Novel 1,3,4-Oxadiazole Derivatives of Dihydropyrimidinones: Synthesis, Anti-Inflammatory, Anthelmintic, and Antibacterial Activity Evaluation

2015 ◽  
Vol 53 (4) ◽  
pp. 1176-1182 ◽  
Author(s):  
Ambareen Shaikh ◽  
Jyotsna Meshram
Keyword(s):  
Antibacterial Activity ◽  
Activity Evaluation ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

Synthesis and anti-HIV Activity of New Benzimidazole, Benzothiazole and Carbohyrazide Derivatives of the anti-Inflammatory Drug Indomethacin

2011 ◽  
Vol 66 (9) ◽  
pp. 953-960 ◽  
Author(s):  
Najim A. Al-Masoudi ◽  
Nadhir N. A. Jafar ◽  
Layla J. Abbas ◽  
Sadiq J. Baqir ◽  
Christophe Pannecouque
Keyword(s):  
Phenyl Isothiocyanate ◽  
Reverse Transcriptase Inhibitors ◽  
Inflammatory Drug ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Further Development ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

There is an urgent need for the design and development of new and safer drugs for the treatment of HIV infection, active against the currently resistant viral strains. New derivatives of the non-steroidal anti-inflammatory drug indomethacin bearing benzimidazoles, benzothiazole, purine and pyridine residues 8 - 13 were synthesized with the aim of developing new non-nucleoside reverse transcriptase inhibitors (NNRTIs).Alternatively, new imine analogs 16 - 20 were synthesized from condensation of indomethacinyl hydrazide 15, prepared from the ester 14, with various ketone precursors. Treatment of 15 with phenyl isothiocyanate or triethyl orthoformate afforded the phenylcarbonothioyl and the oxadiazole derivatives 21 and 22, respectively. The new compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 10 were the most active in inhibiting HIV-2 and HIV-1, respectively, with EC50 ≥ 17.60 μgmL−1 and > 1.15 μgmL−1 (therapeutic indexes (SI) of ≥ 3 and < 1, respectively), and are leading candidates for further development.

The synthesis, anti-inflammatory and antimicrobial activity evaluation of novel thioanalogs of 3,4-dihydrothiopyrimidin-2(1H)-one derivatives of N-aryl urea

2012 ◽  
Vol 21 (12) ◽  
pp. 4252-4260 ◽  
Author(s):  
Rajesh H. Tale ◽  
Atish H. Rodge ◽  
Girish D. Hatnapure ◽  
Ashish P. Keche ◽  
Kalpana M. Patil ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Activity Evaluation ◽  
Anti Inflammatory ◽  
Derivatives Of

scholarly journals SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVE: DERIVED FROM CIPROFLOXACIN

2019 ◽  
pp. 205-209
Author(s):  
ANUJ SINGHAI ◽  
M.K. GUPTA
Keyword(s):  
Antibacterial Activity ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
Gram Negative ◽  
Oxadiazole Derivatives ◽  
Gram Negative Organisms ◽  
Derivatives Of

Objective: The purpose of this research is synthesized and evaluates different derivatives of oxadiazole. Methods: A novel series of substituted 1,3,4-oxadiazole derivative were synthesized by condensing different amine with 1-cyclopropyl-6-fluoro-7- (piperazin-1-yl)-3-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)quinolin-4(1H)-one (III) in the presence of formaldehyde. The structure of these novel synthesized compounds was characterized on the bases of physicochemical and spectral analysis. The title compounds (IVa-h) were screened for antibacterial activity by disc diffusion method. Results: Substituted 1,3,4-oxadiazole derivative was synthesized, characterized, and evaluated for antibacterial activity. Compounds IVa, IVd, IVe, IVf, and IV h showed enhance activities then ciprofloxacin against all Gram-positive and Gram-negative organisms. Compound IVe showed the highest activity against Staphylococcus aureus and compound IV showed the highest activity against Escherichia coli. Conclusion: The present study demonstrates the synthesis and characterization of 1,3,4-oxadiazole derivatives derived from ciprofloxacin. These compounds were evaluated for antibacterial activity against different Gram-positive and Gram-negative organism. In some cases, antibacterial activity is found to be enhanced as compared to standard drug ciprofloxacin.

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

Sign in / Sign up

Export Citation Format

Share Document