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Bioorganic Chemistry

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https://www.readbyqxmd.com/read/28087168/synthesis-structure-activity-relationships-studies-of-benzoxazinone-derivatives-as-%C3%AE-chymotrypsin-inhibitors
#1
Bishnu P Marasini, Fazal Rahim, Shahnaz Perveen, Aneela Karim, Khalid Mohammed Khan, Atta-Ur-Rahman, M Iqbal Choudhary
A series of benzoxazinones 1-28 were synthesized via reaction of anthranilic acid with various substituted benzoyl chlorides in the presence of triethylamine in chloroform. Compounds 1-18 showed a good inhibition of α-chymotrypsin with IC50±SEM values between 6.5 and 341.1μM. Preliminary structure-activity relationships studies indicated that the presence of substituents on benzene ring reduces the inhibitory potential of benzoxazinone. Also the increased inhibitory potential due to fluoro group at phenyl substituent was observed followed by chloro and bromo substituents...
January 4, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28069264/synthesis-in-vitro-%C3%AE-glucuronidase-inhibitory-activity-and-in-silico-studies-of-novel-e-4-aryl-2-2-pyren-1-ylmethylene-hydrazinyl-thiazoles
#2
Uzma Salar, Khalid Mohammed Khan, Shazia Syed, Muhammad Taha, Farman Ali, Nor Hadiani Ismail, Shahnaz Perveen, Abdul Wadood, Mehreen Ghufran
Current research is based on the synthesis of novel (E)-4-aryl-2-(2-(pyren-1-ylmethylene)hydrazinyl)thiazole derivatives (3-15) by adopting two steps route. First step was the condensation between the pyrene-1-carbaldehyde (1) with the thiosemicarbazide to afford pyrene-1-thiosemicarbazone intermediate (2). While in second step, cyclization between the intermediate (2) and phenacyl bromide derivatives or 2-bromo ethyl acetate was carried out. Synthetic derivatives were structurally characterized by spectroscopic techniques such as EI-MS, (1)H NMR and (13)C NMR...
December 31, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28069265/8-hydroxyirilone-5-methyl-ether-and-8-hydroxyirilone-new-antioxidant-and-%C3%AE-amylase-inhibitors-isoflavonoids-from-iris-germanica-rhizomes
#3
Sabrin R M Ibrahim, Gamal A Mohamed, Mohamed F Zayed, Samir A Ross
Iris species are well recognized as wealthy sources of isoflavonoids. In the present study, phytochemical investigation of the rhizomes of Iris germanica (Iridaceae) procure the isolation of two new isoflavonoids namely, 8-hydroxyirilone 5-methyl ether (2) and 8-hydroxyirilone (3), along with eight known isoflavonoids: irilone 4'-methyl ether (1), irilone (4), irisolidone (5), irigenin S (6), irigenin (7), irilone 4'-O-β-d-glucopyranoside (8), iridin S (9), and iridin (10). The isolated flavonoids were structurally characterized with the assist of comprehensive spectroscopic analyses (UV, IR, 1D and 2D NMR, and HRMS) and comparing with the published data...
December 30, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28057325/design-synthesis-and-biological-screening-of-some-novel-celecoxib-and-etoricoxib-analogs-with-promising-cox-2-selectivity-anti-inflammatory-activity-and-gastric-safety-profile
#4
Shahinda S R Alsayed, Heba A H Elshemy, Mohamed A Abdelgawad, Mahmoud S Abdel-Latif, Khaled R A Abdellatif
Two new series of 4,6-diaryl-3-cyanopyridine 4a-r and 1,3,5-triaryl-2-pyrazolines 6a-f and were prepared. The new compounds were evaluated for their in vitro COX-2 selectivity and in vivo anti-inflammatory activity. Compounds 4o,r and 6d,f had moderate to high selectivity index (S.I.) compared to celecoxib (selectivity indexes of 4.5, 3.14, 4.79 and 3.21, respectively) and also, showed in vivo anti-inflammatory activity approximately equal to or higher than celecoxib (edema inhibition %=60.5, 64.5, 59.3 and 59...
December 26, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28043717/protein-tyrosine-phosphatase-1b-inhibitors-as-antidiabetic-agents-a-brief-review
#5
REVIEW
Mansi Verma, Shyam Ji Gupta, Anurag Chaudhary, Vipin K Garg
Diabetes mellitus and obesity are one of the most common health issues spread throughout world and raised the medical attention to find the new effective agents to treat these disease state. Occurrence of the drug resistance to the insulin and leptin receptor is also challenging major issues. The molecules that can overcome this resistance problem could be effective for the treatment of both type II diabetes and obesity. Protein Tyrosine Phosphatase (PTP) has emerged as new promising targets for therapeutic purpose in recent years...
December 26, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28043716/synthesis-molecular-docking-studies-of-hybrid-benzimidazole-as-%C3%AE-glucosidase-inhibitor
#6
Nik Khairunissa Nik Abdullah Zawawi, Muhammad Taha, Norizan Ahmat, Nor Hadiani Ismail, Abdul Wadood, Fazal Rahim
Thiourea derivatives having benzimidazole 1-17 have been synthesized, characterized by (1)H NMR, (13)C NMR and EI-MS and evaluated for α-glucosidase inhibition. Identification of potential α-glucosidase inhibitors were done by in vitro screening of 17 thiourea bearing benzimidazole derivatives using Baker's yeast α-glucosidase enzyme. Compounds 1-17 exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 35.83±0.66 and 297.99±1.20μM which are more better than the standard acarbose (IC50=774...
December 26, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28043718/azomethine-based-nano-chemicals-development-in-vitro-and-in-vivo-fungicidal-evaluation-against-sclerotium-rolfsii-rhizoctonia-bataticola-and-rhizoctonia-solani
#7
Prithusayak Mondal, Rajesh Kumar, Robin Gogoi
Fungal diseases posing a severe threat to the production of pulses, a major protein source, necessitates the need of new highly efficient antifungal agents. The present study was aimed to develop azomethine based nano-fungicides for protecting the crop from fungal pathogens and subsequent yield losses. The protocol for the formation of nano-azomethines was generated and standardized. Technically pure azomethines were transformed into their nano-forms exploiting polyethylene glycol as the surface stabilizer...
December 24, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28041662/synthesis-characterization-in-vitro-cytotoxicity-and-antimicrobial-investigation-and-evaluation-of-physicochemical-properties-of-novel-4-2-methylacetamide-benzenesulfonamide-derivatives
#8
Mustafa Durgun, Hasan Turkmen, Gulay Zengin, Huseyin Zengin, Mehmet Koyunsever, Ismail Koyuncu
In this study, several sulfonamide derivatives, 4-(2-methylacetylamino)benzenesulfonamides were synthesized. Chemical structures of the derivatives were characterized by (1)H NMR, (13)C NMR, LC-MS-MS, UV-Vis, FTIR, photoluminescence and elemental analysis. Sulfanilamide was reacted with 2-bromopropionyl bromide, in the presence of pyridine, to form bromo-substituted sulfonamide key intermediates, which were subsequently treated with secondary amines to obtain novel sulfonamide derivatives. All the synthesized compounds were evaluated for in vitro antimicrobial activities and cytotoxicity...
December 24, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28043719/synthesis-characterization-anticancer-antimicrobial-and-carbonic-anhydrase-inhibition-profiles-of-novel-3ar-4s-7r-7as-2-4-e-3-3-aryl-acryloyl-phenyl-3a-4-7-7a-tetrahydro-1h-4-7-methanoisoindole-1-3-2h-dione-derivatives
#9
Umit M Kocyigit, Yakup Budak, Meliha Burcu Gürdere, Şaban Tekin, Tuğba Kul Köprülü, Fatih Ertürk, Kezban Özcan, İlhami Gülçin, Mustafa Ceylan
In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80...
December 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28040207/synthesis-characterization-and-pharmacological-evaluation-of-certain-enzymatically-cleavable-nsaids-amide-prodrugs
#10
Tilal Elsaman, Omar A A Aldeeb, Tarek Aboul-Fadl, Elnazeer I Hamedelneil
The presence of free carboxylic acid group in majority of non-steroidal anti-inflammatory drug (NSAIDs) is responsible from GI irritation. Coupling of the appropriate NSAIDs (diclofenac, naproxen, dexibuprofen and meclofenamic acid) 1-4, respectively with the appropriate amino acid ester 5 using dicyclohexylcarbodiimide afforded prodrugs 6-13. The structures of the prodrugs were verified based on spectral data. Chemical hydrolysis studies performed in three different non enzymatic buffer solutions at pH 1.2, 5...
December 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28038777/facile-synthesis-of-novel-substituted-aryl-thiazole-sat-analogs-via-one-pot-multi-component-reaction-as-potent-cytotoxic-agents-against-cancer-cell-lines
#11
Salma Mirza, Syeda Asma Naqvi, Khalid Mohammed Khan, Uzma Salar, M Iqbal Choudhary
In this study, twenty-five (25) substituted aryl thiazoles (SAT) 1-25 were synthesized, and their in vitro cytotoxicity was evaluated against four cancer cell lines, MCF-7 (ER(+ve) breast), MDA-MB-231 (ER(-ve) breast), HCT116 (colorectal) and HeLa (cervical). The activity was compared with the standard anticancer drug doxorubicin (IC50=1.56±0.05μM). Among them, compounds 1, 4-8, and 19 were found to be toxic to all four cancer cell lines (IC50 values 5.37±0.56-46.72±1.80μM). Compound 20 was selectively active against MCF7 breast cancer cells with IC50 of 40...
December 21, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28043720/discovery-of-imidazopyridine-derivatives-as-novel-c-met-kinase-inhibitors-synthesis-sar-study-and-biological-activity
#12
Yifei Yang, Yuan Zhang, LingYun Yang, Leilei Zhao, Lianghui Si, Huibin Zhang, Qingsong Liu, Jinpei Zhou
Receptor tyrosine kinase c-Met acts as an alternative angiogenic pathway in the process and contents of cancers. A series of imidazopyridine derivatives were designed and synthesized according to the established docking studies as possible c-Met inhibitors. Most of these imidazopyridine derivatives displayed nanomolar potency against c-Met in both biochemical enzymatic screens and cellular pharmacology studies. Especially, compound 7g exhibited the most inhibitory activity against c-Met with IC50 of 53.4nM and 253nM in enzymatic and cellular level, respectively...
December 19, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27939960/synthesis-and-in-vitro-anti-leishmanial-activity-of-4-arylpiperazin-1-yl-1-thiophen-2-yl-9h-pyrido-3-4-b-indol-3-yl-methanone-derivatives
#13
Penta Ashok, Subhash Chander, Larry M C Chow, Iris L K Wong, Rajnish Prakash Singh, Prabhat Nath Jha, Murugesan Sankaranarayanan
In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these reported analogues, compounds 7b, 7c, 7f, 7g, 7i, 7j, 7m, 7o displayed potent activity (15.55, 7.70, 7.00, 3.80, 14.10, 9.25, 3.10, 4.85μM, respectively) against L. donovani promastigotes than standard drugs miltefosine (15...
December 2, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27923497/in-vivo-anti-inflammatory-activity-and-docking-study-of-newly-synthesized-benzimidazole-derivatives-bearing-oxadiazole-and-morpholine-rings
#14
Ankita Rathore, Raja Sudhakar, Mohamed Jawed Ahsan, Abuzer Ali, Naidu Subbarao, Surender Singh Jadav, Sadiq Umar, M Shahar Yar
In search of potential therapeutics for inflammatory disease, we report herein the synthesis, characterization and anti-inflammatory activities of a new series of 1-{(5-substituted-1,3,4-oxadiazol-2-yl)methyl}-2-(morpholinomethyl)-1H-benzimidazoles (5a-r). The anti-inflammatory activity of the compounds was evaluated using carrageenan induced rat paw edema test. Some compounds showed excellent anti-inflammatory activity in carrageenan induced rat paw edema test. 1-{(5-(2-Chlorophenyl)-1,3,4-oxadiazol-2-yl)methyl}-2-(morpholinomethyl)-1H-benzimidazole (5g) showed maximum anti-inflammatory (74...
November 29, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27914694/synthesis-of-novel-chromenones-linked-to-1-2-3-triazole-ring-system-investigation-of-biological-activities-against-alzheimer-s-disease
#15
Mina Saeedi, Maliheh Safavi, Elahe Karimpour-Razkenari, Mohammad Mahdavi, Najmeh Edraki, Farshad Homayouni Moghadam, Mahnaz Khanavi, Tahmineh Akbarzadeh
In this work, novel chromenones linked to 1,2,3-triazole ring system were synthesized and evaluated for their anti-ChE activity. Among them, N-((1-(2-chlorobenzyl)-1H-1,2,3-triazol-5-yl)methyl)-8-methoxy-2-oxo-2H-chromene-3-carboxamide (6m) showed good anti-acetylcholinesterase activity (IC50=15.42μM). Also, compound 6m demonstrated neuroprotective effect against H2O2-induced cell death in PC12 neurons, however, it showed no beta-secretase (BACE1) inhibitory activity. Docking and kinetic studies separately confirmed dual binding activity of compound 6m since it targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE...
November 24, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27955923/thymidine-esters-as-substrate-analogue-inhibitors-of-angiogenic-enzyme-thymidine-phosphorylase-in-vitro
#16
Sumaira Javaid, Marium Ishtiaq, Muniza Shaikh, Abdul Hameed, M Iqbal Choudhary
Thymidine phosphorylase (TP) catalyzes the cleavage of thymidine into thymine and 2-deoxy-α-d-ribose-1-phosphate. Elevated activity of TP prevents apoptosis, and induces angiogenesis which ultimately leads to tumor growth and metastasis. Critical role of TP in cancer progression makes it a valid target in anti-cancer research. Discovery of small molecules as TP inhibitors is vigorously pursued in cancer therapy. In the present study, we functionalized thymidine as benzoyl ester to synthesize compounds 3-16...
November 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27912907/bioactivity-guided-isolation-of-anti-inflammatory-triterpenoids-from-the-sclerotia-of-poria-cocos-using-lps-stimulated-raw264-7-cells
#17
Seoung Rak Lee, Seulah Lee, Eunjung Moon, Hye-Jin Park, Hyun Bong Park, Ki Hyun Kim
Poria cocos Wolf (Polyporaceae) has been used as a medicinal fungus to treat various diseases since ancient times. This study aimed to investigate the anti-inflammatory chemical constituents of the sclerotia of P. cocos. Based on bioassay-guided fractionation using lipopolysaccharide (LPS)-stimulated Raw264.7 cells, chemical investigation of the EtOH extract of the sclerotia of P. cocos resulted in the isolation and identification of eight compounds including six triterpenoids, namely poricoic acid A (1), 3-O-acetyl-16α-hydroxydehydrotrametenolic acid (2), polyporenic acid C (3), 3β-hydroxylanosta-7,9(11),24-trien-21-oic acid (4), trametenolic acid (5), and dehydroeburicoic acid (6), as well as (-)-pinoresinol (7) and protocatechualdehyde (8)...
November 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27908538/antimalarial-activity-of-novel-4-aminoquinolines-active-against-drug-resistant-strains
#18
Srinivasarao Kondaparla, Awakash Soni, Ashan Manhas, Kumkum Srivastava, Sunil K Puri, S B Katti
In the present study we have synthesized a new class of 4-aminoquinolines and evaluated against Plasmodium falciparum in vitro (3D7-sensitive strain & K1-resistant strain) and Plasmodium yoelii in vivo (N-67 strain). Among the series, eleven compounds (5, 6, 7, 8, 9, 11, 12, 13, 14, 15 and 21) showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogues showed 100% suppression of parasitemia on day 4 in the in vivo mouse model against N-67 strain when administered orally...
November 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27894776/design-synthesis-cyclooxygenase-inhibition-and-biological-evaluation-of-new-1-3-5-triaryl-4-5-dihydro-1h-pyrazole-derivatives-possessing-amino-methanesulfonyl-pharmacophore
#19
Khaled R A Abdellatif, Wael A A Fadaly
A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole 10a-l was designed and synthesized via cyclization of chalcones 8a-f with 4-amino/methanesulfonylphenylhydrazine hydrochloride 9a-b. All the synthesized compounds were evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity, ulcerogenic liability and analgesic activity. All compounds were more COX-2 inhibitors than COX-1. While most compounds showed good anti-inflammatory activity, the trimethoxy derivatives (10a, 10b, 10g and 10h) were the most potent derivatives (ED50=55...
November 21, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27894775/synthesis-characterization-and-biological-studies-of-schiff-bases-derived-from-heterocyclic-moiety
#20
Angamaly Antony Shanty, Jessica Elizabeth Philip, Eeettinilkunnathil Jose Sneha, Maliyeckal R Prathapachandra Kurup, Sreedharannair Balachandran, Puzhavoorparambil Velayudhan Mohanan
Some new Schiff bases (H1-H7) have been synthesized by the condensation of 2-aminophenol, 2-amino-4-nitrophenol, 2-amino-4-methylphenol, 2-amino benzimidazole with thiophene-2-carboxaldehyde and pyrrole-2-carboxaldehyde. The structures of newly synthesized compounds were characterized by elemental analysis, FT-IR, (1)H NMR, UV-VIS, and single crystal X-ray crystallography. The in vitro antibacterial activity of the synthesized compounds has been tested against Salmonella typhi, Bacillus coagulans, Bacillus pumills, Escherichia coli, Bacillus circulans, Pseudomonas, Clostridium and Klebsilla pneumonia by disk diffusion method...
November 21, 2016: Bioorganic Chemistry
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