Antitubercular Research Papers - Academia.edu (original) (raw)

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- Chemistry, Organic Chemistry, Antitubercular, Mannich base

In an attempt to find a new class of antimicrobial and antitubercular agent, a new series of chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus were synthesized with appropriate chemical reagent. Chalcones (D1-D5) were synthesized by the classical Claisen-Schmidt condensation of substituted ketone (C) with variously substituted aldehydes via conventional method. Now treatment of chalcones with hydrazine hydrate/glacial acetic acid and guanidine hydrochloride/Alkali afforded the corresponding acetyl pyrazoline (E1-E5) and amino pyrimidine (F1-F5) derivatives respectively. The chemical structures of all newly synthesized compounds were established on the basis of their FTIR, 1H NMR, 13C NMR, LC-MS as well as elemental analysis. All the newly design compounds were assayed for their in vitro antimicrobial activity against selected pathogens by the Broth dilution method and in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using Lowenstein-Jensen MIC method. Most of the compounds showed appreciable antimicrobial activity against the all tested strains. Among the synthesized compounds D1, D2, D3, E1, E3, E4, F3 and F4 exhibited excellent antimicrobial activity and said to be the most proficient members of the series. Compound D5 and F5 exhibited promising antitubercular activity.

- by Chemistry International
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- Organic Synthesis, Antitubercular, Antimicrobial activity, Bioactivity

Despite the hepatotoxic effects of Rifampicin (RIF), its use is inevitable in the management of tuberculosis. No satisfactory treatment is available for prevention of this adverse effect. This study was undertaken to evaluate the protective effect of Nigella sativa extract (NSE) against Rifampicin induced subchronic hepatotoxicity. Male wistar rats were divided in 4 groups of 8 each and received vehicle, RIF (100 mg/ kg), RIF (100 mg/kg)+NSE (250 mg/kg) or RIF (100 mg/kg)+NSE (500 mg/kg) orally respectively for 28 days. Blood was withdrawn at day 14 and 28 for estimation of circulatory liver markers and anti-oxidant levels. At the end of the experiment histopathological study and estimation of SOD, CAT, GSH and LPO in liver samples was done. Pre-treatment of NSE produced significant hepatoprotection by decreasing the level of serum Alkaline phosphatase (ALP) (p<0.01), Serum glutamic pyruvic transaminase (SGPT) (p<0.001), Serum glutamic oxaloacetic transaminase (SGOT) (p<0.001), serum bilirubin (p<0.01), and liver MDA (p<0.05) levels by increasing the level of SOD (p<0.01), CAT (p<0.01), and GSH (p<0.001). Liver histopathology showed mononuclear infiltration, degenerative changes in hepatocytes, bridging necrosis extending from one portal tract to another along with portal triditis and microvesicular steatosis. Pre-treatment group of NSE (500 mg/kg) showed near normal liver architecture with microvesicular steatosis. Pre-treatment groups of NSE (250 mg/kg) showed near normal regaining of architecture of liver with persisting fatty degeneration in the portal tract. The results indicate that NSE possesses hepatoprotective action against RIF induced sub chronic hepatoxicity. Further research is needed to advocate its use in prevention of drug induced hepatotoxicity.

- by Ali Ahmad
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- Pharmacology, Tuberculosis and Infectious Disease, Medicinal Plants, Hepatology

Seven different plants from Nigerian herbs were investigated for antiinfective properties. The plant crude extracts, obtained by maceration with methanol, were subjected to array of antimicrobial screening tests. Antimycobacterial susceptibility of M. tuberculosis (H37Rv strain) was performed by Alamar Blue Assay. The results showed Spondias mombin and Anacardium occidentale to have 68 and 63% inhibition respectively against P. aeruginosa (ATCC 27853). The secondary test on the S. mombin extract against P. aeruginosa had IC 50 of 37.32μg/ml. Two EtOAC-MeOH soluble fractions of exhibited good antimicrobial activities. One fraction (AOF9) exhibited antifungal activity against Candida glabrata with IC 50 value of 9.0µg/ml while the other fraction (AOF8) showed antibacterial activity against Pseudomonas aeruginosa with IC 50 value of 28.3µg/ml. The result of the antimycobacterial screening tests proved Spondias mombin most potent for providing antiturbercular compounds and was further investigated by HPLCbased activity profiling. The HPLC fractions revealed SM8-9, SM14 and SM15 to be effective (94.9, 98.3 and 92.8% Inhibitions respectively) against M. tuberculosis H37RV as compared with reference drugs. The findings show Spondias mombin and Anacardium occidentale to possess good anti-infective potentials and these support the folkloric uses of the plants for the treatment of infectious diseases.

- by Am Jour of Phytomed & Clinical Therapeut
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- Pharmacology, Microbiology, Pharmacy, Antitubercular

- by Anjani Solankee
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- Organic Synthesis, Antitubercular, Antimicrobial activity, Chalcones

A series of 1,3,4-oxadiazole and pyrazole derivatives have been synthesized and evaluated for antitubercular activity. All the structures of the newly synthesized compounds have been supported by IR, 1 H NMR, MS and CHN analysis. All the... more

- by Atheer Majeed
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- Chemistry, Organic Chemistry, Antitubercular, Mannich base

- by Anjani Solankee
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- Chemistry, Organic Synthesis, Antitubercular, Antimicrobial activity

- by Anjani Solankee
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- Organic Synthesis, Antitubercular, Antimicrobial activity, Chalcones

A series of triazines have been synthesized starting from 5-alkyl-1,3,4-thiadiazole-2-thioles (1a-d). On reaction with ethyl bromoacetate in the presence of anhydrous K 2 CO 3 under microwave irradiation (MWI), these yielded corresponding esters (2a-d) which on hydrazinolysis under MWI produced (5-alkyl-1,3,4-thiadiazol-2-yl sulfanyl) acetohydrazides (3a-d). The reaction of 3a-d with-bromoacetophenone under MWI yielded 6-aryl-3-[(5-alkyl-1,3,4-thiadiazol-2-yl sulfanyl)methyl]-1,2,4-triazines (4a-h). All the synthesized triazines showed in vitro antitubercular activity.

In an attempt to find a new class of antimicrobial and antitubercular agent, a new series of chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5-triazine nucleus were synthesized with appropriate chemical reagent. Chalcones (D 1-D 5) were synthesized by the classical Claisen-Schmidt condensation of substituted ketone (C) with variously substituted aldehydes via conventional method. Now treatment of chalcones with hydrazine hydrate/glacial acetic acid and guanidine hydrochloride/Alkali afforded the corresponding acetyl pyrazoline (E 1-E 5) and amino pyrimidine (F 1-F 5) derivatives respectively. The chemical structures of all newly synthesized compounds were established on the basis of their FTIR, 1 H NMR, 13 C NMR, LC-MS as well as elemental analysis. All the newly design compounds were assayed for their in vitro antimicrobial activity against selected pathogens by the Broth dilution method and in vitro antitubercular activity against Mycobacterium tuberculosis H 37 Rv using Lowenstein-Jensen MIC method. Most of the compounds showed appreciable antimicrobial activity against the all tested strains. Among the synthesized compounds D 1 , D 2 , D 3 , E 1 , E 3 , E 4 , F 3 and F 4 exhibited excellent antimicrobial activity and said to be the most proficient members of the series. Compound D 5 and F 5 exhibited promising antitubercular activity. Capsule Summary: 1,3,5-Triazine based some new chalcones, acetyl pyrazolines and aminopyrimidines were synthesized by conventional route which exerted good antimicrobial as well as antitubercular activity.

- by Chemistry International
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- Antitubercular, Antimicrobial activity, Chalcones, Antimicrobial

Infectious diseases including bacterial, fungal and tuberculosis are responsible for the suffering of humans worldwide. Based on this observation we predetermined to prepare and five novel lipophilic diarylpropenones (Chalcones) (3a-3e) against tubercular, bacterial and fungal strains. The compounds were prepared by base the catalyzed condensation of 2,4,6-trimethyl acetophenone with substituted aromatic aldehydes, purified by recrystallization and characterized by elemental analysis and IR, 1H NMR, and Mass spectroscopic techniques. Further, the compounds were biologically screened for their antitubercular, antibacterial, and antifungal actions. Results of these activities revealed that the compounds possess potential antifungal and antitubercular activities and poor antibacterial activity. The greater activities against tubercular and fungal strains may be due to the lipophilicity rendered by the three magic methyl groups and halogen atoms. The compounds showed no cytotoxicity against the normal human cell line L02. These compounds may act as new scaffolds for the design and development of new molecules against tubercular and fungal infections. Advanced studies need to be carried out in order to determine their potency in vivo.

- by Afzal Shaik
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- Antitubercular, Chalcones, Antifungal Activity, Antibacterial activity