Reference

N-Mannich bases of o-ethoxybenzamide as potential analgesics

N-Mannich bases of o-ethoxybenzamide as potential analgesics. Chaturvedi, S. C.; Ezeugwu, A. C. (Dep. Pharm. Chem., Univ. Nigeria, Nsukka, Nigeria). Indian J. Pharm. Sci., 46(3), 114-16 (English) 1984. CODEN: IJSIDW. ISSN: 0250-474X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 25, 27, 28 N-Mannich bases of o-ethoxybenzamide of aliph. 104123-76-4 and 104123-80-0 which are cas registry numbers of chemicals are mentioned., arom. and heterocyclic amines were synthesized. All the compds. had greater analgesic activity than the parent compd. o-Ethoxybenzamide [938-73-8], N-(diethylaminoethyl)-o-ethoxybenzamide HCl [104123-76-4] and N,N'-bis (o-ethoxybenzamidomethyl)piperazine [104123-78-6] showed analgesic activity comparable to that of morphine. Structure-activity relations are discussed. .

Intestinal first-pass metabolism of phenacetin, acetaminophen, ethenzamide, and salicylamide in rabbits pretreated with 3,4-benzo[a]pyrene

Intestinal first-pass metabolism of phenacetin, acetaminophen, ethenzamide, and salicylamide in rabbits pretreated with 3,4-benzo[a]pyrene. Nakamura, Junzo; Nakamura, Tadahiro; Podder, Samir Kumar; Sasaki, Hitoshi; Shibasaki, Juichiro (Fac. Pharm. Sci., Nagasaki Univ., Nagasaki 852, Japan). Biochem. Pharmacol., 36(7), 1171-4 (English) 1987. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 4 The effects of induction of intestinal drug-metabolizing enzymes with 3,4-benzo[a]pyrene [50-32-8] on the absorption of phenacetin (PHT) [62-44-2], acetaminophen (NAPA) [103-90-2], ethenzamide (ETB) [938-73-8], and salicylamide (SAM) [65-45-2] were examd. in rabbits using in situ intestinal sacs with complete mesenteric venous blood collection. The appearance of both free drug and its metabolites into the mesenteric blood was measured directly by cannulating the mesenteric vein of exposed rabbit intestine and collecting all venous blood draining from the absorbing region. 3,4-Benzo[a]pyrene pretreatment resulted in enhanced PHT metab. as was shown from the decreased appearance of PHT and the increased appearance of NAPA and acetaminophen glucuronide [16110-10-4] in mesenteric venous blood. However, no effect of 3,4-benzo[a]pyrene on the metab. 65-45-2 and 50-32-8 are also in the experiment. of NAPA was found. These results indicate enzyme induction for O-deethylation of PHT by pretreatment with 3,4-benzo[a]pyrene. In control rabbits, ETB was not metabolized in the intestinal wall. In addn., the effect was hardly detectable in the metab. of ETB and SAM after pretreatment with 3,4-benzo[a]pyrene. It is suggested that ETB, in contrast with PHT, is not O-deethylated to SAM in rabbit intestinal wall. .