Medicinal and Process Chemistry: Recent submissions

Now showing items 341-360 of 531

Topological Descriptors in Modeling the Antimalarial Activity: N1-(7-Chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine as Prototype

Deshpande, Shreekant; Solomon, V R; Katti, S B; Prabhakar, Y S (2009)

The antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl) piperazine analogues is correlated to several descriptors from constitutional, topological, 2D autocorrelation, functional and empirical classes. ...
A convenient synthesis of chiral amino acid derived 3,4-dihydro-2H-benzo[b][1,4]thiazines and antibiotic Levofloxacin

Parai, M K; Panda, Gautam (2009)

A series of 3,4-dihydro-2H-benzo[b][1,4]thiazine derivatives 8a-g were synthesized via- a copper-catalyzed intramolecular N-aryl amination reaction on substituted 2-(2-bromophenylthio)-ethanamines which were synthesized ...
Design and Synthesis of 2-(2,6-Dibromo-phenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as Anti-HIV agents

Rawal, R K; Tripathi, R K; Katti, S B; Pannecouque, Christophe; Clercq, E D (2009)

A series of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones were designed, synthesized and evaluated as selective HIV-1 RT enzyme inhibitors. The results of the HIV-1 RT kit based assay and MT-4 cell tests showed ...
Is Feature Selection Essential for ANN Modeling?

Goodarzi, Mohammad; Deshpande, Shreekant; Murugesan, Vanangamudi; Katti, S B; Prabhakar, Y S (2009)

In modeling approaches, artificial neural networks (ANNs) have a special place to address the nonlinear phenomena or curved manifold. Often one or other feature selection approach is used prior to ANN to feed the input ...
CoMFA and CoMSIA studies on thiazolidin-4-one as anti-HIV-1 agents

Murugesan, Vanangamudi; Prabhakar, Y S; Katti, S B (2009)

Comparative molecular field analysis (CoMFA) and Comparative molecular similarity indices analysis (CoMSIA) were performed on thiazolidin-4-one class of compounds as HIV-1 Reverse Transcriptase (HIV-1 RT) inhibitors using ...
Tetrahydronaphthyl azole oxime ethers: the conformationally rigid analogues of oxiconazole as antibacterials

Bhandari, Kalpana; Srinivas, Nagarapu; Keshva, G B S; Shukla, P K (2009)

A series of novel (Z)- and (E)-2-imidazolo-/triazolo-methyl tetrahydronaphthyl oxime ethers (7-28) were synthesized as conformationally constrained analogues of oxiconazole and evaluated for antifungal and antibacterial ...
Application of phenolate ion-mediated intramolecular epoxide ring opening in the enantioselective synthesis of functionalized 2,3-dihydrobenzofuran and 1-benzopyran derivatives

Dinda, S K; Das, S K; Panda, Gautam (2009)

The enantioselective synthesis of 2-isopropenyl-2,3-dihydrobenzofurans, 4-(2,3-dihydrobenzofuran-2-yl)-2-methylbut-3-en-2-ols, 2-hydroxymethylchromans, and 4-chroman-2-yl-2-methyl-but-3-en-2-ols has been achieved using ...
Derivatives of human beta-Casein fragments (54-59) exhibit highly potent immunosuppressant activity.

Puri, A; Bhattacharya, M; Tripathi, L M; Haq, W (2009)

Human β-casein fragment (54-59) having the amino acid sequence Val-Glu-Pro-Ile-Pro-Tyr, has shown potent immunostimulant activity. Several analogs of this hexapeptide have been synthesized with modification at the N-terminal ...
Application of Nazarov cyclization to access [6-5-6] and [6-5-5]tricyclic core embedded New Heterocycles : An easy entry to structures related to Taiwaniaquinoids

Singh, Ritesh; Parai, M K; Panda, Gautam (2009)

A concise and general route to synthesize new class of [6-5-6] tricyclic core embedded polyheterocycles has been accomplished using diastereoselective Nazarov cyclization with an overall yield of 35-40%. Versatility of ...
Synthetic studies towards steroid-amino acid hybrids

Shagufta; Singh, Ritesh; Panda, Gautam (2009)

New prototype of natural steroid amino acid hybrid containing nine membered D-ring in the steroid skeleton has been synthesized from commercially available estrone using standard synthetic organic transformations. NaIO4 ...
An approach towards the total synthesis of (+)-epiquinamide and (+)-α-conhydrine from Garner aldehyde

Srivastava, A K; Das, S K; Panda, Gautam (2009)

A short and stereoselective route for the synthesis of 1-hydroxyquinolizidine, an advanced synthetic intermediate for the total synthesis of (+)-epiquinamide is presented. The key synthetic steps involve diastereoselective ...
Enantioselective synthesis of functionalized 1-benzoxepines by phenoxide ion-mediated 7-endo-tet carbocyclization of cyclic sulfates

Das, S K; Dinda, S K; Panda, Gautam (2009)

Asymmetric synthesis of 2,3-disubstituted-1-benzoxepines is described. Key steps include Sharpless asymmetric dihydroxylation of trans-α,β-unsaturated esters and phenoxide ion-mediated intramolecular 7-endo-tet carbocyclization ...
A new synthetic route to unsymmetrical 9-arylxanthenes

Das, S K; Singh, Ritesh; Panda, Gautam (2009)

A facile and general three-step synthetic route towards unsymmetrical 9-arylxanthenes has been developed. The reaction sequence involves nucleophilic substitution reaction of commercially available 2-fluorobenzaldehydes ...
Design, synthesis and antitubercular activity of compounds containing aryl and heteroaryl groups with alkylaminoethyl chains

Panda, Gautam; Parai, M K; Srivastava, A K; Chaturvedi, Vinita; Manju, Y K; Sinha, Sudhir (2009)

Aryl and heteroaryl derivatives with an alkylaminoethyl chain on the hydroxyl group of the benzene ring are prepared and evaluated against Mycobacterium tuberculosis H37Rv and showed the activity in the range of 3.12-25 ...
Aryloxy cyclohexyl imidazoles: a novel class of antileishmanial agents

Srinivas, Nagarapu; Palne, Shraddha; Nishi; Gupta, Suman; Bhandari, Kalpana (2009)

Thirteen novel aryloxy cyclohexane based mono and bis imidazoles were synthesized and evaluated in vitro as antileishmanials against L. donovani and cytotoxicity assessed. These compounds were better than the existing ...
Discovery of novel antileishmanial agents in an attempt to synthesize aplysinopsin pentamidine hybrid molecule

Porwal, Sharad; Chauhan, Shikha; Chauhan, P M S; Shakya, Nishi; Verma, Aditya; Gupta, Suman (2009)

In an attempt to synthesize pentamidine-aplysinopsin hybrid molecule 25, a lead molecule 8 (containing Z-configured aplysinopsin moiety) was identified for antileishmanial activity. Optimization of lead 8 provided 24 ...
Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents

Sharma, Moni; Chaturvedi, Vinita; Manju, Y K; Bhatnagar, Shalini; Srivastava, Kumkum; Puri, S K; Chauhan, P M S (2009)

Frequency of tuberculosis and malaria is progressively increasing worldwide. New emerging strain of bacterium and resistance to currently available drugs make this field more conscientious and alarming. In this connection ...
Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents

Kumar, Ashok; Srivastava, Kumkum; Kumar, S R; Puri, S K; Chauhan, P M S (2009)

Despite emergence of resistance to CQ and other 4-aminoquinoline drugs in most of the endemic regions, research findings provide considerable support that there is still significant potential to discover new affordable, ...
Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials

Sunduru, Naresh; Srivastava, Kumkum; Rajakumar, S; Puri, S K; Saxena, J K; Chauhan, P M S (2009)

In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activity. ...
Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4–aminoquinoline with potent antiplasmodial activity

Sunduru, Naresh; Sharma, Moni; Srivastava, Kumkum; Rajakumar, S; Puri, S K; Saxena, J K; Chauhan, P M S (2009)

Frequency of malaria and its resistance to chemotherapeutic options are emerging rapidly. To counter this problem, a series of 4–aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized ...

Now showing items 341-360 of 531

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