Salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H2LASSBio-1064) and their complexes [Zn(LASSBio-466)H2O]2 (1) and [Zn(HLASSBio-1064)Cl]2 (2) were evaluated in animal models of peripheral and central nociception, and acute inflammation. All studied compounds significantly inhibited acetic acid-induced writhing response. Upon coordination the anti-nociceptive activity was favored in the complex 1. H2LASSBio-466 inhibited only the first phase of the formalin test, while 1 was active in the second phase, like indomethacin, indicating its ability to inhibit nociception associated with the inflammatory response. Hence coordination to zinc(II) altered the pharmacological profile of H2LASSBio-466. H2LASSBio-1064 inhibited both phases but this effect was not improved by coordination. The studied compounds did not increase the latency of response in the hot plate model, indicating their lack of central anti-nociceptive activity. All compounds showed levels of inhibition of zymosan-induced peritonitis comparable or superior to indomethacin, indicating an expressive anti-inflammatory profile.
The N-acylhydrazone (NAH) moiety is considered a privileged structure, being present in many compounds with diverse pharmacological activities. Among the activities attributed to NAH derivatives anti-inflammatory and analgesic ones are recurrent. As part of a research program aiming at the design of new analgesic and anti-inflammatory lead-candidates, a series of cyclohexyl-N-acylhydrazones 10–26 were structurally designed from molecular modification on the prototype LASSBio-294, representing a new class of cycloalkyl analogues. Compounds 10–26 and their conformationally restricted analogue 9 were synthetized and evaluated as analgesic and anti-inflammatory agents in classical pharmacologic protocols. The cyclohexyl-N-acylhydrazones 10–26 and the cyclohexenyl analogue 9 showed great anti-inflammatory and/or analgesic activities, but compound 13 stood out as a new prototype to treat acute and chronic painful states due to its important analgesic activity in a neuropathic pain model.
In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 μM.
RESUMO: A capecitabina é um agente quimioterápico indicado, dentre outros casos, como monoterapia no câncer de mama metastático. A síndrome mão-pé consiste numa das reações adversas associadas ao seu uso e caracteriza-se por eritema doloroso, edema, disestesia, descamação, bolhas e úlceras nas regiões palmar e plantar. Objetivou-se descrever o caso de uma paciente portadora de carcinoma de mama esquerda com metástase hepática que apresentou síndrome mão-pé decorrente do tratamento com capecitabina. Trata-se de um relato de caso ocorrido num hospital universitário de um estado do nordeste do Brasil em 2016. Foi necessária a suspensão do protocolo antineoplásico utilizado. Observou-se remissão parcial dos sintomas após o uso do gel de Aloe vera para o tratamento das áreas afetadas. Ressalta-se a importância do relato para conhecimento dessa reação adversa, facilitando sua identificação e manejo, para promover melhora da qualidade de vida do paciente oncológico. DESCRITORES: Síndrome mão-pé; Antineoplásicos; Neoplasias da mama. CAPECITABINE-INDUCED HAND-FOOT SYNDROME: A CASE REPORTABSTRACT: Capecitabine is a chemotherapeutic agent indicated, among other things, as monotherapy for metastatic breast cancer. Hand-foot syndrome is one of the adverse effects associated with its use and is characterized by painful erythema, edema, dysesthesia, desquamation, blistering and ulcers in the palms and soles. This study presents a case report on a patient with left-sided breast cancer metastasized to the liver, who suffered from capecitabine-induced hand-foot syndrome. The patient was being treated at a university hospital in a state in the Northeast of Brazil in 2016. Her antineoplastic protocol had to be suspended. After the use of Aloe vera gel to treat the affected areas, there was a partial remission of symptoms.It is important to expand knowledge about this adverse reaction, facilitating its identification and management, in order to improve quality of life in cancer patients. DESCRIPTORS: Hand-foot Syndrome; Antineoplastic Agents; Breast Neoplasms. Cogitare Enferm. 2017 Jan/mar; 22(1): 01-04 SÍNDROME MANO-PIE INDUCIDO POR CAPECITABINA: RELATO DE CASO RESUMEN: La capecitabina es un agente quimioterápico indicado, entre otros casos, como monoterapia en cáncer de mama metastático. El síndrome mano-pie consiste en una de las reacciones adversas asociadas a su uso, caracterizada por eritema doloroso, edema, parestesia, descamación, ampollas y úlceras en regiones palmar y plantar. Se objetivó describir el caso de una paciente con carcinoma en mama izquierda, con metástasis hepática presentando síndrome de mano-pie derivado del tratamiento con capecitabina. Relato de caso ocurrido en hospital universitario de estado del Noreste brasileño en 2016. Fue necesaria la suspensión del protocolo antineoplásico utilizado. Se observó remisión parcial de los síntomas luego de uso de gel de Aloe Vera para tratamiento de las áreas afectadas. Se destaca la importancia del relato para conocimiento de esta reacción adversa, permitiendo su ide...
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