Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues

Ahsan, Mohamed Jawed; Samy, Jeyabalan Govinda; Khalilullah, Habibullah; Bakht, Mohamed Afroz; Hassan, Mohd. Zaheen

doi:10.1016/j.ejmech.2011.09.035

Cited by 31 publications

(17 citation statements)

References 13 publications

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“…SAR study reveals, 4‐chlorophenyl substitution on N ‐aryl group showed maximum inhibitory activity than 4‐nitrophenyl substitution or when there was no substitution (Fig. ) .…”

Section: Pyrazole Derivatives For Treatment Of Tuberculosismentioning

confidence: 99%

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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“…SAR study reveals, 4‐chlorophenyl substitution on N ‐aryl group showed maximum inhibitory activity than 4‐nitrophenyl substitution or when there was no substitution (Fig. ) .…”

Section: Pyrazole Derivatives For Treatment Of Tuberculosismentioning

confidence: 99%

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

Keri

Chand

Ramakrishnappa

et al. 2015

Archiv der Pharmazie

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“…[1][2][3][4][5][6][7][8] Earlier we have reported the antitubercular and anticonvulsant activities of some novel pyrazoline derivatives. [9][10][11][12] The present letter is the continuation of the previous work and we have focused here on the bioinformatics of the synthesized compounds with the help of computational method viz. Petra, Osiris, Molinspiration and ALOGPS and correlate the biological activities, and to identify the pharmacophores for antiviral and antibacterial activities.…”

Section: Introductionmentioning

confidence: 99%

POMA analyses as new efficient bioinformatics’ platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

Ahsan

Jeyabalan

Khalilullah

et al. 2012

Bioorganic & Medicinal Chemistry Letters

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“…Therefore, it is necessary to search for new antibiotic agents. Five member heterocyclic compounds such as pyrazole are important are important nitrogen containing compounds and numerous pyrazole derivatives have been found to possess considerable biological activities [6], such as antimicrobial [7][8][9], antiamoebic [10,11], antinociceptive [12], anticancer [13], antidepressant [14] and anti-inflammatory [15] . On the other hand, pyrazoline derivatives are also widely used in materials science fields such as non-linear optics (NLO) [16], optical limiting [17], electrochemical sensing [18], Langmuir films and photoinitiated polymerization [19].…”

Section: Introductionmentioning

confidence: 99%

Green synthesis of novel pyrazole containing Schiff base derivatives as antibacterial agents on the bases of in-vitro and DFT

et al. 2013

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A series of pyrazole containing Schiff bases were synthesized, by the reaction of 3,5-dimethyl-1-phenylpyrazole-4-carboxaldehyde and the corresponding active amines under microwave irradiation. The structures of the synthesized compounds were established by spectroscopic data (FT-IR, 1 H NMR, 13 C NMR and ESI-MS) and elemental analyses. The anti-bacterial activity of these compounds were tested in vitro by the disc diffusion assay against two Gram-positive and two Gram-negative bacteria, and then the minimum inhibitory concentration using chloramphenicol as reference drug. All the molecules were modeled and optimized by using density functional theory, DFT/B3LYP method. Calculated descriptors, the lower unoccupied molecular orbital and the density were used to interpret the antibacterial activity of the compounds. The results showed that compound 3 is better inhibitor of both types of test bacteria as compared to chloramphenicol.Pyrazole Schiff bases Chloramphenicol Antibacterial activity Density functional theory Minimum inhibitory concentration

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Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues

Cited by 31 publications

References 13 publications

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

Recent Progress on Pyrazole Scaffold‐Based Antimycobacterial Agents

POMA analyses as new efficient bioinformatics’ platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues

Green synthesis of novel pyrazole containing Schiff base derivatives as antibacterial agents on the bases of in-vitro and DFT

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