clotrimazole used. Some of the compounds were subjected for their possible analgesic activity by tailflick method at the dose of 50 mg/kg and compared with that of standard paracetamol.
Keywords
Isoxazoles Derivatives, Antimicrobial Activity and Analgesic Activity.
- Analytical Parameters of Isolated Constituents of Root’s of Syzygium cuminii (L) skeel
Authors
1 Department of Pharmaceutical Chemistry, Luqman College of Pharmacy, Gulbarga-585201, IN
Source
Asian Journal of Research in Chemistry, Vol 4, No 10 (2011), Pagination: 1542-1543Abstract
Syzygium cuminii (L) skeel commonly known as 'jamun' is widely used in Indian folk medicine for the treatment of diabetes Mellitus. The present study an attempt has been made to produce a complete analytical and chemical profile of the isolated constituents of ischolar_main's of syzygium cuminii(L) skeel . The pharmacological and pharmaceutical work is going on in our laboratory.Keywords
Syzygium cuminii (L) skeel, Constituents, Diabetes.- Synthesis, Characterization and Anti-Microbial Evaluation of Substituted Isoxazole Derivatives
Authors
1 Department of Pharmaceutical Chemistry, Luqman College of Pharmacy, Gulbarga - 585102, IN
Source
Asian Journal of Research in Chemistry, Vol 4, No 7 (2011), Pagination: 1158-1160Abstract
The prevalence of isoxazole cores in natural and biologically active molecules has stimulated the need for elegant and efficient ways to make these heterocycles as lead. A systematic investigation of this class of heterocycle revealed that isoxazole containing pharmacoactive agent's possess analgesic, anti-inflammatory and antimicrobial activities. 4-(5'- substituted-aryl-4,5'-dihydro-isoxazole-3'-yl-amino) phenols possessing potent biological activities. N-(4'- hydroxyphenyl) acetamide (2) was synthesized by the condensation of p-amino phenol (1) with acetyl chloride by refluxing in alkaline medium for 20 minutes. 3-substituted N-(4'-hydroxyphenyl) propanamides (3a-g) were prepared by the reaction of N-(4-hydroxy phenyl) acetamide with various substituted aryl aldehydes by refluxing for 6 hours in ethanol. The resultant compounds on refluxing for 6 hours with hydroxylamine hydrochloride gave the title compounds 4-(5'-substituted-aryl-4', 5'-dihydro-isoxazole-3'-yl-amino) phenols (4a-g). The synthesized derivatives have been characterized by FT-IR, 1HNMR and Mass spectral analysis. All the derivatives synthesized were screened for their anti-bacterial and antifungal activities at the concentration level of 100 μg/ml by cup-plate method. Some of the compounds such as 4a, 4b, 4c, 4d and 4f have shown significant antibacterial and antifungal activity when compared to standard drugs Ciprofloxacin (antibacterial activity) and Clotrimazole (antifungal activity). The results obtained indicate that, when the phenyl group at 5th position of isoxazole nucleus contains the substituents as electron withdrawing atoms/groups particularly at ortho and meta positions could be a decisive factor for the compounds to have the increased potency over the other positions.