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The synthesis of a series of N-(methylene-4-oxo coumarinyl) carbamates by the condensation of various carbamates with 4-hydroxy coumarins in the presence of triethylorthoformate was undertaken to obtain the the title compounds in 50-55% yields. Preliminary data shows that only few molecules are active against B. subtilis, S. aureus, E. coli and P. aeruginosa at minium inhibitory concentrations (MIC) of 100, 300, 500 micrograms/ml compared to streptomycin (CAS 57-92-1) and kanamycin (CAS 59-01-8). The alkyl groups present in the benzenoid part and the higher amino acid residues like 3a, 3c, 5a and 5b were found to be more active in the title compounds (i.e. 2d and 2e).
Dazzle Capsule, a Poly herbal formulation is marketed in management of Arthritis and joint-musculo skeletal pain. In this study, safety and efficacy of this polyherbal formulation was investigated in which it was being proved safe for use via acute toxicity study and efficacy was being evaluated by carrageenan-induced rat paw oedema test in rats in order to explore its anti-inflammatory activity at the dose level of 90 and 180 mg/kg, p.o, compared with Indomethacin (10 mg/kg, p.o.). It showed an highly significant reduction in oedema (p<0.001). Indomethacin inhibited oedema by 30.054% and 36.216% at 2 and 3 hr after carrageenan injection, respectively. The inhibitory effect of Dazzle Capsule began at 2 hr or later after carrageenan injection depending upon the administered dose. Low doses of Dazzle Capsule (90 mg/kg) gave highly significant inhibitory effects of 37.894-39.378%, and higher doses (180 mg/kg) caused highly significant inhibition of 19.125-30%. The reduction of oedema by Indomethacin and Dazzle Capsule at 2 hr or more after carrageenan injection suggested that both compounds produce anti-inflammatory effects in the second phase of oedema, indicating inhibition of prostaglandin synthesis. Hence, it was concluded that, Dazzle Capsule is having potent anti-inflammatory activity yet safe polyherbal formulation for use in arthritis management.
Synthesis and Biological Evaluation of N-Substituted α-Amino Acids from 4-Hydroxy Coumarins. -12 Coumarin derivatives of type (IV) are prepared and tested for their antibacterial activities. Only a few compounds are active at MIC of 100, 300, and 500 µg/ml. -(CHAVDA, M.; SHAH*, A.; BHATT, S.; DEO, K.; KUNDU, P.; Arzneim.-Forsch. 53 (2003) 3, 196-200; Dep. Chem., Saurashtra Univ., Rajkot 360 005, India; Eng.) -M. Bohle 28-152
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