88369-50-0Relevant academic research and scientific papers
Antibacterial and enzyme inhibition screening of some new acetamide and azomethine derivatives
Rasool, Shahid,Rehman, Aziz-Ur,Abbasi, Muhammad Athar,Siddiqui, Sabahat Zahra,Shah, Syed Adnan Ali,Ahmad, Irshad,Afzal, Saira
, p. 2704 - 2710 (2016/03/08)
The synthesis of poly-functional moieties as one unit has been under consideration by the synthetic chemists to search out new potent molecules. 2-Chlorobenzoic acid (1) was converted to 5-(2-chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4) through a series of steps. This nucleophile was attached with different electrophiles, prepared by the reaction of aryl/alkyl amines with 2-bromoacetylbromide, in NaH/DMF to synthesize N-substituted-2-((5-(2-chlorophenyl)-1,3,4-Oxadiazol-2- yl)sulfanyl)acetamide, 7a-f. The molecule 4 was stepped to ethyl ester and carbohydrazide. The carbohydrazide was made to react with aryl carboxaldehydes in methanol to synthesize N'-substituted-2-(5-(2-chlorophenyl)-1,3,4-Oxadiazol-2-ylthio)acetohydrazide, 11a-i. The structures of all the molecules were corroborated through IR, 1H-NMR and EI-MS spectral data. Both the series were screened for antibacterial and enzyme inhibition activity.
Synthesis of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives and their cytotoxic activity
Kurumurthy, Chavva,Veeraswamy, Banda,Sambasiva Rao, Pillalamarri,Santhosh Kumar, Gautham,Shanthan Rao, Pamulaparthy,Loka Reddy, Velaturu,Venkateswara Rao, Janapala,Narsaiah, Banda
, p. 746 - 749 (2014/02/14)
A series of novel 1,2,3-triazole tagged pyrazolo[3,4-b]pyridine derivatives 3 and 4 were prepared respectively starting from 6-phenyl-4-(trifluoromethyl)- 1H-pyrazolo[3,4-b]pyridin-3-amine 1 via selective N-propargylation, followed by reaction with divers
N-substituted derivatives of 5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl-2- sulfanyl acetamide as valuable bioactive compounds
Rehman, Aziz-Ur,Gul, Samreen,Abbasi, Muhammad Athar,Nafeesa, Khadija,Siddiqa, Asia,Khan, Khalid Mohammed,Shahid, Muhammad,Subhani, Zinayyera
, p. 503 - 511 (2014/08/05)
In the described research work, a new series of N-substituted derivatives of 5-(4- chlorophenyl)-1,3,4-Oxadiazol-2-yl-2-sulfanyl acetamide has been synthesized. The synthesis was carried out by converting 4-chlorobenzoic acid (1) into ethyl 4-chlorobenzoate (2), 4- chlorobenzohydrazide (3) and then 5-(4-chlorophenyl)-1,3,4-Oxadiazol-2-thiol (4) respectively. The target molecules 6a-o were synthesized by reacting compound 4 with different N-alkyl/aryl substituted 2-bromoacetamide (5a-o) in equimolar ratios of using DMF and sodium hydride (NaH). The structure of all the synthesized compounds was confirmed by spectral data like EI-MS, IR and 1H-NMR. The compounds were also analysed for antimicrobial & hemolytic activity and most of them were found active against the selected microbial species at variable extent relative to reference standards. But 6f and 6o were the active against the selected panel of microbes and former was most potent one. This series revealed less toxicity and may consider for further biological screening and application trial except 6g and 6j, exhibiting high cytotoxicity.
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors
Wang, Zhiwei,Wu, Baogen,Kuhen, Kelli L.,Bursulaya, Badry,Nguyen, Truc N.,Nguyen, Deborah G.,He, Yun
, p. 4174 - 4177 (2007/10/03)
A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.
THERAPEUTICS
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Page/Page column 56, (2008/06/13)
The present invention relates to the use of a compound of formula (I); wherein: R1 comprises a carbonyl group and R2 is a hydrocarbyl group; optionally wherein said ring is further substituted; or a pharmaceutically acceptable salt thereof; in the manufacture of a medicament for use in one or more of: modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; modulating calcium spikes in mammalian cells; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes; treating diseases in one or more of brain, heart, pancreatic cells (e.g. pancreatic acinar and pancreatic beta cells), immune cells, T-cells, haemopoietic cells including phagocytes by modulating the release of intracellular calcium from a store controlled by nicotinic acid adenine dinucleotide phosphate; treating diseases in one or more of brain, heart, and T-cells by modulating calcium spikes in mammalian cells.
Compounds derived from an amine nucleus that are inhibitors of IMPDH enzyme
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, (2008/06/13)
The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.
Synthesis of New Arylbenzofurodiazepin-6-ones
Viti, Giovanni,Giannotti, Danilo,Nannicini, Rossano,Ricci, Renzo,Pestillini, Vittorio
, p. 1369 - 1375 (2007/10/02)
Two new tetracyclic structures, containing the diazepine ring, were synthesized: 5,6-dihydro-12H-benzofurobenzodiazepin-6-one and 5,6-dihydro-12H-benzofuropyridodiazepin-6-one.Thus N-(2-haloaryl)-2-acetamides were cyclized to the corresponding N-(2-haloaryl)-3-amino-2-benzofurancarboxamides and then, through the formation of the central diazepine ring, to the title compounds.Formation of the diazepine ring took place only when an electron-withdrawing group was present in the molecule to facilitate the nucleophilic attack of an amine in the benzofuran intermediate.
