- Synthesis and biological evaluation of sulfonamidooxazoles and β-keto sulfones: Selective inhibitors of 11β-hydroxysteroid dehydrogenase type I
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The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11β-HSD1 inhibitors and the serendipitous discovery of β-keto sulfones as potent 11β-HSD1 inhibitors are described here. These two classes of compounds are not active against 11β-HSD2 and therefore may have significant therapeutic potential for metabolic syndrome, type 2 diabetes and related metabolic dysfunctions.
- Xiang, Jason,Ipek, Manus,Suri, Vipin,Massefski, Walt,Pan, Ning,Ge, Ying,Tam, May,Xing, Yuzhe,Tobin, James F.,Xu, Xin,Tam, Steve
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- Molecular properties prediction, synthesis, and antimicrobial activity of bis(azolyl)sulfonamidoacetamides
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A library of bis(azolyl)sulfonamidoacetamides was prepared by the reaction of azolylsulfonylamines with azolylchloroacetamides in the presence of pyridine/4-(dimethylamino)pyridine (DMAP) under ultrasonication. The reaction proceeded well with DMAP, resulting in a higher yield of the products. The antimicrobial activity of the compounds indicated that N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl)amino}-2-oxoethyl)sulfamoyl]-4-phenylthiazol-2-yl}benzamide (22a), N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl]amino}-2-oxoethyl)sulfamoyl]-4-(4-chlorophenyl)thiazol-2-yl}benzamide (22c), and N-{5-[N-(2-{[4-(4-chloro-1H-pyrrol-2-yl)-1H-imidazol-2-yl]amino}-2-oxoethyl)sulfamoyl]-4-(4-chloro-phenyl)-1H-imidazol-2-yl}benzamide (24c) exhibited a low minimal inhibitory concentration (MIC) against Bacillus subtilis, equal to the standard drug, chloramphenicol. Compounds 22c and 24c also showed low MICs against Aspergillus niger, equal to the standard drug, ketoconazole. The molecular properties of the synthesized molecules were studied to identify druglikeness properties of the target compounds. On the basis of molecular properties prediction, 19a, 19b, 20b, 20c, 21a–c, 22b, 22c, and 23a–c can be treated as drug candidates.
- Siva sankar,Narendra babu,Rekha, Tamatam,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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- Synthesis, Characterization, and Antioxidant Activity of a New Class of Amido linked Azolyl Thiophenes
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A new class of amido linked azolyl thiophenes was prepared from the synthetic intermediates azolyl amines and 5-chlorothiophene-2-carbonyl chloride adopting conventional and ultrasonication methodologies. It was observed that the reaction took place in shorter reaction times with higher yields under ultrasonication. The structures of the synthesized compounds were characterized by spectral parameters and also tested for antioxidant activity. Among all the tested compounds, methoxy substituted oxazolyl thiophene carboxamide (8c) displayed promising antioxidant activity. Besides, the electron donating groups on the phenyl ring enhanced the antioxidant activity when compared with the electron withdrawing groups.
- Thatha, Sreenivasulu,Ummadi, Nagarjuna,Venkatapuram, Padmavathi,Adivireddy, Padmaja
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p. 1410 - 1418
(2018/06/20)
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- Synthesis and Antimicrobial Activity of Azolyl Pyrimidines
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A new class of azolyl pyrimidines linked by diamino sulfone moiety was prepared and studied their antimicrobial activity. Chloro-substituted and nitro-substituted thiazolyl pyrimidines (9c and 9e) showed excellent antibacterial activity against Bacillus subtilis, while imidazolyl pyrimidines (10c and 10e) exhibited promising antifungal activity against Aspergillus niger.
- Butta, Ragavendra,Donthamsetty V, Sowmya,Adivireddy, Padmaja,Venkatapuram, Padmavathi
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p. 524 - 530
(2017/02/03)
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000347
(2015/10/05)
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- Comparative material study and synthesis of 4-(4-nitrophenyl)oxazol-2-amine via sonochemical and thermal method
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The present paper deals with the synthesis of aminooxazole derivatives via thermal and ultrasonic methods using deep eutectic solvent as medium. It was observed that ultrasound-assisted method gave 90% yield in just 8 min as against 3.5 h required to get
- Singh, Balvant S.,Lobo, Hyacintha R.,Pinjari, Dipak V.,Jarag, Krishna J.,Pandit, Aniruddha B.,Shankarling, Ganapati S.
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p. 633 - 639
(2013/02/22)
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- A novel and efficient one pot synthesis of 2,4-disubstituted thiazoles and oxazoles using phenyltrimethylammoniumtribromide in ionic liquid
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A novel and efficient one-pot procedure has been described for synthesis of 2,4-disubstituted thiazoles and oxazoles from substituted ketones using phenyltrimethylammoniumtribromide as in situ brominating agent followed by reaction with thioamide/thiourea and amides/ureas, respectively in [bmim][BF4] ionicliquid. The advantages of the procedure include avoiding the handling of lacrymetric compounds, hazardous and toxic organic solvents along with good to excellent yield of the products.
- Muthyala, Manoj Kumar,Kumar, Anil
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p. 959 - 964
(2012/10/29)
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- Formation of Thioamide Derivatives from Reactions of Isothiocyanates with Oxazol-2-amines
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4-Substituted oxazol-2-amines react with isothiocyanates to give products having a thioamide function at C5.The reaction is considered to be an electrophilic process in competition with the usual reaction of the amino group with the isothiocyanate.The nature of the isothiocyanate and the type of substituent at C4 affect the amount of the thioamide product formed.Some chemical properties of the thioamides are also investigated.
- Crank, George,Khan, Humaid R.
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p. 447 - 458
(2007/10/02)
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