S. Nanjunda Swamy

Synthesis and evaluation of 1-benzhydryl-sulfonyl-piperazine derivatives as inhibitors of MDA-MB-231 human breast cancer cell proliferation

A series of novel 1-benzhydryl-sulfonyl-piperazine derivatives 7(a-e) were designed by a nucleophilic substitution reaction of 1-benzhydryl-piperazine with various sulfonyl chlorides and characterized by 1H nuclear magnetic resonance (NMR), liquid chromatography mass spectrometry (LC/MS), Fourier-transform infrared (FTIR), and elemental analysis. Our research is focused on identifying synthetically occurring chemotherapeutic substances capable of inhibiting, retarding, or reversing the process of multistage carcinogenesis. The title compounds were evaluated for their efficacy in inhibiting MDA-MB-231 breast cancer cell proliferation. Compound 1-benzhydryl-4-(4-tert-butyl-benzenesulfonyl)-piperazine (7d) showed significant inhibitory activity.

N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde Derivatives as Anti-tumor Agents Against Ehrlich Ascites tumor Cells In Vivo

A new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives were synthesized by using the different bioactive heteroaralkyl halides with 2-butyl-4-chloro-1H-imidazole-5-carbaldehyde in presence of powdered potassium carbonate in DMF medium. These compounds were screened for their antitumor activity. Our results show that treatment of imidazole derivatives inhibit proliferation EAT cells, decreases the ascites volume and increases the survivability of the animals in vivo. These compounds also inhibited the cellular proliferation of HUVEC cells in vitro by MTT assay. Further, these compounds could induce apoptosis, which is evident by the nuclear condensation of imidazole derivatives treated EAT cells in vivo by the cytological analysis. We have identified that pyrrolidine substituted imidazole derivative as potent anti-tumor compound. These inhibitors could represent as promising candidates for anticancer therapies, where the formation of peritoneal malignant ascites is a major cause of morbidity and mortality.

Synthesis and antimicrobial activity of 1-benzhydryl-sulfonyl-4-(3-(piperidin-4-yl) propyl)piperidine derivatives against pathogens of Lycopersicon esculentum: a structure-activity evaluation study.

Several 1-benzhydryl-sulfonyl-4-(3-(piperidin-4-yl)propyl)piperidine derivatives 8(a–j) were prepared by the treatment of substituted benzhydryl chlorides with 4-(3-(piperidin-4-yl)propyl)piperidine followed by N-sulfonation with sulfonyl chlorides in the presence of dry methylene dichloride and triethyl amine. The synthesized compounds were characterized by 1H-NMR, IR, and elemental analysis. All the synthesized compounds were evaluated in vitro for their efficacy as antimicrobial agents by artificial inoculation technique against standard strains of two important bacterial viz., Xanthomonas axonopodis pv. vesicatoria and Ralstonia solanacearum as well as and two fungal pathogens namely Alternaria solani and Fusarium solani of tomato plants. We have briefly investigated the structure-activity relation studies and reveal that the nature of substitutions on benzhydryl ring and sulfonamide ring influences the antibacterial activity. Among the synthesized new compounds 8b, 8d, 8g, 8h, 8i, and 8j were showed significant potent antimicrobial activities compared to the standard drugs Chloramphenicol, Mancozeb.

Microwave-Assisted Solvent-Free Synthesis of N-alkyl Benzotriazole Derivatives: Antimicrobial Studies

To elucidate further our structural activity relation on the chemistry and antimicrobial activity, a series of novel N-alkylated benzotriazole derivatives bearing pharmaceutically important substituted biphenyl and benzyl halides were synthesized. The synthesized compounds were characterized and tested for in vitro antimicrobial activities by MIC determination against a panel of susceptible and resistant Gram-positive and Gram-negative microorganisms. The synthesis has been carried out using microwave irradiation method with solvent and without solvent. The obtained results showed high yields. Interestingly, compounds 2a and 2b showed a two fold increased antibacterial activity than the standard drug tested and the compounds 2d and 2e showed potent antifungal activity than the standard drug tested.

Crystal and Molecular Structure Analysis of 1,2,4-Triazolo-N-amino-thiols

The compound 4-amino-5-(4-methyl)-4H-[1,2,4]-triazole-3-thiol [AMT], C3H6N4S, crystallizes in the orthorhombic space group Pca21 with cell parameters a = 9.8130(3)Å, b = 8.8600(5)Å, c = 6.5400(5)Å, V = 568.61(6)Å3, and Z = 4. The structure was solved by direct methods using SHELXS-97 and refined using SHELXL-97. The final residual factor is R1 = 0.0465 for 1726 reflections and 75 parameters. The compound 4-amino-5-(4-chlorophenyl)-4H-[1,2,4]-triazole-3-thiol[ACT], C8H7ClN4S, crystallizes in the triclinic space group with cell parameters a = 8.0440(8)Å, b = 11.527(1)Å, c = 11.7780(7)Å, α = 66.537(6)○, β = 72.990(6)○, γ = 76.001(3)○, V = 948.1(1)Å3, and Z = 4. The structure was solved by direct methods using SHELXS-97 and refined using SHELXL-97. The final residual factor is R1 = 0.0644 for 6805 reflections and 254 parameters.

Synthesis and X-ray crystal studies of 6-(2-chlorophenyl)-3-methyl[1,2,4] triazolo[4,5-6][1,3,4]thiadiazole

The compound 6-(2-chlorophenyl)-3-methyl[1,2,4]triazolo[4,5-b][1,3,4]thiadiazole, was synthesised using different reagents and conditions, characterised by spectroscopic techniques and finally confirmed by X-ray crystal structure analysis. The title compound crystallises in monoclinic class under the space group P21/c with cell parameters, a=10.6710 (6)Å, b=7.3660 (4)Å, c=14.3900 (8)Å, β=110.403 (3)°, Z=2 and R1= 0.0396 for 2715 reflections [I>2ΣI]. The structure exhibits inter-molecular hydrogen bonding.