Biopolym. Cell. 2021; 37(1):33-45.
http://dx.doi.org/10.7124/bc.000A4A
Bioorganic Chemistry
Synthesis and diuretic activity of novel 5-amino-1,3,4-thiadiazole-2-thiol derivatives
1Drapak I. V., 1Zimenkovsky B. S., 1Slabyy M. V., 1, 2Holota S. M., 3Perekhoda L. O., 1Yaremkevych R. V., 1Nektegayev I. O.
  1. Danylo Halytsky Lviv National Medical University
    69, Pekarska Str., Lviv, Ukraine, 79010
  2. Lesya Ukrainka Volyn National University
    13, Voli Ave., Lutsk, Ukraine, 43025
  3. National University of Pharmacy
    53, Pushkinska Str., Kharkiv, Ukraine, 61002

Abstract

Aim. Synthesis, in vivo study and characterization of diuretic activity of novel 5-amino-1,3,4-thiadiazole-2-thiol derivatives. Methods. Organic synthesis (one-pot reaction). 1H NMR spectroscopy. Biological methods: in vivo study on white rats model; urinalysis; saluretic/natriuretic/carbonic anhydrase inhibition indexes; biochemical laboratory tests (ALT, AST, ALP, γ-GGT, total bilirubin and protein levels determination). Results. The series of 5-amino-1,3,4-thiadiazole-2-thiol derivatives have been synthesized using convenient one-pot approach. All compounds were evaluated for their diuretic activity by estimation of total urinary output per day and urinalysis profile. The 5-benzylthio-1,3,4-thiadiazol-2-amine derivatives 2a, 2c and 2e have been found the most active and have been studied for their kaliuretic, saluretic, and natriuretic properties and estimated for carbonic anhydrase inhibition ability. The structure – diuretic activity relationship has been formed. Conclusions. Series of 1,3,4-thiadiazole-bearing derivatives have been designed and synthesized and some derivatives have demonstrated a high level of diuretic action with satisfactory kaliuretic, saluretic, and natriuretic properties.
Keywords: 5-amino-1,3,4-thiadiazole-2-thiol derivatives, diuretic activity, saluretic/natriuretic/carbonic anhydrase inhibition indexes, SAR,
Full text: (PDF, in English)

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