Genetic Instability and Disease Progression of Indian Rett Syndrome Patients.

Rett syndrome (RTT) is the rare neurodevelopmental disorder caused by mutations in methyl CpG binding protein 2 (MECP2) gene with a prevalence of 1:10,000 worldwide. The hallmark clinical features of RTT are developmental delay, microcephaly, repetitive behaviours, gait abnormalities, respiratory abnormalities and seizures. Still, the understanding on the diagnosis of RTT among clinicians are less.

Molecular properties prediction, synthesis, and antimicrobial activity of bis(azolyl)sulfonamidoacetamides.

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.

Synthesis of Amido Sulfonamido Heteroaromatics Under Ultrasonication and Their Antimicrobial Activity.

A convenient and facile methodology for N-sulfonylation of heteroaryl amines with ethyl chlorosulfonylacetate in the presence of dispersed sodium in THF under ultrasonication is reported. The corresponding heteroaryl sulfonamido esters are directly condensed with heteroaryl amines to get amido sulfonamido heteroaromatics in the presence of a mild base in THF under ultrasonication. Utilization of easy reaction conditions, shorter reaction times, and isolation of products in high yields under ultrasonication make this process as economically viable.

Synthesis, Molecular Properties Prediction and Antimicrobial Activity of Imidazolyl Schiff Bases, Triazoles and Azetidinones.

Benzylidenehydrazinyl imidazoles (3) are prepared from 2-hydrazinyl imidazoles (2) on treatment with hydrazine. The imine functionality in 3 is utilized to develop 5'-aryl-N-(4-aryl-1H-imidazol-2-yl)-1H-1,2,3-triazol-1-amines (5) by 1,3-dipolar cycloaddition of diazomethane followed by aromatization with I in DMSO. Compounds 3 are also explored to prepare 4'-aryl-1-(4-aryl-1H-imidazol-2-ylamino)-3-chloroazetidin-2-ones (6) on treatment with chloroacetyl chloride.

Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles.

A new class of methylthio linked pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles were prepared under conventional and ultrasound irradiation methods. All the compounds were obtained in higher yields and in shorter reaction times in ultrasound irradiation method when compared with the conventional method. The title compounds were tested for antimicrobial activity.

Green approach for the synthesis of thiophenyl pyrazoles and isoxazoles by adopting 1,3-dipolar cycloaddition methodology and their antimicrobial activity.

A variety of N-((1,3-diphenyl-5-aryl-1H-pyrazol-4-yl)sulfonyl)thiophene-2-carboxamides (7) and N-((5-aryl-3-phenylisoxazol-4-yl)sulfonyl)thiophene-2-carboxamides (8) were prepared from (E)-N-(arylethenesulfonyl)thiophene-2-carboxamides (4) adopting 1,3-dipolar cycloaddition of nitrile imines and nitrile oxides generated from araldehyde phenylhydrazones and araldoximes in the presence of iodosobenzene and CTAB followed by oxidation with I in DMSO. The compounds 4f, 7e, 7f, 8e and 8f showed potential antibacterial activity against B. subtilis whereas 8e and 8f exhibited potential antifungal activity against A.

Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines.

A new class of mono and bis heterocycles - styryl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines, pyrrolyl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines and pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines were prepared from the synthetic intermediate Z-styrylsulfonylacetic acid adopting simple and well versed synthetic methodologies and studied their antimicrobial activity. Amongst all the tested compounds styryl thiadiazole 5c exhibited promising antimicrobial activity against Pseudomonas aeruginosa and Penicillium chrysogenum.

Does non-medical grade power cord compromise the safety of medical equipment?

A tertiary care 1000 bedded hospital contains more than 10,000 pieces of equipment worth approximately 41 million USD, while the power cords supplied along with the imported equipment do not comply with country-specific norms. Moreover, the local vendors procure power cords with type D/M plug to complete installation and also on-site electrical safety test is not performed. Hence, this project was undertaken to evaluate the electrical safety of all life-saving equipment purchased in the year 2013, referring to the guidelines of International Electrotechnical Commission 62353, the Association for the Advancement of Medical Instrumentation (AAMI) and National Fire Protection Association (NFPA)-99 hospital standard for the analysis of protective earth resistance and chassis leakage current.

Synthesis and antimicrobial activity of amino linked heterocycles.

Amino-linked benzoxazolyl/benzothiazolyl/benzimidazolyl quinazolines were prepared and their antimicrobial activity studied. The nitro-substituted benzothiazolyl quinazoline (8f) may be a potential antibacterial agent against Staphylococcus aureus and nitro-substituted benzimidazolyl quinazoline (9f) may be a potential antifungal agent against Aspergillus niger.

Synthesis and antimicrobial activity of amine linked bis- and tris-heterocycles.

A series of amine linked bis- and tris-heterocycles were prepared from heteroaryl cinnamamides and tested for antimicrobial activity. The compounds 11c and 12c exhibited excellent antibacterial activity while 12a and 12c displayed excellent antifungal activity.

Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole.

A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 μg/mL) and Penicillium chrysogenum (38 mm, MIC 12.

Synthesis and antimicrobial activity of (1,4-phenylene)bis(arylsulfonylpyrazoles and isoxazoles).

A new class of (1,4-phenylene)bis(arylsufonylpyrazoles and isoxazoles) were synthesized by 1,3-dipolar cycloaddition of nitrile imines and nitrile oxides to the 1,4-bis((E)-2-(arylsulfonyl)vinyl)benzenes in the presence of chloramine-T. Compound 7f exhibited pronounced antimicrobial activity.

Synthesis, antioxidant, and cytotoxic activities of N-azole substituted thiomorpholine derivatives.

A new class of N-azole substituted thiomorpholine derivatives were prepared and their antioxidant and cytotoxic activities were studied. The methyl substituted oxazolyl thiomorpholine dioxide 9b exhibited radical scavenging activity greater than the standard ascorbic acid. On the other hand, the thiazolyl thiomorpholine 10c having a chloro substituent on the aromatic ring was identified as a remarkable lead molecule for cytotoxic activity against A549 and HeLa cells, with IC50 values of 10.

Synthesis and antioxidant activity of styrylsulfonylmethyl 1,3,4-oxadiazoles, pyrazolyl/isoxazolyl-1,3,4-oxadiazoles.

A new class of mono and bis heterocycles-styrylsulfonylmethyl 1,3,4-oxadiazoles, pyrazolyl/isoxazolyl-1,3,4-oxadiazoles were prepared and studied their antioxidant activity. The compound methyl substituted 2-(p-methylphenylamino-sulfonylmethyl)-5-[Z-(p-methylstyrylsulfonylmethyl)]-1,3,4-oxadiazole displayed slightly higher antioxidant activity than the standard ascorbic acid.

Synthesis and antioxidant activity of bis and tris heterocycles.

A variety of bis heterocycles, oxazolyl/thiazolyl/imidazolyl oxadiazoles having a styryl sulfonylmethyl group at the 5-position of oxadiazole and tris heterocycles having a pyrrolyl/pyrazolyl sulfonylmethyl group at the 5-position of oxadiazole were prepared adopting simple and versatile synthetic methodologies. All the compounds were screened for their antioxidant activities. Compound 5b displayed radical scavenging activity in all the three methods greater than the standard ascorbic acid, whereas compounds 8b and 14b showed activities equal to the standard ascorbic acid.

Synthesis, antimicrobial and cytotoxic activities of sulfonamidomethane linked heterocycles.

A new class of sulfonamidomethane pyrrolyl-oxadiazoles/thiadiazoles and pyrazolyl-oxadiazoles/thiadiazoles was prepared from arylsulfonylaminoacetic acid hydrazides and E-cinnamic acid. The lead compounds were tested for antimicrobial and cytotoxic activities. The thiadiazole compounds having chloro substituent on the aromatic ring 4c, 8c and 10c exhibited comparable antibacterial activity against Pseudomonas aeruginosa and also antifungal activity against Penicillium chrysogenum.

Synthesis and antioxidant activities of acetamidomethylsulfonyl bis heterocycles-oxazolyl/thiazolyl/imidazolyl-1,3,4-oxadiazoles.

A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl-1,3,4-oxadiazoles, -thiazolyl-1,3,4-oxadiazoles, and -imidazolyl-1,3,4-oxadiazoles were synthesized from the synthetic intermediates, methyl 2-((4-aryloxazol-2-ylcarbamoyl)methylsulfonyl)acetate, methyl 2-((4-arylthiazol-2-ylcarbamoyl)methylsulfonyl)acetate, and methyl 2-((4-aryl-1H-imidazol-2-ylcarbamoyl)methylsulfonyl)acetate. All the title compounds were tested for their antioxidant activity. The oxadiazolylmethylsulfonyloxazolylacetamide displayed excellent radical-scavenging activity when compared with the standard ascorbic acid.

Synthesis and antioxidant activity of a variety of sulfonamidomethane linked 1,3,4-oxadiazoles and thiadiazoles.

A variety of sulfonamidomethane linked 1,3,4-oxadiazoles and 1,3,4-thiadiazoles were prepared and tested for antioxidant activity. The methyl substituted arylsulfonylaminomethyl-1,3,4-oxadiazole 9b showed excellent antioxidant activity.

Synthesis and antimicrobial activity of azole derivatives.

A new class of mono and bis heterocycles, sulfonylmethaneamido linked oxazoles, thiazoles, imidazoles, pyrrolyl oxazoles, pyrrolyl thiazoles and pyrrolyl imidazoles were prepared adopting simple and versatile synthetic methodologies. The compound chloro substituted imidazolyl styrylsulfonylacetamide is the most potent antimicrobial agent particularly against Pseudomonas aeruginosa and Penicillium chrysogenum.

Synthesis and antioxidant activity of a new class of mono- and bis-heterocycles.

A new class of mono- and bis-heterocycles, 2-arylsulfonylaminosulfonylmethyl-5-styrylsulfonylmethyloxadiazoles, pyrazolyl oxadiazoles, and isoxazolyl oxadiazoles, were synthesized and tested for their antioxidant activity. The styrylsulfonylmethyloxadiazole 5b showed good antioxidant activity when compared with the standard ascorbic acid.

N-(4-Chloro-phen-yl)-1-(5-{[(2-phenyl-ethen-yl)sulfon-yl]meth-yl}-1,3,4-oxadiazol-2-yl)methane-sulfonamide.

In the title compound, C(18)H(16)ClN(3)O(5)S(2), the dihedral angles between the oxadiazole ring and the phenyl and chloro-benzene rings are 23.4 (2) and 45.4 (2)°, respectively.

Synthesis, antimicrobial and cytotoxic activities of sulfone linked bis heterocycles.

A new class of sulfone linked bis heterocycles viz., pyrrolyl/pyrazolyl arylaminosulfonylmethyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, and 1,2,4-triazoles were prepared and tested for antimicrobial activity and cytotoxicity. The chloro-substituted compounds 5c, 8c and 14c showed comparable antibacterial activity to chloramphenicol against Pseudomonasaeruginosa and compound 5c exhibited comparable antifungal activity to ketoconazole against Penicilliumchrysogenum.

Synthesis and antioxidant activity of a new class of bis and tris heterocycles.

A series of novel heterocycles, bisbenzoxazolyl/benzothiazolyl/benzimidazolyl pyrazoles/isoxazoles/pyrimidines were synthesized and evaluated for their antioxidant activity. The bisbenzoxazolylisoxazole 10 exhibited good antioxidant activity when compared with the standard ascorbic acid.