Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

Ahsan, Mohamed Jawed; Samy, Jeyabalan Govinda; Soni, Savita; Jain, Naresh C.; Kumar, Lalit; Sharma, L. K.; Yadav, Hemant Kumar; Saini, Lokesh; Kalyansing, Rajput Gopal; Devenda, Narendra S.; Prasad, Ravindra; Jain, Chandra Bhushan

doi:10.1016/j.bmcl.2011.07.035

Cited by 27 publications

(16 citation statements)

References 13 publications

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“…A series of 3a,4-dihydro-3 H -indeno[1,2- c ]pyrazole-2-carboxamide analogues were synthesized and evaluated for antitubercular activity. The compound 347 was found to be the most promising compound active against M. tuberculosis H37Rv and isoniazid resistant M. tuberculosis with MIC concentration 3.12 µM and 6.25 µM, respectively [ 249 ]. A new N -aryl-1,4-dihydropyridines derivatives bearing 1 H -pyrazole ring were synthesized and evaluated for antitubercular activity.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…Ahsan et al .,[ 35 ] has synthesized a series of 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogs and evaluated them for anti-tubercular activity. Compound 4o showed low to high inhibitory activities against MTB H37Rv and INH resistant MTB with MIC 3.12 lM and 6.25 lM, respectively [ Figure 33 ].…”

Section: Synthetic Aspects Of Pyrazolementioning

confidence: 99%

Current status of pyrazole and its biological activities

et al. 2016

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Pyrazole are potent medicinal scaffolds and exhibit a full spectrum of biological activities. This review throws light on the detailed synthetic approaches which have been applied for the synthesis of pyrazole. This has been followed by an in depth analysis of the pyrazole with respect to their medical significance. This follow-up may help the medicinal chemists to generate new leads possessing pyrazole nucleus with high efficacy.

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“…When compared with INH the compound 42 was fourfold less active than INH against Mtb and twofold more active than INH against INHR‐Mtb . From SAR concluded same as above, 3‐substituted compounds with electron withdrawing groups such as 4‐fluorophenyl produced more inhibitory activity than 2‐chlorophenyl and 2‐pyridyl substitution . In another article, same author reported synthesis pyrazole‐2‐carboxamide analogues as anti‐TB agents.…”

Section: Pyrazole Derivatives For Treatment Of Tuberculosismentioning

confidence: 79%

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

Keri

Chand

Ramakrishnappa

et al. 2015

Archiv der Pharmazie

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New and reemerging infectious diseases will continue to pose serious global health threats well into the 21st century and according to the World Health Organization report, these are still the leading cause of death among humans worldwide. Among infectious diseases, tuberculosis claims approximately 2 million deaths per year worldwide. Also, agents that reduce the duration and complexity of the current therapy would have a major impact on the overall cure rate. Due to the development of resistance to conventional antibiotics there is a need for new therapeutic strategies to combat Mycobacterium tuberculosis. Subsequently, there is an urgent need for the development of new drug candidates with newer targets and alternative mechanism of action. In this perspective, pyrazole, one of the most important classes of heterocycles, has been the topic of research for thousands of researchers all over the world because of its wide spectrum of biological activities. To pave the way for future research, there is a need to collect the latest information in this promising area. In the present review, we have collated published reports on the pyrazole core to provide an insight so that its full therapeutic potential can be utilized for the treatment of tuberculosis. In this article, the possible structure-activity relationship of pyrazole analogs for designing better antituberculosis (anti-TB) agents has been discussed and is also helpful for new thoughts in the quest for rational designs of more active and less toxic pyrazole-based anti-TB drugs.

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Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

Cited by 27 publications

References 13 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Current status of pyrazole and its biological activities

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

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