Alberti C, Tironi C, Bainotti F, Deleide G
Farmaco Sci. 1977 Feb;32(2):92-105.
The research on the change of antibacterial activity due to the introduction of a nitro group in the benzene nucleus linked at the heterocyclic nitrogen of N-phenylsulfanilamidopyrazoles is continued with the preparation of 1-(2'-nitrophenyl)-4-sulfanilamidopyrazole (IIa: -NO2 in 2'; R=-H), 1-(3'-nitrophenyl)-4-sulfanilamidopyrazole (IIb: -NO2 in 3'; R=-H) and 1-(4'-nitrophenyl)-4-sulfanilamidopyrazole (IIc: -NO2 in 4'; R=-H). By analogy with the results obtained for the derivatives of 4-sulfanilamidopyrazole (I) previously prepared, enhancement of the bacteriostatic activity in vitro against S. aureus and E. coli, have been observed in almost all the cases, especially with 1-(3-nitrophenyl)-4-sulfanilamidopyrazole (IIb).
通过制备1-(2'-硝基苯基)-4-磺胺基吡唑（IIa：2'位有-NO₂；R = -H）、1-(3'-硝基苯基)-4-磺胺基吡唑（IIb：3'位有-NO₂；R = -H）和1-(4'-硝基苯基)-4-磺胺基吡唑（IIc：4'位有-NO₂；R = -H），继续研究在与N-苯基磺胺基吡唑的杂环氮相连的苯环中引入硝基后抗菌活性的变化。与先前制备的4-磺胺基吡唑（I）衍生物所获得的结果类似，几乎在所有情况下，尤其是1-(3-硝基苯基)-4-磺胺基吡唑（IIb），观察到对金黄色葡萄球菌和大肠杆菌的体外抑菌活性增强。
