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作为药物制剂的N-三氟乙酰基衍生物。V. 某些N-杂环三氟乙酰胺的抗炎和抗菌活性评估

N-trifluoroacetyl derivatives as pharmacological agents. V. Evaluation of antiinflammatory and antimicrobial activities of some N-heterocyclic trifluoroacetamides.

作者信息

Vigorita M G, Previtera T, Zappalà C, Trovato A, Monforte M T, Barbera R, Pizzimenti F

机构信息

Dipartimento Farmaco-Chimico facoltà di Farmacia, Università di Messina, Italy.

出版信息

Farmaco. 1990 Feb;45(2):223-35.

PMID:2133997
Abstract

Following the investigation on pharmacological aspects of N-trifluoroacetyl compounds some heterocyclic trifluoroacetamides were prepared and explored as potential antiinflammatory-analgesic and antimicrobial agents. The trifluoroacetamides 3, 4, 5, and 6 reached significant activity in the hot plate analgesic test; the same 4 and 5, along with 7 and 8 showed inhibitory properties in the adjuvant arthritis test; only 7 however, displayed a significant dose-dependent activity in the carrageenin edema test. In addition the parent heterocyclic amines were similarly explored for comparison. Test for antimicrobial activity were carried out in parallel. Among the examined compounds, only 4-aminomorpholine and 2-aminobenzimidazole were found active when assayed against gram+ and gram- bacteria and mycetes.

摘要

在对 N-三氟乙酰化合物的药理学方面进行研究之后,制备了一些杂环三氟乙酰胺,并将其作为潜在的抗炎镇痛和抗菌剂进行了探索。三氟乙酰胺 3、4、5 和 6 在热板镇痛试验中达到了显著活性;同样的 4 和 5 以及 7 和 8 在佐剂性关节炎试验中表现出抑制特性;然而,只有 7 在角叉菜胶水肿试验中表现出显著的剂量依赖性活性。此外,还对母体杂环胺进行了类似的探索以作比较。同时进行了抗菌活性测试。在所检测的化合物中,仅发现 4-氨基吗啉和 2-氨基苯并咪唑在针对革兰氏阳性菌、革兰氏阴性菌和霉菌进行检测时有活性。

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