Antibacterial Screening of Crude Fractions of Calotropis Procera (Linn) and Gc-Ms Profile of Fractions Obtained from the Extracts of Calotropis Procera

Aims: In this article we have developed an eco-friendly one-pot multi-component reaction methodology was employed for the green synthesis of functionalized pyrazole derivatives viz cyclo-condensation of aromatic aldehydes, ethyl acetoacetate and phenyl hydrazine and/or hydrazine hydrate in the presence of cetyltrimethylammoniumbromide (CTAB) at 90°C temperature in aqueous medium. Method: In the present protocol we developed a green method for the synthesis of functionalized pyrazole derivatives through one-pot, multi-component cyclo-condensation of aromatic aldehydes, phenyl hydrazine or hydrazine hydrate and ethyl acetoacetate using cetyltrimethylammoniumbromide (CTAB) as a catalyst in water as solvent. Our methodology confers advantages such as short reaction time, atom economy, purification of product without using column chromatographic and hazardous solvent. The reaction is being catalyzed by cetyltrimethylammoniumbromide (CTAB) and thus products are formed under the green reaction conditions. Results: Initially the reaction of benzaldehyde and phenylhydrazine with ethyl acetoacetate was carried out in water at room temperature in the absence of the catalyst; no product was obtained after 24 h (Table 1 entry 1). When the reaction was carried out using L-proline as catalyst in ethanol at 70°C the yield of product was 20. Conclusion: This research not only provides a green and efficient method for the synthesis of sulfinic esters but also shows new applications of electrochemistry in organic synthesis. We consider that this green and efficient synthetic protocol used to prepare sulfinic esters will have good applications in future. In conclusion, we have developed successfully a green and efficient one-pot multi-component methodology for the synthesis of substituted pyrazoles using CTAB as a catalyst in water as solvent with excellent yields. Purifications of compounds were achieved without the use of traditional chromatographic procedures. This methodology has advantages of operational simplicity, clean reaction profiles and relatively broad scope which make it more attractive for the diversity oriented synthesis of these heterocyclic libraries. In this methodology we suggest the further alternative possibility for formation of substituted pyrazoles. The compound 7h can be used as an anticancer drug in pharma industry.

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Total Synthesis and Antibacterial Screening of (±)-6,8-Dihydroxy-3- undecyl-3,4-dihydroisochromen-1-one: A Structural Analogue of Metabolites from Ononis natrix

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180502114402 ◽

2019 ◽

Vol 16 (3) ◽

pp. 245-248

Author(s):

Hummera Rafique ◽

Aamer Saeed ◽

Ehsan Ullah Mughal ◽

Muhammad Naveed Zafar ◽

Amara Mumtaz ◽

...

Keyword(s):

Total Synthesis ◽

Structural Analog ◽

Diffusion Method ◽

Bacterial Strains ◽

Antibacterial Screening ◽

Maximum Inhibition ◽

Bacillus Subtilus ◽

Hydrolysis Of ◽

Direct Condensation

Background: (±)-6,8-Dihydroxy-3-undecyl-3,4-dihydroisochromen-1-one is one of the structural analog of several substituted undecylisocoumarins isolated from Ononis natrix (Fabaceae), has been successfully synthesized by direct condensation of homopthalic acid (1) with undecanoyl chloride yields isochromen-1-one (2). Methods: Alkaline hydrolysis of (2) gave the corresponding keto-acid (3), which is then reduced to hydroxy acid (4) then its cyclodehydration was carried out with acetic anhydride to afford 3,4- dihydroisochromen-1-one (5). Followed by demethylation step, the synthesis of target 6,8- dihydroxy-7-methyl-3-undecyl-3,4-dihydroisocoumarin (6) was achieved. Results: In vitro antibacterial screening of all the synthesized compounds were carried out against ten bacterial strains by agar well diffusion method. Conclusion: Newly synthesized molecules exhibited moderate antibacterial activity and maximum inhibition was observed against Bacillus subtilus and Salmonella paratyphi.

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In Silico Appraisal, Synthesis, Antibacterial Screening and DNA Cleavage for 1,2,5-thiadiazole Derivative

Current Computer - Aided Drug Design ◽

10.2174/1573409915666190206142756 ◽

2019 ◽

Vol 15 (5) ◽

pp. 445-455 ◽

Cited By ~ 6

Author(s):

Suraj N. Mali ◽

Sudhir Sawant ◽

Hemchandra K. Chaudhari ◽

Mustapha C. Mandewale

Keyword(s):

Molecular Docking ◽

Dna Cleavage ◽

In Silico ◽

Oral Absorption ◽

Inhibition Mechanism ◽

Hydrogen Binding ◽

Docking Score ◽

Antibacterial Screening ◽

Mycobacteria Tuberculosis

Background: : Thiadiazole not only acts as “hydrogen binding domain” and “two-electron donor system” but also as constrained pharmacophore. Methods:: The maleate salt of 2-((2-hydroxy-3-((4-morpholino-1, 2,5-thiadiazol-3-yl) oxy) propyl) amino)- 2-methylpropan-1-ol (TML-Hydroxy)(4) has been synthesized. This methodology involves preparation of 4-morpholino-1, 2,5-thiadiazol-3-ol by hydroxylation of 4-(4-chloro-1, 2,5-thiadiazol-3-yl) morpholine followed by condensation with 2-(chloromethyl) oxirane to afford 4-(4-(oxiran-2-ylmethoxy)-1,2,5-thiadiazol- 3-yl) morpholine. Oxirane ring of this compound was opened by treating with 2-amino-2-methyl propan-1- ol to afford the target compound TML-Hydroxy. Structures of the synthesized compounds have been elucidated by NMR, MASS, FTIR spectroscopy. Results: : The DSC study clearly showed that the compound 4-maleate salt is crystalline in nature. In vitro antibacterial inhibition and little potential for DNA cleavage of the compound 4 were explored. We extended our study to explore the inhibition mechanism by conducting molecular docking, ADMET and molecular dynamics analysis by using Schrödinger. The molecular docking for compound 4 showed better interactions with target 3IVX with docking score of -8.508 kcal/mol with respect to standard ciprofloxacin (docking score= -3.879 kcal/mol). TML-Hydroxy was obtained in silico as non-carcinogenic and non-AMES toxic with good percent human oral absorption profile (69.639%). TML-Hydroxy showed the moderate inhibition against Mycobacteria tuberculosis with MIC 25.00 μg/mL as well as moderate inhibition against S. aureus, Bacillus sps, K. Pneumoniae and E. coli species. Conclusion: : In view of the importance of the 1,2,5-thiadiazole moiety involved, this study would pave the way for future development of more effective analogs for applications in medicinal field.

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Characterization of Antibacterial-Producing Endophytic Fungi of Syzygiumpolyanthum Leaves

Infectious Disorders - Drug Targets ◽

10.2174/1871526519666181226123541 ◽

2020 ◽

Vol 20 (4) ◽

pp. 448-454

Author(s):

Rahmita Burhamzah ◽

Gemini Alam ◽

Herlina Rante

Keyword(s):

Molecular Characterization ◽

Endophytic Fungi ◽

Morphological Characterization ◽

Test Method ◽

Analysis Method ◽

Nitrogen Base ◽

Rdna Genes ◽

Antibacterial Screening ◽

Planting Method

Background: Endophytic fungi live in plants’ tissue and can produce the same bioactive compounds as its host plant produces. Syzygiumpolyanthum leaves have known to be one of the antibacterial compound producers. Aim and Objective: This study aimed to characterize morphologically, microscopically, and molecularly the antibacterial-producing endophytic fungi of Syzygiumpolyanthum leaves. Methods: The isolation of endophytic fungi was done by fragment planting method on PDA medium. The antibacterial screening was performed using the antagonistic test as the first screening followed by the disc diffusion test method. The morphological characterization was based on isolate’s mycelia color, growth pattern, margin, and surface texture of the colony, while the microscopic characterization was based on its hyphae characteristics. The molecular characterization of the isolate was done by nitrogen base sequence analysis method on nucleotide constituent of ITS rDNA genes of the isolate. Results: The results found that isolate DF1 has antibacterial activity against E.coli, S.aureus, P.acne, and P.aeruginosa, with the greatest inhibition at 10% concentration of broth fermentation extract on S.aureus with a diameter of inhibition of 13.77 mm. Conclusion: Based on macroscopic, microscopic, and molecular characterization, DF1 isolate is similar to Ceriporialacerate.

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Response Surface Methodology towards Optimization of Calotropis Procera Essential oil Extraction by using Supercritical CO2.

The Natural Products Journal ◽

10.2174/2210315509666191122095706 ◽

2019 ◽

Vol 09 ◽

Author(s):

Hossein Zaeri ◽

Bahareh Kamyab Moghadas ◽

Bijan Honarvar ◽

Ali Shokuhi Rad

Keyword(s):

Response Surface Methodology ◽

Essential Oil ◽

Response Surface ◽

Extraction Time ◽

Calotropis Procera ◽

Retrieval Rate ◽

The Family ◽

Effects Of Temperature ◽

Carbon Dioxide Co2 ◽

Central Composite

: In this research, the extraction of essential oil from Calotropis Procera with the family name of Asclepiadaceae, by supercritical carbon dioxide (CO2) solvent has been investigated in detail, and the yield and chemical profile of the extracts achieved by this method were compared with those resulted by the conventional Hydro distillation method. To optimize the process parameters of CO2 supercritical extraction (SCE) of the Calotropis Procera, the Response Surface Methodology (RSM) with central composite design (CCD) was employed. The effects of temperature, pressure, and extraction time on the oil yield are considered for investigation. Results showed that the data were sufficiently fitted into the second-order polynomial model. The extraction conditions, including pressure, temperature, and extraction time, were studied between 150-200 bar, 40-50 ºC, and 50-100 min, respectively. The optimal conditions are achieved as the temperature of 47.19ºC, the pressure of 172.2 bar, and time of 86 minutes with the retrieval rate of 31.39%.

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Analytical profile of Arka Taila - An Ayurvedic oil based medicine used in Karnasrava (Otomycosis)

Journal of Ayurveda and Integrated Medical Sciences (JAIMS) ◽

10.21760/jaims.v2i3.8212 ◽

2017 ◽

Vol 2 (3) ◽

Author(s):

Komal D. Jani ◽

Dharmendra P. Jani

Keyword(s):

Quality Control ◽

Fungal Infections ◽

Curcuma Longa ◽

Calotropis Procera ◽

Control Parameters ◽

Scientific Evaluation ◽

Quality Control Parameters ◽

Quality Check ◽

Based Medicine ◽

Excessive Accumulation

Otomycosis denotes diffuse otitis externa due to fungal infections. The fungii are usually secondary invaders of the tissue rendered susceptible by bacterial infection, physical injury or excessive accumulation of cerumen in the external auditory canal. Karnasraava means discharge from ear which can be correlated with otorrhoea. Karnasraava (discharge) is one of symptom of otomycosis. Arka Taila has been mentioned in Shaarangadhara is very simple formula having ingredients i.e. Haridraa (Curcuma longa), Arka Patra Swarasa (Calotropis procera) and Sarshapa Taila (Brassica campetries). The quality control parameters resulted after scientific evaluation of Arka Taila can be used as reference standard for quality control or quality assurance of a pharmaceutical industry in order to have a proper quality check over its preparation and processing.

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Synthesis and Antibacterial Properties of Some 4-Amino Substituted 2-Phenyl-6H-5,1,3-benzothiadiazocines

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19961681 ◽

1996 ◽

Vol 61 (11) ◽

pp. 1681-1688 ◽

Cited By ~ 4

Author(s):

Michal Bodajla ◽

Štefan Stankovský ◽

Katarína Špirková ◽

Soňa Jantová

Keyword(s):

Mass Spectra ◽

Antibacterial Properties ◽

H Nmr ◽

Antibacterial Screening

Some 4-amino substituted 2-phenyl-6H-5,1,3-benzothiadiazocines (4a-4j) were prepared by cyclization of the corresponding N1-[N-(2-chloromethylphenyl)benzimidoyl]-N2-substituted thioureas (3a-3j). The IR,1H NMR and mass spectra of the title compounds are reported together with the results of antibacterial screening.

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