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Current Trends in Biotechnology and PharmacyVol. 5 (1) 1021-1028 January 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1025CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),7.58(1H,d,J=8.6Hz,C-2'’-H)6.95 (1H,d,J=8.8Hz,C-3'’-H),6.96(1H,d,J=8.8Hz,C-5'’-H)7.58 (1H,d,J=8.6Hz,C-6'’-H)Anal.Calcd. for C 16H 13FO 2: C, 75.001; H,5.102.Found: C, 74.209; H, 4.707.1-(3'–Methyl -4'-hydroxyphenyl)-3-(4'’-chlorophenyl)-2-propen-1-one (B 11)Yield: 75%; m.p. 213-214 0 CIR (KBr, cm -1 ): 3628 (O-H), 1650 (C=O), 1506(C=C Quadrant of Ar),1462 (CH=CH), 855 (C-Cl)1H NMR (CDCl 3, äppm): 7.76(1H,d,J=17Hz,=CH-Ar),7.47 (1H,d,J=17Hz,-CO-CH=),7.89 (1H,s,C-2'-H),2.30 (3H,s,C-3'-CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),7.55(1H,d,J=8.5Hz,C-2'’-H)7.57 (1H,d,J=8.5Hz,C-3'’-H),7.53(1H,d,J=8.5Hz,C-5'’-H)7.55 (1H,d,J=8.5Hz,C-6'’-H)Anal.Calcd. for C 16H 13ClO 2: C, 70.503; H,4.802.Found: C, 70.103; H, 4.104.1-(3'–Methyl -4'-hydroxyphenyl)-3-(4'’-bromophenyl)-2-propen-1-one (B 12)Yield: 74%; m.p. 55-58 0 CIR (KBr, cm -1 ): 3624 (O-H), 1652 (C=O), 1507(C=C Quadrant of Ar),1464 (CH=CH), 1020 (C-Br)1H NMR (CDCl 3, äppm): 7.82(1H,d,J=17Hz,=CH-Ar),7.29 (1H,d,J=17Hz,-CO-CH=),7.89 (1H,s,C-2'-H),2.30 (3H,s,C-3'-CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),7.45(1H,d,J=8.6Hz,C-2'’-H)7.59 (1H,d,J=8.5Hz,C-3'’-H),7.56(1H,d,J=8.5Hz,C-5'’-H)7.45 (1H,d,J=8.6Hz,C-6'’-H)Anal.Calcd. for C 16H 13BrO 2: C, 60.591; H,4.132.Found: C, 60.481; H, 4.072.1-(3'–Methyl -4'-hydroxyphenyl)-3-(4'’-methylphenyl)-2-propen-1-one (B 13)Yield: 85%; m.p. 121-123 0 CIR (KBr, cm -1 ): 3629 (O-H), 1653 (C=O),1506 (C=C Quadrant of Ar),1463(CH=CH)1H NMR (CDCl 3, äppm): 7.74(1H,d,J=17Hz,=CH-Ar),7.38 (1H,d,J=17Hz,-CO-CH=),7.89 (1H,s,C-2'-H),2.30 (3H,s,C-3'-CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),7.47(1H,d,J=8.1Hz,C-2'’-H)6.97 (1H,d,J=8.1Hz,C-3'’-H),2.40 (3H,s,C-4'’-CH 3)6.94 (1H,d,J=8.1Hz,C-5'’-H),7.47 (1H,d,J=8.1Hz,C-6'’-H )Anal.Calcd. for C 17H 160 2: C, 80.934; H, 6.934.Found: C, 80.453; H, 6.783.1-(3'–Methyl-4'-hydroxyphenyl)-3-(4'’-methoxyphenyl)-2-propen-1-one(B 14)Yield: 83%; m.p. 209-211 0 CIR (KBr, cm -1 ): 3627 (O-H), 1652 (C=O), 1503(C=C Quadrant of Ar),1461 (CH=CH), 1170 (-O-CH 3)1H NMR (CDCl 3, äppm): 7.80(1H,d,J=17Hz,=CH-Ar),7.37 (1H,d,J=17Hz,-CO-CH=),7.89 (1H,s,C-2'-H),2.30 (3H,s,C-3'-CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),7.56(1H,d,J=8.5Hz,C-2'’-H)6.92 (1H,d,J=8.5Hz,C-3'’-H),3.87 (3H,s,C-4'’-OCH 3)6.92 (1H,d,J=8.5Hz,C-5'’-H),7.56 (1H,d,J=8.5Hz,C-6'’-H )Anal.Calcd. for C 17H 160 3: C, 76.102; H, 6.018.Found: C, 76.001; H, 5.937.1-(3'–Methyl -4'-hydroxyphenyl)-3-(3'’,4'’,5'’- trimethoxyphenyl)-2-propen-1-Synthesis and Anti-Inflammatory
Current Trends in Biotechnology and PharmacyVol. 5 (1) 1021-1028 January 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1026one (B 15)Yield: 80%; m.p. 116-119 0 CIR (KBr, cm -1 ): 3625 (O-H), 1654 (C=O), 1505(C=C Quadrant of Ar),1465 (CH=CH), 1175 (-O-CH 3)1H NMR (CDCl 3, äppm): 7.70(1H,d,J=17Hz,=CH-Ar),7.50 (1H,d,J=17Hz,-CO-CH=),7.89 (1H,s,C-2'-H),2.30 (3H,s,C-3'-CH 3),6.93 (1H,d,J=8.6Hz,C-5'-H)7.80 (1H,d,J=8.6Hz,C-6'-H),6.80 (1H,s ,C-2'’-H),3.85 (9H,s, 3 x -OCH 3)6.80 (1H,s ,C-6'’-H)Anal. Calcd. for C 19H 20O 5: C, 69.502; H,6.153.Found: C, 69.431; H, 6.118.Anti-Inflammatory activityThe anti-inflammatory activity of thesynthesized chalcones was evaluated by usingcarrageenan-induced rat paw oedema method(10,11). Albino rats of either sex (150-200g) wereused in the study. The animals were housed understandard environmental conditions (temperatureof 22 ±1 0 C with an alternating 12 hour light-darkcycle and relative humidity of 60±5%), fed withstandard diet and water ad libitum.Rats were divided into seventeen groupsof six animals in each group. Inflammation wasinduced by injecting 0.05 ml of 1% carrageenan(Sigma) subcutaneously into the sub-plantarregion of the right hind paw and 0.05ml salinewas injected into the sub-plantar region of theleft hind paw for all groups. One hour prior tocarrageenan injection, the groups III – XVIItreated with compounds (B 1–B 15) (10 mg/kg).1% Sodium CMC gel (1ml/kg) was given to groupI used as carrageenan treated control and thestandard drug aceclofenac (2 mg/kg) wasadministered to group II. All the doses wereadministered orally. Anti-inflammatory activitywas evaluated by measuring carrageenan inducedpaw oedema.The thickness of the both paws of eachrat, lower and upper surface was measured usingZeitlin’s constant load level method consisting ofa graduated micrometer combined with a constantloaded level system to magnify the small changesin paw thickness during the course of theexperiment. The percent increase of paw oedemathickness was determined at 0, 0.5, 1, 2, 3, 4 and6 hours after induction of inflammation.The percent increase at each time intervalwas determined by using the formula: Y t- Y o/ Y ox 100Y t= paw thickness at time t hours (after injection)Y o= paw thickness at time 0 hours (before injection)The percent inhibition of paw oedemathickness was calculated by using the formula:Percentage inhibition = x 100 1-y 1 = 100y 2Where Y t= average increase in paw thicknessin groups tested with chalcones and the standardY c= average increase in paw thicknessin controlThe results and statistical analysis of anti-inflammatoryactivity of aceclofenac and the compoundstested are shown in Table 1.All values are represented as mean ± SEM (n=6).*P
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