scholarly journals Analysis of Endophytic Bacterial Diversity From Different Dendrobium Stems and Discovery of an Endophyte Produced Dendrobine-Type Sesquiterpenoid Alkaloids

2022 ◽  
Vol 12 ◽  
Author(s):  
Shan-Shan Wang ◽  
Jia-Meng Liu ◽  
Jing Sun ◽  
Ya-Tao Huang ◽  
Nuo Jin ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Endophytic Bacteria ◽  
Pathogenic Bacteria ◽  
Pathogenic Fungi ◽  
Illumina Miseq ◽  
Antimicrobial Activities ◽  
Whole Genome Analysis ◽  
Significant Difference ◽  
Myrothecium Roridum

As the unique component of Dendrobium, dendrobine-type sesquiterpenoid alkaloids (DSAs) possess a variety of medicinal properties. It has been well documented that plant endophytes can in vitro synthesize secondary metabolites identical or similar to metabolites produced by their host plants. This study aimed to investigate the composition and distribution of endophytic bacteria of Dendrobium stems by Illumina MiSeq platform sequencing and cultivation-dependent methods and then to assess the potential for endophytic bacteria to produce DSAs. Results indicated that it was necessary to combine both cultivation-dependent and cultivation-independent methods to analyze the community structure of endophytic bacterial in plants comprehensively. The length of the Dendrobium stems influenced the endophytic bacterial community. The diversity and richness of endophytic bacteria in group J10_15cm of stems were the highest, which showed a significant difference from the other stem groups. However, there was no certain connection between the diversity and richness of endophytic bacteria and the content of dendrobine. It was most likely due to the influence of several specific endophytic bacteria genera, such as Sphingomonas and Rhodococcus. Athelia rolfsii, Myrothecium roridum, as pathogenic fungi, and Pectobacterium carotovorum subsp. actinidiae, as pathogenic bacteria of Dendrobium, were used to determine the antimicrobial activities. In these assays, six strains belonging to five genera showed antimicrobial activity against at least two phytopathogens. The strain BL-YJ10_15-29 (Paracoccus pueri THG-N2.35, 98.98%) showed the best antimicrobial activity against the three phytopathogens. In addition, 2 DSAs (6-hydroxydendrobine and nobilonine) were identified in the fermentation supernatant of the strain CM-YJ10_15-44 (Pseudomonas protegens CHA0, 99.24%), whereas the whole-genome analysis results further demonstrated that the precursors of the two DSAs [geranyl-PP and (E, E)-famesyl-PP] were synthesized mainly through the methyl-D-erythritol 4-phosphate pathway in this strain. This study provides new insight into the studies on the biosynthesis of DSAs and provides potential biocontrol bacteria.

scholarly journals Synthesis, characterization and microbial screening of some new methyl 4, 6-o-(4-methoxybenzylidene)-?-D-glucopyranoside Derivatives

2014 ◽  
Vol 37 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Sarkar MA Kawsar ◽  
Abul K MS Kabir ◽  
Mohammad M R Bhuiyan ◽  
Jannatul Ferdous ◽  
Mohammad S Rahman
Keyword(s):  
Pathogenic Bacteria ◽  
Pathogenic Fungi ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Additional Information ◽  
Fungal Phytopathogens ◽  
New Compounds ◽  
Academy Of Sciences ◽  
Derivatives Of

Regioselective pentanoylation of methyl 4,6-O-(4-methoxybenzylidene)-?-D-glucopyranoside by the direct acylation method provided the methyl 4,6-O-(4-methoxybenzylidene)-2-O-pentanoyl- ?-D-glucopyranoside in good yield. A number of 3-O-acyl derivatives of this 2-O-pentanoylation product were also prepared in order to obtain new compounds and also gather additional information for structure elucidation. The chemical structure of the newly synthesized compounds was characterized by analytical and spectral methods. Synthesized acylated derivatives of Dglucopyranoside were screened for in vitro antimicrobial activities against ten human pathogenic bacteria and four plant pathogenic fungi. The study revealed that the acylated products exhibited moderate to good antimicrobial activities. It was interesting to observe that the selected compounds were more sensitive against fungal phytopathogens than those of the bacterial strains. DOI: http://dx.doi.org/10.3329/jbas.v37i2.17554 Journal of Bangladesh Academy of Sciences, Vol. 37, No. 2, 145-158, 2013

scholarly journals IN VITRO SCREENING OF ANTIMICROBIAL ACTIVITY OF ETHANOLIC EXTRACT OBTAINED FROM FICUS LYRATA WARB. (MORACEAE) LEAVES

2016 ◽  
Author(s):  
H. Tkachenko ◽  
L. Buyun ◽  
Z. Osadovskyy ◽  
M. Truhan ◽  
Ye. Sosnowski ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Ethanolic Extract ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Traditional Use ◽  
Agar Disc ◽  
Ficus Lyrata

In the current investigation, screening of ethanolic extract obtained from Ficus lyrata leaves against pathogenic bacteria has been done in order to assess the antimicrobial activity aimed at detecting new sources of antimicrobial agents. The antimicrobial activity of the extract was determined using agar disc diffusion method. The antibacterial activity of leaf extract of F. lyrata was tested against human pathogenic bacteria — both Gram-positive (Staphylococcus aureus, methicillin-resistant S. aureus and Streptococcus pneumoniae) and Gram-negative strains (Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli). The results of this study provide evidence that the ethanolic extract of F. lyrata leaves has a mild antimicrobial activities, apparently, attributed to the presence of various secondary metabolites, which confirm the traditional use of this plant for the treatment of diseases caused by pathogens. These data allow us to suggest that the extracts of F. lyrata can be used to discover antibacterial substances for developing new pharmaceuticals to control clinically important pathogens responsible for severe disorders.

scholarly journals In vitro Antimicrobial Activity of Ethanolic Leaf Extracts of Hibiscus Asper Hook. F. and Hibiscus Sabdariffa L. on some Pathogenic Bacteria

2021 ◽  
Vol 2 (3) ◽  
pp. 1-12
Author(s):  
Joseph Olowo Arogbodo ◽  
Oyetayo Bolanle Faluyi ◽  
Festus Omotere Igbe
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Leaf Extract ◽  
Hibiscus Sabdariffa ◽  
Bacterial Isolates ◽  
Leaf Extracts ◽  
In Vitro Antimicrobial Activity ◽  
Significant Difference ◽  
Ethanolic Leaf Extract

Purpose: The study aims to assess the antimicrobial activity of ethanolic leaf extracts of Hibiscus asper and Hibiscus sabdariffa against eight bacterial isolates. Materials and Methods:  An in vitro Antimicrobial activity of ethanolic leaf extract of the two plants against eight nosocomical and pathogenic bacteria viz; Pseudomonas aeruginosa (PAE), Proteus vulgaris (PVU), Klebsiella aerogenes (KAE), Staphylococcus aureus (SAU), Bacillus cereus (BCE), Escherichia coli (ECO), Moraxella catarrhalis (MCA) and Salmonella typhi (STY) was carried out using agar well diffusion assay with the concentration range of 3.13 – 100 mg/mL. Results: H. asper and H. sabdariffa showed significant difference (p< 0.05) in antimicrobial activity against BCE over the rest of the isolates. Inhibition zone diameters exhibited by the isolates to ethanolic leaf extract of H. asper was in descending order of BCE (15.00 ± 1.00a) >ECO (11.67 ± 0.58b) >SAU (7.67 ± 0.58c) >PAE (6.67 ± 0.58d) >STY (5.67 ± 0.58e) while that of H. sabdariffa was in the order BCE (15.33 ± 1.15a) > MCA (11.33 ± 1.15b) > SAU (11.00 ± 1.00bc) > KAE (9.67 ± 0.58c) > PAE (8.00 ± 1.00d) >PVU (7.67 ± 0.57e). PVU, KAE and MCA were resistant to the extract of H. asper while only STY was resistant to that of H. sabdariffa. Conclusion: H. sabdariffa extract demonstrated higher antimicrobial activity against the selected bacterial isolates than H. asper. However, the two extracts minimum inhibition concentrations (MICs) ranged from 25 mg/mL to 12.5 mg/mL. This is worthy of further exploration by pharmacological industries in the formulation of potent broad spectrum antibiotics for combating the present health challenge due to antimicrobial resistance.

scholarly journals INVESTIGATION OF LIPOIDIAL CONTENTS AND THEIR ANTIMICROBIAL ACTIVITY OF FORSSKAOLEA VIRIDIS AND TRICHODESMA EHRENBERGII WILDLY DISTRIBUTED IN EGYPT

2021 ◽  
Author(s):  
Taha A.I. El Bassossy ◽  
Fatma Ali Ahmed
Keyword(s):  
Antimicrobial Activity ◽  
Fatty Acid ◽  
Methyl Ester ◽  
Fatty Acid Methyl Ester ◽  
Peer Review ◽  
Pathogenic Bacteria ◽  
Acid Methyl Ester ◽  
Antimicrobial Activities ◽  
Acid Methyl

Objective: The aim of this work was to assess the antimicrobial activity and investigation of lipoidial contents of F. viridis and T. ehrenbergii wildly distributed in Gebel Elba, Southeast of Egypt for the first time. Methods: The phytochemical investigation of the ether extracts of  F. viridis and T. ehrenbergii carried out by saponification of two lipoidial extracts and  using gas chromatography (GC) with reference standards. The antimicrobial activity of the ether extract was performed as in vitro studies by diffusion agar technique for selected +ve and –ve gram bacterial and fungal strains with reference used drug as a control. Results: The findings of this study revealed that the two lipoidial extracts have sufficient steroidal and fatty acid methyl ester compounds  where F. viridis contain (22) hydrocarbons, (6) sterols and (14) fatty acid methyl esters while, T. ehrenbergii contain (20) hydrocarbons, (5) sterols and (17) fatty acids where β-amyrin and stigmasterol and palmitic and Tricyclic acid were the major concentration of steroid and fatty acid methyl ester contents of F. viridis and T. ehrenbergii respectively. The lipoidial extract of F. viridis and T. ehrenbergii exhibited moderate antimicrobial activity against all tested strains as compared to reference used drug. Conclusion: It can be elicited that the ethereal extracts of two plants have moderate antimicrobial activity against selected strains.                                  Peer Review History: Received 20 November  2020; Revised 11 Decembe; Accepted 3 January, Available online 15 January 2021 UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:                           Comments of reviewer(s):         Average Peer review marks at initial stage: 5.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, [email protected] Dr. Mohamed Said Fathy Al-Refaey, University of Sadat City, Menofia, Egypt, [email protected] Similar Articles: ANTIMICROBIAL ACTIVITIES FOR HADHRAMI HONEY ON GROWTH OF SOME PATHOGENIC BACTERIA ANTIMICROBIAL AND ANTIOXIDANT ACTIVITY OF PSIDIUM GUAJAVA. (GUAVA) MEDICINAL PLANT LEAVES USED IN FOLK MEDICINE FOR TREATMENT OF WOUNDS AND BURNS IN HUFASH DISTRICT AL MAHWEET GOVERNORATE–YEMEN CHEMICAL COMPOSITION AND ANTIMICROBIAL ACTIVITY OF THE ESSENTIAL OILS OF FOUR VARIETIES OF LIPPIA MULTIFLORA IN BENIN IN-VITRO ANTIBACTERIAL ACTIVITY OF LACTOBACILLI METABOLITES LOADED HYDROGEL FORMULATIONS AGAINST PSEUDOMONAS AERUGINOSA

scholarly journals Phenolic Contents, in vitro Antioxidant and Antimicrobial Activities of Genista microcephala Coss. & Dur.

2018 ◽  
Vol 5 (2) ◽  
pp. 8-22
Author(s):  
Djamila Maanani ◽  
Narimane Segueni ◽  
Salah Rhouati ◽  
Yavuz Selim Çakmak ◽  
Maltem Asan-Ozusaglam ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Total Phenolic ◽  
In Vitro Tests ◽  
Phenolic Contents ◽  
Significant Difference ◽  
Total Antioxidant ◽  
Antioxidant And Antimicrobial Activities

Abstract This study was carried out to determine the phenolic contents as well as to evaluate the antioxidant and antimicrobial activities of Genista microcephala. Total phenolic and flavonoid compounds were quantified. Antioxidant activity was evaluated by various in vitro tests, including Ferric Ion Reducing Activity (FRP), Cuprac Ion Reducing Antioxidant Capacity (CUPRAC), and total antioxidant capacities (TAC). The antimicrobial activity of ethyl acetate and butanolic extracts of G. microcephala in addition of fatty acids content of different parts of the studied plant was evaluated against human pathogenic bacteria, fish bacteria and two yeast. The used methods were agar diffusion method and the determination of minimal bactericidal and fungicidal concentrations (MBC and MFC). No significant difference was found between the two used solvents on total phenolic content (TPC). While, difference in total flavonoid content (TFC) were found to be significant. Ethylene acetate extract was the most actif regarding antioxidant assay. The tested activity seems to be due to the high content of this extract on isoflavonoids. The tested extracts demonstrated the lowest inhibition concentration for B.cereus RSKK 863.

scholarly journals Comparative Antimicrobial Activities of some Monosaccharide and Disaccharide Acetates

2013 ◽  
Vol 5 (3) ◽  
pp. 515-525 ◽  
Author(s):  
M. M. Matin ◽  
M. M. H. Bhuiyan ◽  
A. Afrin ◽  
D. C. Debnath
Keyword(s):  
Pathogenic Bacteria ◽  
Pathogenic Fungi ◽  
Salmonella Typhi ◽  
Antimicrobial Activities ◽  
Shigella Dysenteriae ◽  
Curvularia Lunata ◽  
Sucrose Octaacetate ◽  
Antimicrobial Studies ◽  
Activity Structure

A number of furanose (2,4) and pyranose (5,7,9,11,13) acetates were prepared by direct acetylation method. For comparative antimicrobial studies sucrose octaacetate (14) was also prepared. All the compounds (1-14) were screened for in vitro antibacterial activity against ten human pathogenic bacteria viz. Bacillus subtilis, Bacillus cereus, Bacillus megaterium, Staphylococcus aureus, Escherichia coli, INABA ET (Vibrio), Pseudomonas species, Salmonella paratyphi, Salmonella typhi and Shigella dysenteriae. These compounds were also screened for in vitro antifungal activity against four pathogenic fungi viz. Aspergillus niger, Alternaria alternata, Curvularia lunata and Fusarium equiseti. The study revealed that the pyranose acetate derivatives (5,7,9,11,13) are more prone towards antimicrobial functionality than those of the furanose acetates (2,4) and sucrose octaacetate (14).  Keywords: Glucofuranose; Glucopyranose; Acetylation; Antimicrobial activity; Structure activity relationship (SAR).  © 2013 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.  doi: http://dx.doi.org/10.3329/jsr.v5i3.15695 J. Sci. Res. 5 (3), 515-525 (2013)

A new phenanthrene derivative from Entada abyssinica with antimicrobial and antioxidant properties

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Larissa M. Magnibou ◽  
Peron B. Leutcha ◽  
Billy T. Tchegnitegni ◽  
Steven C. N. Wouamba ◽  
Cyrille Y. F. F. Magne ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Methyl Ester ◽  
Crude Extract ◽  
Antioxidant Properties ◽  
Pathogenic Fungi ◽  
Antimicrobial Activities ◽  
Root Bark ◽  
Significant Activity ◽  
Dioic Acid

Abstract Entada abyssinica Steud. Ex A. Rich (Leguminosae) is a medicinal plant used traditionally for the treatment of infections. A phytochemical investigation of the methanol extract of E. abyssinica root bark led to the isolation of a new phenanthrene derivative named phenentada (1), together with seven known compounds (8 S, 13 E)-kolavic acid 15-methyl ester (2) and 8 S-kolavic acid 15-methyl ester (3) obtained as mixture, 8 S-kolavic acid 15-methyl ester (3), 8 S-kolavic acid 18-methyl ester (4), 13,14,15,16-tetranorclerod-3-ene-12,18-dioic acid (5), 1′,26′-bis-[(S)-2,3-dihydroxypropyl] hexacosanedioate (6), campesterol (7) and 3-O-β -d-glucopyranosylstigmasterol (8). Their structures were determined by NMR spectroscopy (1D and 2D), mass spectrometry (HRESIMS) and by comparison with previously reported data. The crude extract and some isolated compounds were evaluated for their in vitro antimicrobial activities by the microdilution method while, the antioxidant activity was evaluated by the DPPH methods. Regarding the antimicrobial activity, the crude extract showed significant inhibitory activities against bacteria strains (MIC 7.81–31.3 μg mL−1) and yeasts (MIC 15.6–31.3 μg mL−1) whereas all compounds tested exhibited significant activity against Staphylococcus epidermidis. Moreover, compounds 4, 5 and 6 and the mixture 2/3 showed significant antimicrobial activity on Candida parapsilosis strain (MIC = 3.12 μg mL−1), as well as selected antifungal property against candida pathogenic fungi strains. On the other hand, compounds (1) demonstrated the best bioactivities against Candida albicans and Salmonella enterica with MIC = 3.12 μg mL−1 while the mixture 2/3 appeared to have the highest inhibition on gram (+) bacteria strain S. epidermidis with MIC of 0.78 μg mL−1 and compound 5 (MIC = 1.56 μg mL−1) against the gram (−) bacteria strain. Furthermore, the SC50 values measured by the antioxidant test for all samples varied between 47.21 and 52.44 μg mL−1 for DPPH. These results support the traditional uses of E. abyssinica in the management of several diseases including the claim in the skin disease treatment. Additionally, here is reported the first time isolation of a phenanthrene derivative in the Fabaceae family to the best of our knowledge.

scholarly journals ANTIMICROBIAL ACTIVITY OF CALLYSPONGIA DIFFUSA (MARINE SPONGE) ASSOCIATED ENDOPHYTIC BACTERIA L STRAINS

2017 ◽  
Vol 9 (7) ◽  
pp. 90
Author(s):  
Vijayanand B. Warad ◽  
Prasanna Habbu ◽  
Rajesh Shastri
Keyword(s):  
Antimicrobial Activity ◽  
Marine Sponge ◽  
Pathogenic Bacteria ◽  
Antimicrobial Activities ◽  
Bioactive Metabolites ◽  
Haemolytic Activity ◽  
Chloroform Fraction ◽  
Callyspongia Diffusa

Objective: To screen the antimicrobial activity Of Callyspongia Diffusa (Marine Sponge) Associated Endophytic Bacterial Strains.Methods: We have isolated endophytic bacterias CDB-1 and CDB-2 from marine sponge Callyspongia diffusa and identified as Pseudomonas taiwanensis strain and Lysinibacillussphaericus strain respectively by the phylogenetic analysis. Fractions of CDB-1 and CDB-2 were screened for in vitro and in vivo antimicrobial activities against pathogenic bacteria and mycobacterium tuberculosis H37 RV strain by Minimum Inhibitory Concentration (MIC) method.Results: The lowest MIC against Kleibesella pnumoniae, Escherichia coli and Enterococcus feacalis was found to be 0.2 µg/ml and 0.4 µg/ml respectively for CDB-2. A significant antifungal activity was observed against Candida albicans (0.2-0.8 µg/ml) and Aspergillus niger (0.2-0.4 µg/ml). Further, Chloroform fraction of CDB-1 and ethyl acetate fraction of CDB-2 have shown significant anti-tubercular activity against the tested organism with MIC of 6.25µg/ml. This was supported by in vivo antimicrobial activity against K. Pneumonia infection in mice and least haemolytic activity against erythrocytes was observed. Compared to chloramphenicol.Conclusion: In this study, we have reported the marine natural species offer a rich source of bioactive metabolites that can exploit to develop novel, useful and potential therapeutic agents.

ANTIMICROBIAL ACTIVITIES OF METHANOL EXTRACT FROM UNIDENTIFIED SPONGE ASSOCIATED BACTERIA IN LEMUKUTAN ISLAND, KALIMANTAN BARAT

2009 ◽  
Vol 1 (2) ◽  
Author(s):  
Risa Nofiani ◽  
Siti Nurbetty ◽  
Ajuk Sapar
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Pathogenic Bacteria ◽  
Methanol Extract ◽  
Agar Medium ◽  
Antimicrobial Activities ◽  
Antimicrobial Compounds ◽  
Associated Bacteria ◽  
Minimum Inhibitory Concentrations ◽  
Sponge Associated Bacteria

<p>The increase of issues on the antibiotics resistant pathogenic bacteria has triggered high exploration for new antimicrobial compounds. One of the potential sources is sponge-associated bacteria. The aim of this study was to get sponge-associated bacteria extract containing antimicrobial activities. On the basis screening of antimicrobial activity using by streaking on agar medium, there were two potential isolates with antimicrobial activities namely LCS1 and LCS2. The two isolates were cultivated,then secondary metabolite product were extracted using methanol as a solvent. Minimum inhibitory concentrations (MICs) of extract LCS 1 were 1,000 μg/well for S. aureus, 950 μg/well for Salmonella sp.and 800 μg/well for Bacillus subtilis. Minimum inhibitory concentrations of extract LCS 2 were 500 μg/well for S. aureus, 1,050 μg/well for Salmonella sp., 750 μg/well for Bacillus subtilis, 350 μg/well for P. aeruginosa, 750 μg/sumur terhadap B. subtilis. Based on the MIC values, the two assay extracts have a relatively low antimicrobial activity.</p> <p>Keywords:Antimicrobial,Sponges associated bacteria,MICs</p>

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

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