Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity.

Desai, Jigar; Patel, Bhaumin; Panchal, Nandini; Gite, Archana; Darji, Brijesh; Viswanathan, Kasinath; Trivedi, Jinal; Vyas, Purvi; Pawar, Vishwanath; Giri, Poonam; S, Sachchidanand; Sharma, Rajiv; Jain, Mukul; Iyer, Pravin; Kumar, Sanjay

Desai, Jigar; Patel, Bhaumin; Panchal, Nandini; Gite, Archana; Darji, Brijesh; Viswanathan, Kasinath; Trivedi, Jinal; Vyas, Purvi; Pawar, Vishwanath; Giri, Poonam; S, Sachchidanand; Sharma, Rajiv; Jain, Mukul; Iyer, Pravin; Kumar, Sanjay.

Afiliación

Desai J; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India. Electronic address: jigardesai@zyduslife.com.
Patel B; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Panchal N; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Gite A; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Darji B; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Viswanathan K; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Trivedi J; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Vyas P; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Pawar V; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Giri P; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
S S; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Sharma R; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Jain M; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Iyer P; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
Kumar S; Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.

Bioorg Med Chem Lett ; 111: 129911, 2024 Oct 01.

Article en En | MEDLINE | ID: mdl-39067715

ABSTRACT

ABSTRACT

Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. The Novel Bacterial Topoisomerase Inhibitors (NBTIs) bind to a different site from that of the quinolones with novel mechanism of action. This evades the existing target-mediated bacterial resistance associated with quinolones. This article presents our efforts to identify in vitro potent and broad-spectrum antibacterial agent 4l.

Asunto(s)

Antibacterianos; Pruebas de Sensibilidad Microbiana; Piperidinas; Antibacterianos/farmacología; Antibacterianos/química; Antibacterianos/síntesis química; Piperidinas/química; Piperidinas/farmacología; Piperidinas/síntesis química; Relación Estructura-Actividad; Inhibidores de Topoisomerasa/farmacología; Inhibidores de Topoisomerasa/química; Inhibidores de Topoisomerasa/síntesis química; Girasa de ADN/metabolismo; Inhibidores de Topoisomerasa II/farmacología; Inhibidores de Topoisomerasa II/química; Inhibidores de Topoisomerasa II/síntesis química; Topoisomerasa de ADN IV/antagonistas & inhibidores; Topoisomerasa de ADN IV/metabolismo; Estructura Molecular; Descubrimiento de Drogas; Relación Dosis-Respuesta a Droga; Humanos

Palabras clave

DNA gyrase; MIC; NBTI; Topoisomerase

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Pruebas de Sensibilidad Microbiana / Antibacterianos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido

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