Design and synthesis of new quinoline hybrid derivatives and their antimicrobial, antimalarial and antitubercular activities

986-998All the molecules have been designed on the basis of previously reported active pharmacophores via molecular hybridization. A convenient protocol for the preparation of N-((2-(piperazin-1-yl) quinolin-3-yl)methyl)aniline derivatives via mutli-step synthesis has been described. Spectral analysis using Mass, 1H and 13C NMR spectral techniques have been studied in order to confirm the structure of synthesized end molecules. All synthesized compounds have been screened for in vitro antimicrobial, antimalarial and antitubercular activities. Structural activity relationship study (SAR) have also been discussed. Interestingly, target molecules are found to show good to excellent antibacterial, antifungal and antimalarial potency

Synthesis, docking study and biological evaluation of novel N-(1,3-benzothiazole-2-yl)-2-(pyridine-3-ylformohydrazido) acetamide derivatives

1721-1737A series of N-(1,3-benzothiazole-2-yl)-2(pyridine-3-ylformohydrazido acetamide derivatives have been synthesized by facile and efficient conventional method. The structures of the compounds have been elucidated with the aid of elemental analysis, IR, ESI-MS, and 1H and 13C NMR spectral data. Molecular docking revealed that synthesized derivatives and target proteins are actively involved in the binding pattern and had a significant correlation with biological activity. Molecular dynamics studies have also been performed and ADME parameters for the synthesized compounds determined. Biological evaluation of all synthesized compounds have been carried out in vitro for their antibacterial, antituberculosis and antifungal efficacy against various bacterial and fungal strains and H37Rv. The different studies indicate that newly synthesized compounds possess moderate to good biological activities

Data from: Green approach for synthesis of bioactive Hantzsch 1,4-dihydropyridine derivatives based on thiophene moiety via multicomponent reaction

A novel green and efficient one-pot multicomponent reaction of dihydropyridine derivatives was reported as having good to excellent yield. In the presence of the catalyst ceric ammonium nitrate (CAN), different 1,3-diones and same starting materials as 5-bromothiophene-2-carboxaldehyde and ammonium acetate were used at room temperature under solvent-free condition for the Hantzsch pyridine synthesis within a short period of time. All compounds were evaluated for their in vitro antibacterial and antifungal activity and, interestingly, we found that 5(b–f) show excellent activity compared with Ampicillin, whereas only the 5e compound shows excellent antifungal activity against Candida albicans compared with griseofulvin. The cytotoxicity of all compounds has been assessed against breast tumour cell lines (BT-549), but no activity was found. The X-ray structure of one such compound, 5a, viewed as a colourless block crystal, corresponded accurately to a primitive monoclinic cell

Reflection List

Reflection Lis

Design and synthesis of new quinoline hybrid derivatives and their antimicrobial, antimalarial and antitubercular activities

All the molecules have been designed on the basis of previously reported active pharmacophores via molecular hybridization. A convenient protocol for the preparation of N-((2-(piperazin-1-yl) quinolin-3-yl)methyl)aniline derivatives via mutli-step synthesis has been described. Spectral analysis using Mass, 1H and 13C NMR spectral techniques have been studied in order to confirm the structure of synthesized end molecules. All synthesized compounds have been screened for in vitro antimicrobial, antimalarial and antitubercular activities. Structural activity relationship study (SAR) have also been discussed. Interestingly, target molecules are found to show good to excellent antibacterial, antifungal and antimalarial potency. 

Supplementary Material for RSC Open Science 03.1.2017

Supplementary Material for RSC Open Science 03.1.201

CrystalStructure

CrystalStructur

Green synthesis of pyrazolo[4,3-<em>d</em>]isoxazol derivatives and their antimicrobial, antimalarial and antituberculosis evaluation

1033-1041This article deals with the synthesis of new pyrazolo[4,3-d]isoxazol derivatives by utilizing 3,4-disubstituted isoxazol-5(4H)-ones and thiosemicarbazide catalyzed by triethylamine in PEG-400 under MWI at 300 W as well as under thermal heating at 90°C. All the synthesized compounds have been characterized by various spectroscopic techniques such as 1H and 13C NMR, IR, ESI-MS and elemental analysis. All the synthesized compounds have been screened for antimicrobial, antimalarial and antituberculosis activities

Synthesis of pyrazolo[4ʹ,3ʹ:5,6]pyrano[2,3-<em>d</em>]pyrimidine derivatives and their antimicrobial, antimalarial and antituberculosis evaluation

997-1005This article deals with the synthesis of a new pyrazolo[4ʹ,3ʹ:5,6]pyrano[2,3-d]pyrimidine derivatives by the reaction of 1,4-dihydropyrano[2,3-c]-pyrazole-5-carbonitriles with ethyl cyanoacetate catalyzed by triethylamine (TEA) in ethanol under reflux conditions. All the synthesized compounds have been checked for their purity by melting point and TLC, and have been characterized through various spectroscopic techniques such as 1H and 13C NMR, IR, ESI-MS and elemental analysis. All synthesized compounds have been screened for antimicrobial, antimalarial and antituberculosis activity

An efficient synthesis of novel carbohydrate and thiosemicarbazone hybrid benzimidazole derivatives and their antimicrobial evaluation

604-612<span style="font-size:11.0pt;font-family: " times="" new="" roman";mso-fareast-font-family:"times="" roman";mso-bidi-font-family:="" mangal;mso-ansi-language:en-gb;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-GB">A library of thiosemicarbazide hybrid <span style="font-size:11.0pt; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" mso-bidi-font-family:mangal;mso-ansi-language:en-in;mso-fareast-language:en-us;="" mso-bidi-language:hi"="">2-(aldo-polyhydroxyalkyl)benzimidazole derivatives have been designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds have been elucidated with the aid of elemental analysis, IR, mass and 1H NMR spectral data. These novel synthesized compounds have been evaluated for their antibacterial activity against two gram-positive bacteria (S. aureus and S. pyogenus) and two gram-negative bacteria (P. aeruginosa and E. coli). The title compounds have also been studied for their antifungal activity against C. albicans, A. niger and A. clavatus using the broth dilution technique.</span