scholarly journals Synthesis and Biological Evaluation of Four New Ricinoleic Acid-Derived 1-O-alkylglycerols

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 113 ◽  
Author(s):  
René Pemha ◽  
Victor Kuete ◽  
Jean-Marie Pagès ◽  
Dieudonné Emmanuel Pegnyemb ◽  
Paul Mosset
Keyword(s):  
Antimicrobial Activity ◽  
Ricinoleic Acid ◽  
Alkyl Chain ◽  
Analysis Data ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Lead Compound ◽  
Elementary Analysis ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

A series of novel substituted 1-O-alkylglycerols (AKGs) containing methoxy (8), gem-difluoro (9), azide (10) and hydroxy (11) group at 12 position in the alkyl chain were synthesized from commercially available ricinoleic acid (12). The structures of these new synthesized AKGs were established by NMR experiments as well as from the HRMS and elementary analysis data. The antimicrobial activities of the studied AKGs 8–11 were evaluated, respectively, and all compounds exhibited antimicrobial activity to different extents alone and also when combined with some commonly used antibiotics (gentamicin, tetracycline, ciprofloxacin and ampicillin). AKG 11 was viewed as a lead compound for this series as it exhibited significantly higher antimicrobial activity than compounds 8–10.

scholarly journals Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Biomedicines ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 955
Author(s):  
Dimitris Matiadis ◽  
See-Ting Ng ◽  
Eric H.-L. Chen ◽  
Georgia Nigianni ◽  
Veroniki P. Vidali ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Therapeutic Strategy ◽  
Specific Inhibitor ◽  
Biological Evaluation ◽  
Lead Compound ◽  
Cleavage Activity ◽  
Curcumin Derivatives ◽  
Aβ Clearance ◽  
Activity Enhancement ◽  
Synthesis And Biological Evaluation

Background: Alzheimer’s disease (AD) involves impairment of Aβ clearance. Neprilysin (NEP) is the most efficient Aβ peptidase. Enhancement of the activity or expression of NEP may provide a prominent therapeutic strategy against AD. Aims: Ten hydroxylated monocarbonyl curcumin derivatives were designed, synthesized and evaluated for their NEP upregulating potential using sensitive fluorescence-based Aβ digestion and inhibition assays. Results: Compound 4 was the most active one, resulting in a 50% increase in Aβ cleavage activity. Cyclohexanone-bearing derivatives exhibited higher activity enhancement compared to their acetone counterparts. Inhibition experiments with the NEP-specific inhibitor thiorphan resulted in dramatic cleavage reduction. Conclusion: The increased Aβ cleavage activity and the ease of synthesis of 4 renders it an extremely attractive lead compound.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF SPIRO (INDOLE-THIAZOLIDINE) DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 71-74
Author(s):  
PRIYANKA NIVRUTTI SHINDE ◽  
MANISH ASHOK RASKAR
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Mercaptoacetic Acid ◽  
Ir Absorption ◽  
Absorption Bands ◽  
Synthesis And Biological Evaluation ◽  
Anhydrous Zncl2

Objective: The present study aims to synthesize and biological evaluation of Spiro-[Indole-Thiazolidine] derivatives as antimicrobial agents. Methods: The reaction sequence involves microwave-induced preparation of N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene)pyridine-4-carbohydrazide [3] from isoniazid [1] and isatin [2] followed by the cyclo condensation of [3] and mercaptoacetic acid under microwave condition to achieve the synthesis of spiro-[indole-thiazolidine] derivatives [4]. The resulting compounds were then allowed to react with various aromatic and heterocyclic aromatic aldehydes to afford arylidene derivatives [5a-l]. Result: Isoniazid (1) on condensation with isatin (2) in the presence of catalytic amount of glacial acetic acid furnished N-(2-oxo-1,2-dihydro-3’H-indol-3-ylidene) pyridine-4-carbohydrazide (3), which showed characteristic IR, absorption bands. Compound (3) underwent Spiro cyclization upon its reaction with mercaptoacetic acid in the presence of anhydrous ZnCl2 to form spiro-[indole-thiazolidine] compound (4). Compound (4) was then condensed with aromatic aldehydes to give arylidene derivatives (5a-l), which were characterized by IR and 1H NMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by the cup plate method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria.

Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents

2019 ◽  
Vol 4 (3) ◽  
pp. 152-158
Author(s):  
P.C. Burde ◽  
A.M. Rahatgaonkar
Keyword(s):  
Ionic Liquid ◽  
Ambient Temperature ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Biphasic System ◽  
Facile Synthesis ◽  
Convenient Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.

scholarly journals Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-N-substituted-hydrazinecarbothioamides

2012 ◽  
Vol 22 (4) ◽  
pp. 2014-2022 ◽  
Author(s):  
Subhas S. Karki ◽  
Amol A. Kulkarni ◽  
Sujeet Kumar ◽  
Suresh Kumar Veliyath ◽  
Erik De Clercq ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

scholarly journals Synthesis, spectral studies and biological activity of 2, 3-disubstituted imidazo [2, 1-b] benzothiazole derivatives

2018 ◽  
Vol 6 (01) ◽  
pp. 01-08
Author(s):  
Yashveer Singh ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Vivek Kumar Gupta ◽  
Monika Gupta
Keyword(s):  
Antimicrobial Activity ◽  
Catalytic Domain ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Thiazole Ring ◽  
Standard Drug ◽  
Atp Binding Site ◽  
Benzothiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

Benzothiazole is a heterocyclic compound formed by the fusion of benzene and thiazole ring. The moiety had been reported to act via competing with ATP binding site at the catalytic domain of tyrosine kinase. The present work involves the synthesis and biological evaluation of 4, 5 disubstituted imidazo [2, 1-b] benzothiazole derivatives. The antimicrobial activity of the synthesized derivatives was carried out against Gram + ve bacteria Staphylococcus aureus (MTCC 3160) and Gram –ve bacteria Bordetella bronchiseptica (MTCC 6838), Pseudomonas aeruginosa (T11) and fungal strains Candida albicans (MTCC 1637). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The compounds 6a1, 6a2, 6a3, 6b1 and 8a1 exhibited good antimicrobial activity against all the strains. The derivative 8a1 was further screened for anticancer activity against MCF-7 cell line using Doxorubicin as standard. The structures of the synthesized compounds were established by IR and NMR spectral studies.

scholarly journals Synthesis and biological evaluation of new Benzimidazole derivatives

2018 ◽  
Vol 29 (1) ◽  
pp. 107 ◽  
Author(s):  
Hadeel Majed ◽  
Firyal W. Askar
Keyword(s):  
Schiff Bases ◽  
Nmr Spectra ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Synthesis And Biological Evaluation

Agroup of benzimidazole derivatives bearing different heterocyclic moieties such as Schiff bases, 2-azetidinone and  4-thiazolidinone were efficiently prepared. The structures of the newly compounds were characterized by FTIRand ¹H NMR spectra. The synthesized compounds were evaluated for their antimicrobial activities against gram-positive and gram negative bacteria and fungi using the microdilution procedure.

scholarly journals Novel Substituted Indazoles towards Potential Antimicrobial Agents

2021 ◽  
Vol 37 (2) ◽  
pp. 508-512
Author(s):  
Jaganmohana Rao Saketi ◽  
S N Murthy Boddapati ◽  
Raghuram M ◽  
Geetha Bhavani Koduru ◽  
Haribabu Bollikolla
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Xanthomonas Campestris ◽  
Antimicrobial Agents ◽  
Evaluation Studies ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains

The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to goodin vitroantimicrobial activities.

scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLE-PYRAZOLE INTEGRATED CHALCONES AS ANTIOXIDANT AND ANTI-INFLAMMATORY AGENTS

2019 ◽  
pp. 311-315
Author(s):  
DNYANESHWAR SIRSAT ◽  
PRADEEP KATE ◽  
MADHUSUDAN BACHUTE
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Schmidt Reaction ◽  
Chemical Structures ◽  
1H Nuclear Magnetic Resonance ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

Objective: The objective of the present study was to synthesize the thiazole-pyrazole integrated chalcones and their in vitro antioxidant and anti- inflammatory evaluation. Methods: The designed hybrid thiazole-pyrazole integrated chalcones (3a-j) were synthesized by Claisen–Schmidt reaction of substituted 1-(4-methyl-2-phenylthiazol-5-yl) ethanone and substituted pyrazole aldehyde in the presence of 10% NaOH in ethanol solvent under reflux condition. The chemical structures of synthesized compounds were confirmed by IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high- resolution mass spectra. Results: All the title compounds were screened for their in vitro antioxidant and anti-inflammatory activity. The screening data indicated that tested compounds showed potent antioxidant activity with moderate anti-inflammatory potential. Conclusion: Antioxidant screening data reveal that most of the synthesized compounds possess excellent 1,1-diphenyl-2-picrylhydrazyl and NO radical scavenging activity. Most of the compounds found to possess marked anti-inflammatory potential by effectively inhibiting the heat-induced albumin denaturation.

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