Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors

被引：28

作者：

Biava, Mariangela ^{[1
]}

Battilocchio, Claudio ^{[1
]}

Poce, Giovanna ^{[1
]}

Alfonso, Salvatore ^{[1
]}

Consalvi, Sara ^{[1
]}

Di Capua, Angela ^{[2
]}

Calderone, Vincenzo ^{[3
]}

Martelli, Alma ^{[3
]}

Testai, Lara ^{[3
]}

Sautebin, Lidia ^{[4
]}

Rossi, Antonietta ^{[4
]}

Ghelardini, Carla ^{[5
]}

Mannelli, Lorenzo Di Cesare ^{[5
]}

Giordani, Antonio ^{[6
]}

Persiani, Stefano ^{[6
]}

Colovic, Milena ^{[6
]}

Dovizio, Melania ^{[7
,8
]}

Patrignani, Paola ^{[7
,8
]}

Anzini, Maurizio ^{[2
]}

机构：

[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, I-00185 Rome, Italy

[2] Univ Siena, Dipartimento Biotecnol Chim & Farm, I-53100 Siena, Italy

[3] Univ Pisa, Dipartimento Farm, I-56126 Pisa, Italy

[4] Univ Naples Federico II, Dipartimento Farm, I-80131 Naples, Italy

[5] Univ Florence, Area Farmaco & Salute Bambino, Dipartimento Neurol, I-50139 Florence, Italy

[6] Rottapharm Madaus, I-20052 Monza, Italy

[7] Univ G DAnnunzio, I-66100 Chieti, Italy

[8] CeSI, I-66100 Chieti, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 02期

关键词：

CINODs; Cyclooxygenases; Coxibs; 1,5-Diarylpyrroles; Pharmacodynamic hybrids; Nitric oxide; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; BIOLOGICAL EVALUATION; IN-VITRO; 1,5-DIARYLPYRROLE SCAFFOLD; CYCLOOXYGENASE-2; INHIBITORS; GASTROINTESTINAL TOXICITY; DOCKING SIMULATIONS; DONATOR NAPROXCINOD; ACID-DERIVATIVES; BLOOD-PRESSURE;

D O I：

10.1016/j.bmc.2013.12.008

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives that highlighted outstanding pharmacological properties. In particular, the glycine derivative proved to be extremely active in suppressing hyperalgesia and edema. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：772 / 786

页数：15

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