Novel N-phenylcarbamothioylbenzamides with anti-inflammatory activity and prostaglandin E₂ inhibitory properties

Figures & data

Figure 1 Synthetic pathway for the new N-phenylcarbamothioylbenzamides 1a–h.

Figure 2 Percent inhibition of carrageenan paw edema for N-phenylcarbamothioylbenzamides 1a–h in mice.^a

Notes:
^aDoses administered: indomethacin and test compounds 1a–h (0.028 mmol). Percentage of inhibition of edema expressed as means of five replicates ± standard error of the mean. *Significantly statistically different from IND group (P = 0.049 for 1a, 0.0015 for 1d, and 0.033 for 1f); **significantly statistically different from IND group and groups treated with 1a (P = 0.0014 for 1e and 0.0022 for 1h), 1b, 1c, and 1d (P = 0.031 for 1e), 1f (P = 0.026 for 1e), and 1g (P = 0.0011 for 1h); ^#no activity observed.
Abbreviations: CON, placebo control; IND, positive control.

Table 1 Effect of indomethacin and compounds 1a, 1e, and 1h on ulcerogenic properties

Compound	Ulcer incidence, number/group	Ulcer index, mean ± SEM (mm)	% incidence
IND	4/5	0.60 ± 0.11	80
1a	4/5	0.50 ± 0.16	80
1e	1/5	0.20 ± 0.02a,b	20
1h	1/5	0.40 ± 0.12	20

Notes:

a Significantly statistically different from IND values (P = 0.001);

b significantly statistically different from 1a (P = 0.009).

Abbreviations: IND, indomethacin; SEM, standard error of the mean.

Figure 3 Inhibition of prostaglandin E₂ (PGE₂) by test compounds 1a, 1e, and 1h.

Notes: Percent inhibition of PGE₂ synthesis expressed as means of five replicates ± standard error of the mean. Doses administered: indomethacin and test compounds 1a, 1e, and 1h (0.028 mmol/kg). *significantly statistically different from CON group (P < 0.001); ^#significantly statistically different from IND group (P = 0.040) and 1a (P < 0.001).
Abbreviations: CON, placebo control; IND, positive control.